vorinostat [Ligand Id: 6852] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL98 (MK-0683, MK0683, NSC-701852, NSC-748799, NSC-759852, Suberoylanilide hydroxamic acid, Vorinostat, Zolinza) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Apoptosis regulator BAX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5318] [UniProtKB: Q07812] | ||||||||
| ChEMBL | Binding affinity to recombinant human full length His-tagged BAX expressed in Escherichia coli BL21 (DE3) cells preincubated for 30 min followed by FITC-BIM addition and measured after 20 mins by fluorescence polarization assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2020) 63: 12083-12099 [PMID:33021789] |
| Beta amyloid A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067] | ||||||||
| ChEMBL | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation after 24 hrs by thioflavin-T fluorescence method | B | 4.7 | pIC50 | >20000 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of recombinant BRD4 bromodomain 1 (unknown origin) using histone H4 peptide as substrate incubated for 1 hr under dark condition by HTRF assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Medchemcomm (2014) 5: 342-351 |
| ChEMBL | Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of BRD4 in human HL60 cells assessed as reduction in C-myc production after 24 hrs by ELISA | B | 6.13 | pIC50 | 740 | nM | IC50 | Bioorg Med Chem (2017) 25: 3677-3684 [PMID:28549889] |
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
| DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358] | ||||||||
| ChEMBL | Inhibition of human DNMT1 enzyme using polydeoxy-inosine polydeoxy-cytosine DNA as substrate incubated for 15 mins in presence of SAM by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2020) 63: 8977-9002 [PMID:32320239] |
| histone deacetylase 1/HDAC1/REST corepressor 3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296112] [GtoPdb: 2658] [UniProtKB: Q13547, Q9P2K3] | ||||||||
| ChEMBL | Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay | B | 8.52 | pKi | 3.04 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 1001-1004 [PMID:29496367] |
| GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900] | ||||||||
| ChEMBL | Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) after 3 hrs by fluorescence polarization assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 150: 667-677 [PMID:29567459] |
| ChEMBL | Inhibition of HSP90a (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 190: 112086-112086 [PMID:32058238] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by automated patch clamp assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496] |
| ChEMBL | Inhibition of human ERG by automated Q-patch assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2011) 54: 4752-4772 [PMID:21650221] |
| ChEMBL | Inhibition of recombinant human ERG expressed in HEK293 cells at -80 mV holding potential measured for 9 mins by Qpatch clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154] |
| ChEMBL | Inhibition of human ERG | B | 6.49 | pIC50 | 322 | nM | IC50 | Eur J Med Chem (2020) 206: 112677-112677 [PMID:32823005] |
| Histone deacetylase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5541] [UniProtKB: Q9XYC7] | ||||||||
| ChEMBL | Inhibition of Plasmodium falciparum HDAC1 | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2010) 53: 6100-6111 [PMID:20669972] |
| ChEMBL | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells | B | 7.23 | pIC50 | 59 | nM | IC50 | J Med Chem (2009) 52: 2185-2187 [PMID:19317450] |
| Plasmodium falciparum histone deacetylase 1/Histone deacetylase in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293190] [GtoPdb: 3072] [UniProtKB: Q7K6A1] | ||||||||
| ChEMBL | Inhibition of Plasmodium falciparum 3D7 histone deacetylase infected in human erythrocytes assessed as alteration of histone H3 acetylation after 3.5 hrs by SDS-PAGE | B | 7 | pIC50 | 100 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC1 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | B | 7.4 | pKd | 40 | nM | Kd | Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579] |
| ChEMBL | Inhibition of HDAC1 | B | 7.2 | pKi | 63 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC1 | B | 7.32 | pKi | 48 | nM | Ki | J Med Chem (2008) 51: 2898-2906 [PMID:18412327] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 2985-2992 [PMID:30122227] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay | B | 8 | pKi | 10 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| ChEMBL | Inhibition of human recombinant HDAC1 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of recombinant His-tagged human HDAC1 expressed in insect cells assessed as hydrolase activity using fluorogenic Ac-LGK-ac-AMC as substrate measured after 60 mins by fluorescence analysis | B | 8.19 | pKi | 6.4 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
| ChEMBL | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of human HDAC1 | B | 8.89 | pKi | 1.3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of HDAC1 in human COLO205 cells assessed as induction of histone H3 acetylation | B | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of HDAC1 in presence of DTT | B | 6.11 | pIC50 | 775 | nM | IC50 | J Med Chem (2007) 50: 5720-5726 [PMID:17958342] |
| ChEMBL | Inhibition of human recombinant HDAC1 using modified Boc-Lys(Ac)-AMC MAL as substrate after 1 hr by fluorescent activity assay | B | 6.22 | pIC50 | 600 | nM | IC50 | ACS Med Chem Lett (2014) 5: 973-978 [PMID:25221651] |
| ChEMBL | Inhibition of HDAC1 in human 293T cells after 16 hrs by fluorimetry | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 336-340 [PMID:19084395] |
| ChEMBL | Inhibition of Histone deacetylase 1 (HDAC1) of HeLa nuclear extracts | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorimetric assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
| ChEMBL | Inhibition of human recombinant HDAC1 by fluorimetry | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2009) 52: 2909-2922 [PMID:19419205] |
| ChEMBL | Inhibition of human HDAC1 by fluorescence assay | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of full length His-tagged human recombinant HDAC1 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis | B | 6.51 | pIC50 | 310 | nM | IC50 | Eur J Med Chem (2013) 66: 56-68 [PMID:23792316] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 6.51 | pIC50 | 306 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay | B | 6.51 | pIC50 | 306 | nM | IC50 | J Med Chem (2016) 59: 8233-8262 [PMID:27541357] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis | B | 6.51 | pIC50 | 306 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1357-1362 [PMID:29545103] |
| ChEMBL | Inhibition of C-terminal FLAG His tagged full length human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus infected sf21 cells using RHKKAc as substrate in presence of ATP | B | 6.51 | pIC50 | 306 | nM | IC50 | J Med Chem (2017) 60: 8336-8357 [PMID:28953386] |
| ChEMBL | Inhibition of human HDAC1 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | B | 6.51 | pIC50 | 306 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.51 | pIC50 | 306 | nM | IC50 | Eur J Med Chem (2018) 158: 593-619 [PMID:30243158] |
| ChEMBL | Inhibition of human recombinant HDAC1 using histone H3 substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2014) 57: 6259-6265 [PMID:24972008] |
| ChEMBL | Inhibition of HDAC1 by fluorescent activity assay | B | 6.54 | pIC50 | 290 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5735-5738 [PMID:21875796] |
| ChEMBL | Inhibition of HDAC1 by fluorometric assay | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2012) 55: 9562-9575 [PMID:23116147] |
| ChEMBL | Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 (1 to 482 residues) expressed in sf21 cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human recombinant HDAC1 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 6.59 | pIC50 | 260 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of human HDAC-1 using RHKK(Ac) as substrate by fluorescence assay | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.59 | pIC50 | 258 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 6.59 | pIC50 | 258 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC1 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.59 | pIC50 | 258 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of human HDAC-1 using RHKK(Ac) as substrate | B | 6.59 | pIC50 | 258 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC1 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.59 | pIC50 | 258 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human HDAC1 by fluorimetric assay | B | 6.59 | pIC50 | 258 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of Nanoluc-fused HDAC1 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac)AMC as substrate | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2015) 58: 2809-2820 [PMID:25734520] |
| ChEMBL | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate-3 by fluorescence assay | B | 6.63 | pIC50 | 236 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of recombinant human HDAC1 | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 375-379 [PMID:26706171] |
| ChEMBL | Inhibition of full length His6-tagged GST-fused recombinant human HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.68 | pIC50 | 210.98 | nM | IC50 | Eur J Med Chem (2016) 112: 81-90 [PMID:26890114] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis | B | 6.69 | pIC50 | 203.06 | nM | IC50 | Bioorg Med Chem (2015) 23: 4728-4736 [PMID:26100440] |
| ChEMBL | Inhibition of human HDAC1 | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibitory activity against human Histone deacetylase 1 | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2004) 47: 3409-3417 [PMID:15189037] |
| ChEMBL | Inhibition of HDAC1 by in vitro deacetylation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis | B | 6.71 | pIC50 | 196 | nM | IC50 | ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575] |
| ChEMBL | Inhibition of full length recombinant human GST fused His6-tagged HDAC1 expressed in baculovirus infected High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate measured after 24 hrs | B | 6.71 | pIC50 | 195 | nM | IC50 | Eur J Med Chem (2017) 128: 293-299 [PMID:28213282] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate incubated for 24 hrs measured after 30 mins by microplate reader based spectrophotometric analysis | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem (2020) 28: 115639-115639 [PMID:32773090] |
| ChEMBL | Inhibition of recombinant human HDAC1 (482 residues) expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4415-4420 [PMID:28818449] |
| ChEMBL | Inhibition of HDAC1 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2015) 58: 9214-9227 [PMID:26555243] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.72 | pIC50 | 190 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) incubated for 60 mins using microplate reader analysis | B | 6.74 | pIC50 | 180.3 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.74 | pIC50 | 180 | nM | IC50 | Medchemcomm (2014) 5: 342-351 |
| ChEMBL | Inhibition of human recombinant His6-tagged and GST-fuses HDAC1 expressed in insect High5 cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4540-4545 [PMID:22738629] |
| ChEMBL | Inhibition of HDAC1 | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay | B | 6.79 | pIC50 | 162.7 | nM | IC50 | Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2015) 96: 1-13 [PMID:25874326] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2015) 23: 3457-3471 [PMID:25953722] |
| ChEMBL | Inhibition of HDAC 1 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.85 | pIC50 | 142 | nM | IC50 | Eur J Med Chem (2018) 144: 398-409 [PMID:29288941] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | B | 6.85 | pIC50 | 142 | nM | IC50 | Eur J Med Chem (2019) 168: 515-526 [PMID:30851694] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 6.85 | pIC50 | 142 | nM | IC50 | J Nat Prod (2019) 82: 1442-1450 [PMID:31120744] |
| ChEMBL | Inhibition of recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus after 10 mins by fluorimetric analysis | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2021) 64: 10403-10417 [PMID:34185525] |
| ChEMBL | Inhibition of human HDAC1 | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2008) 51: 7417-7427 [PMID:19007204] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.86 | pIC50 | 138.5 | nM | IC50 | Eur J Med Chem (2021) 226: 113870-113870 [PMID:34610548] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 6.87 | pIC50 | 136 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of human recombinant HDAC1 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis | B | 6.88 | pIC50 | 131 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3295-3299 [PMID:23601706] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 60 mins by fluorimetric assay | B | 6.88 | pIC50 | 131 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) | F | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 363-369 [PMID:17107790] |
| ChEMBL | Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments) | F | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 370-375 [PMID:17095213] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay | B | 6.91 | pIC50 | 122 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of HDAC1 | B | 6.92 | pIC50 | 121 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4457-4460 [PMID:26376355] |
| ChEMBL | Inhibition of human recombinant HDAC1 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2021) 64: 14620-14646 [PMID:34582215] |
| ChEMBL | Inhibition of recombinant HDAC1 by fluorimetric assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1403-1408 [PMID:19181524] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 15 mins by fluorimetric assay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2010) 53: 4654-4667 [PMID:20491440] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2013) 21: 3240-3244 [PMID:23602523] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4844-4846 [PMID:21745740] |
| ChEMBL | Inhibition of human recombinant HDAC1 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method | B | 6.92 | pIC50 | 119.5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 671-676 [PMID:30996816] |
| ChEMBL | Inhibition of full length GST-tagged human HDAC1 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | B | 6.92 | pIC50 | 119 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay | B | 6.92 | pIC50 | 119 | nM | IC50 | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Ex vivo inhibition of human HDAC1 in human Caco-2 cells by fluorometric cellular activity assay | B | 6.92 | pIC50 | 119 | nM | IC50 | J Med Chem (2010) 53: 1937-1950 [PMID:20143840] |
| ChEMBL | Inhibition of full length FLAG-tagged recombinant HDAC1 (unknown origin) transfected in human HeLa cells assessed as deacetylation of [3H]-acetylated histones after 2 hrs by scintillation counting analysis | B | 6.92 | pIC50 | 119 | nM | IC50 | J Med Chem (2013) 56: 7201-7211 [PMID:23964961] |
| ChEMBL | Inhibition of human HDAC1 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | B | 6.92 | pIC50 | 119 | nM | IC50 | J Med Chem (2016) 59: 1545-1555 [PMID:26653328] |
| ChEMBL | Inhibition of recombinant C-terminal His/FLAG-tagged human HDAC1 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay | B | 6.93 | pIC50 | 117 | nM | IC50 | J Med Chem (2019) 62: 1138-1166 [PMID:30645113] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition measured after 20 mins by fluorescence assay | B | 6.93 | pIC50 | 117 | nM | IC50 | J Med Chem (2016) 59: 2423-2435 [PMID:26937828] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL as substrate incubated for 90 mins by fluorescence assay | B | 6.95 | pIC50 | 111 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| ChEMBL | Inhibition of C-terminal His/FLAG-tagged full length recombinant human HDAC1 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2016) 122: 92-101 [PMID:27344487] |
| ChEMBL | Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of recombinant human full length HDAC1 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
| ChEMBL | Inhibition of HDAC1 by fluorometric assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6200-6204 [PMID:22932316] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using substrate after 30 mins by fluorometric analysis | B | 6.97 | pIC50 | 106 | nM | IC50 | Eur J Med Chem (2017) 133: 11-23 [PMID:28371677] |
| ChEMBL | Inhibition of recombinant human HDAC1 using fluorogenic substrate by fluorescence assay | B | 6.99 | pIC50 | 101.98 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay | B | 7 | pIC50 | 101 | nM | IC50 | Medchemcomm (2019) 10: 1109-1115 [PMID:31391882] |
| ChEMBL | Inhibition of recombinant human HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem (2018) 26: 4706-4715 [PMID:30115492] |
| ChEMBL | Inhibition of human recombinant C-terminal FLAG-tagged HDAC1 expressed in baculovirus by fluorimetry | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 336-340 [PMID:19084395] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC1 (482 residues) expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.01 | pIC50 | 98.13 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC1 | B | 7.02 | pIC50 | 96 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863] |
| ChEMBL | Inhibition of HDAC1 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 7.02 | pIC50 | 96 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of HDAC1 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | B | 7.02 | pIC50 | 96 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7084-7086 [PMID:23089527] |
| ChEMBL | Inhibition of HDAC1 after 30 mins by Fluor de Lys fluorescence assay | B | 7.02 | pIC50 | 96 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6139-6142 [PMID:21889343] |
| ChEMBL | Inhibition of HDAC1 after 17 hrs | B | 7.02 | pIC50 | 96 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 7.03 | pIC50 | 93.6 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of human recombinant full length HDAC1 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins | B | 7.03 | pIC50 | 93.34 | nM | IC50 | Bioorg Med Chem (2014) 22: 6146-6155 [PMID:25261927] |
| ChEMBL | Inhibition of recombinant His6-tagged GST-fused human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs | B | 7.03 | pIC50 | 93.34 | nM | IC50 | Bioorg Med Chem (2015) 23: 5881-5890 [PMID:26211462] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay | B | 7.04 | pIC50 | 91 | nM | IC50 | Medchemcomm (2015) 6: 1816-1825 |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem (2013) 21: 6981-6995 [PMID:24095018] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of recombinant human full length C-terminal Flag/His-tagged HDAC1 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method | B | 7.05 | pIC50 | 89 | nM | IC50 | Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257] |
| ChEMBL | Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay | B | 7.05 | pIC50 | 88.5 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 7.06 | pIC50 | 87.9 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 7.06 | pIC50 | 87.4 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-pNA as substrate preincubated for 20 mins followed by substrate addition and further incubated for 90 mins by fluorescence assay | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2020) 63: 6959-6978 [PMID:32551649] |
| ChEMBL | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.09 | pIC50 | 81 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2021) 64: 4020-4033 [PMID:33745280] |
| ChEMBL | Inhibition of purified recombinant HDAC1 | B | 7.11 | pIC50 | 77 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4909-4912 [PMID:21742496] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | B | 7.12 | pIC50 | 76 | nM | IC50 | ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Cbz-Lys(TFAc)-AMC as substrate by fluorometric analysis | B | 7.12 | pIC50 | 76 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 7.14 | pIC50 | 71.8 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of recombinant HDAC1 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 7.16 | pIC50 | 69 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.16 | pIC50 | 69 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of human recombinant full-length HDAC1 (1 to 482 residues) expressed in baculovirus using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.16 | pIC50 | 69 | nM | IC50 | Eur J Med Chem (2017) 141: 596-602 [PMID:29102179] |
| ChEMBL | Inhibition of human recombinant HDAC1 | B | 7.17 | pIC50 | 68.1 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of HDAC1 | B | 7.17 | pIC50 | 68 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.18 | pIC50 | 65.4 | nM | IC50 | Eur J Med Chem (2015) 89: 628-637 [PMID:25462271] |
| ChEMBL | Inhibition of human HDAC1 using H3(1-21)K9 after 60 mins by fluorescence assay | B | 7.19 | pIC50 | 65.2 | nM | IC50 | J Nat Prod (2017) 80: 201-204 [PMID:28026946] |
| ChEMBL | Inhibition of human HDAC1 after 30 mins by microplate reader analysis | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127023-127023 [PMID:32067866] |
| ChEMBL | Inhibition of C-terminal FLAG/His-tagged full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 7.2 | pIC50 | 63.5 | nM | IC50 | Eur J Med Chem (2018) 143: 792-805 [PMID:29223096] |
| ChEMBL | Inhibition of HDAC1 using KI-177 as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | B | 7.2 | pIC50 | 62.9 | nM | IC50 | Eur J Med Chem (2011) 46: 4042-4049 [PMID:21712146] |
| ChEMBL | Inhibition of human HDAC1 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) measured after 30 mins by fluorescence assay | B | 7.21 | pIC50 | 61 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462] |
| ChEMBL | Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | B | 7.25 | pIC50 | 56 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) by fluorescence based assay | B | 7.26 | pIC50 | 54.6 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.28 | pIC50 | 52 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111] |
| ChEMBL | Inhibition of recombinant full length human HDAC1 (1 to 482 amino acids) expressed in Baculovirus infected insect Sf9 cells incubated for 30 mins measured by fluorescence assay | B | 7.29 | pIC50 | 51 | nM | IC50 | Medchemcomm (2014) 5: 1887-1891 |
| ChEMBL | Inhibition of HDAC1 in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate measured after 2 hrs by fluorescence based assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 7.31 | pIC50 | 49 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Inhibition of human HDAC 1 | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3969-3971 [PMID:17507219] |
| ChEMBL | Inhibition of HDAC1 | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2008) 51: 7053-7056 [PMID:18942826] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | Eur J Med Chem (2020) 185: 111725-111725 [PMID:31655430] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 15 mins by fluorogenic assay | B | 7.32 | pIC50 | 47.4 | nM | IC50 | J Med Chem (2015) 58: 4550-4572 [PMID:25993269] |
| ChEMBL | Inhibition of full length recombinant FLAG/His-tagged C-terminal human HDAC1 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay | B | 7.33 | pIC50 | 47 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1336-1340 [PMID:31531206] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.34 | pIC50 | 46 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | B | 7.34 | pIC50 | 45.5 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant full length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2017) 60: 5334-5348 [PMID:28581289] |
| ChEMBL | Inhibition of C-terminal FLAG/His-tagged recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2017) 60: 5493-5506 [PMID:28574690] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154] |
| ChEMBL | Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mins by HTRF assay | B | 7.36 | pIC50 | 44 | nM | IC50 | ACS Med Chem Lett (2017) 8: 830-834 [PMID:28835797] |
| ChEMBL | Inhibition of human HDAC1 expressed in Escherichia coli using fluorogenic substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay | B | 7.36 | pIC50 | 44 | nM | IC50 | Eur J Med Chem (2011) 46: 5387-5397 [PMID:21924799] |
| ChEMBL | Inhibition of full length human C-terminal His-tagged/C-terminal Flag-tagged HDAC1 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 7.36 | pIC50 | 43.9 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 7.36 | pIC50 | 43.76 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.37 | pIC50 | 43 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.37 | pIC50 | 42.5 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Bioorg Med Chem (2020) 28: 115345-115345 [PMID:32061484] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 30 mins by fluorescence assay | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 5782-5796 [PMID:23786452] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2638-2645 [PMID:31400938] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.38 | pIC50 | 42 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC1 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of human full-length recombinant HDAC1 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of full length human recombinant HDAC1 expressed in baculovirus expression system using (Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2018) 61: 6056-6074 [PMID:29940115] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.4 | pIC50 | 39.8 | nM | IC50 | J Med Chem (2020) 63: 12083-12099 [PMID:33021789] |
| ChEMBL | Inhibition of full length human recombinant HDAC1 expressed in baculovirus using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3283-3287 [PMID:23622981] |
| ChEMBL | Inhibition of His-tagged HDAC1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2015) 96: 340-359 [PMID:25899338] |
| ChEMBL | Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2013) 56: 9969-9981 [PMID:24304348] |
| ChEMBL | Inhibition of HDAC1 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2012) 55: 1465-1477 [PMID:22260166] |
| ChEMBL | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Boc-Lys (Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) at 10 uM after 60 mins by SAMDI spectrophotometric analysis relative to control | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2013) 56: 3492-3506 [PMID:23547652] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 7.42 | pIC50 | 37.7 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127638-127638 [PMID:33132117] |
| ChEMBL | Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.46 | pIC50 | 34.6 | nM | IC50 | J Med Chem (2014) 57: 3324-3341 [PMID:24694055] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 3 hrs measured after 35 mins by spectrofluorometric analysis | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007] |
| ChEMBL | Inhibition of human recombinant HDAC1 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2015) 58: 4812-4821 [PMID:25974739] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in Escherichia coli BL21(DE3) cells using KL177 as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay | B | 7.47 | pIC50 | 33.5 | nM | IC50 | ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375] |
| ChEMBL | Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | B | 7.48 | pIC50 | 33 | nM | IC50 | ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) by ELISA-based assay | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461] |
| ChEMBL | Inhibition of HADC1 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC1 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330] |
| ChEMBL | Inhibition of recombinant HDAC1 expressed in HEK293 cells | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2008) 51: 3985-4001 [PMID:18558669] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2021) 47: 128207-128207 [PMID:34146703] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC1 expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.49 | pIC50 | 32.33 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2019) 62: 6992-7014 [PMID:31117517] |
| ChEMBL | Inhibition of HDAC1 in human HeLa cells after 72 hrs by ELISA | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2018) 146: 79-92 [PMID:29396364] |
| ChEMBL | Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1031-1036 [PMID:29057046] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 744-749 [PMID:28131715] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of human recombinant C-terminally flag tagged HDAC1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| ChEMBL | Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of HDAC1 | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of HDAC1 in HEK293 cells | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of human HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of HDAC1 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2012) 55: 1731-1750 [PMID:22280363] |
| ChEMBL | Inhibition of human recombinant HDAC1 using fluor de Lys as substrate by fluorometric analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 8663-8678 [PMID:21080647] |
| ChEMBL | Inhibition of human recombinant full length HDAC1 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007] |
| ChEMBL | Inhibition of recombinant human HDAC1 expressed in baculovirus expression system using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
| ChEMBL | Inhibition of HDAC1 (mean IC50) | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5948-5952 [PMID:16987657] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2018) 61: 3166-3192 [PMID:29518312] |
| ChEMBL | Inhibition of HDAC1 by fluorogenic enzyme assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
| ChEMBL | Inhibition of human recombinant HDAC1 (1 to 482 residues) expressed in Baculovirus using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of recombinant full length human C-terminal His/flag-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | B | 7.59 | pIC50 | 26 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) incubated for 30 mins by microplate reader assay | B | 7.59 | pIC50 | 25.8 | nM | IC50 | Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595] |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence based protease coupled assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Medchemcomm (2019) 10: 1828-1837 [PMID:32180916] |
| ChEMBL | Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.6 | pIC50 | 25 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of full-length recombinant human HDAC1 expressed in Baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based microtiter plate reader assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2022) 65: 4818-4831 [PMID:35238576] |
| ChEMBL | Inhibition of recombinant full length human HDAC1 (1 to 482) expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139] |
| ChEMBL | Inhibition of human HDAC1 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | B | 7.64 | pIC50 | 22.7 | nM | IC50 | J Med Chem (2021) 64: 1116-1126 [PMID:33356256] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.65 | pIC50 | 22.4 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of recombinant human FLAG/His-tagged HDAC1 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay | B | 7.65 | pIC50 | 22.4 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC1 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7.65 | pIC50 | 22.37 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| ChEMBL | Inhibition of HDAC1 | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in HEK293 cells | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2010) 53: 8546-8555 [PMID:21080629] |
| ChEMBL | Inhibition of human recombinant HDAC1 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2018) 61: 3779-3798 [PMID:29039662] |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7.68 | pIC50 | 20.9 | nM | IC50 | US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016) |
| ChEMBL | Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis | B | 7.68 | pIC50 | 20.9 | nM | IC50 | J Med Chem (2013) 56: 3645-3655 [PMID:23570542] |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7.68 | pIC50 | 20.9 | nM | IC50 | US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015) |
| ChEMBL | Inhibition of recombinant HDAC1 in HeLa cells | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2007) 50: 4405-4418 [PMID:17691763] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in HEK293 cells | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2009) 52: 2265-2279 [PMID:19301902] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452] |
| ChEMBL | Inhibition of recombinant human HDAC1 using Ac-LGK(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 90 mins by fluorescence based assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2021) 64: 2186-2204 [PMID:33570940] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged human HDAC1 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2021) 213: 113173-113173 [PMID:33493830] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys (Ac)-AMC as substrate measured after 60 mins by ELISA | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 15-21 [PMID:30455152] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader | B | 7.84 | pIC50 | 14.6 | nM | IC50 | J Med Chem (2021) 64: 16573-16597 [PMID:34783558] |
| ChEMBL | Inhibition of recombinant human full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | B | 7.84 | pIC50 | 14.4 | nM | IC50 | ACS Med Chem Lett (2018) 9: 312-317 [PMID:29670692] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.84 | pIC50 | 14.3 | nM | IC50 | Bioorg Med Chem (2018) 26: 3958-3966 [PMID:29954683] |
| ChEMBL | Inhibition of human C-terminal Flag tagged HDAC1 (1 to 482 residues) expressed in SF9 cells using Ac-peptide substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by microplate reader method | B | 7.85 | pIC50 | 14.15 | nM | IC50 | Eur J Med Chem (2020) 204: 112651-112651 [PMID:32738414] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.85 | pIC50 | 14.15 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127610-127610 [PMID:33045329] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| ChEMBL | Inhibition of human recombinant HDAC1 by microplate reader assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Medchemcomm (2015) 6: 613-618 [PMID:26005563] |
| ChEMBL | Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2020) 192: 112189-112189 [PMID:32151834] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Boc-Lys(Ac)-AMC as substrate by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4768-4772 [PMID:25182565] |
| ChEMBL | Inhibition of human recombinant HDAC1 expressed in human HEK293 cells using Ac-NH-GGK(Ac)-AMC as substrate after 180 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Medchemcomm (2012) 3: 829-835 |
| ChEMBL | Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by addition of substrate and trypsin measured by flourescence assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | B | 7.95 | pIC50 | 11.34 | nM | IC50 | Bioorg Med Chem (2017) 25: 4100-4109 [PMID:28601509] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 7.95 | pIC50 | 11.11 | nM | IC50 | Eur J Med Chem (2017) 134: 281-292 [PMID:28419930] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844] |
| ChEMBL | Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2016) 59: 5488-5504 [PMID:27186676] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His/FLAG tagged HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2022) 65: 4156-4181 [PMID:35175762] |
| ChEMBL | Inhibition of recombinant full length HDAC1 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of HDAC1 | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | B | 7.97 | pIC50 | 10.8 | nM | IC50 | Bioorg Med Chem (2017) 25: 27-37 [PMID:27769671] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human HDAC1 after 30 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4051-4055 [PMID:28765013] |
| ChEMBL | Inhibition of C-terminal FLAG/His-tagged human recombinant HDAC1 (1 to 482 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release using fluorogenic HDAC substrate 3 measured every 5 mins by fluorescence based analysis | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2019) 183: 111691-111691 [PMID:31536895] |
| ChEMBL | Inhibition of HDAC1 in human Jurkat cells extract after 30 mins by immunoprecipitation assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3122-3126 [PMID:27177826] |
| ChEMBL | Inhibition of recombinant human GST-fused HDAC1 expressed in HEK293 cells Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant full-length HDAC1 using fluorophore conjugated substrate by fluorescence assay | B | 8.01 | pIC50 | 9.7 | nM | IC50 | J Med Chem (2011) 54: 5576-5582 [PMID:21721525] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630] |
| ChEMBL | Inhibition of human recombinant HDAC1 after 30 mins by fluorometric assay | B | 8.05 | pIC50 | 8.9 | nM | IC50 | J Med Chem (2012) 55: 3777-3791 [PMID:22439863] |
| ChEMBL | Inhibition of human recombinant HDAC1 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1265-1271 [PMID:26804233] |
| ChEMBL | Inhibition of human KDAC1 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | J Med Chem (2022) 65: 3667-3683 [PMID:35152694] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using Fluor de Lys substrate by fluorescence assay relative to control | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2019) 168: 110-122 [PMID:30802729] |
| histone deacetylase 1/Histone deacetylase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4001] [GtoPdb: 2658] [UniProtKB: O09106] | ||||||||
| ChEMBL | Binding affinity towards HDAC1 (Histone deacetylase 1) in mouse A20 cells, expressed as binding constant (pKi) | B | 7.17 | pKi | 67.61 | nM | Ki | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
| ChEMBL | Inhibition of mouse HDAC1 | B | 6.95 | pIC50 | 112.2 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
| ChEMBL | In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
| ChEMBL | Inhibition of mouse Histone deacetylase 1 (HDAC1) receptor | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
| ChEMBL | Inhibition of mouse HDAC1 | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
| ChEMBL | Inhibition of mouse liver HDAC1 | B | 6.95 | pIC50 | 112 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| GtoPdb | - | - | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378] |
| ChEMBL | Inhibition of HDAC10 | B | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of human recombinant HDAC10 using Ac-Arg-His-Lys (Ac)-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay | B | 7.4 | pKi | 40 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| ChEMBL | Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay | B | 5.9 | pIC50 | 1258.93 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| ChEMBL | Inhibition of HDAC 10 in human HeLa nuclear extract measured after 60 mins by fluorometric analysis | B | 6.01 | pIC50 | 982 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of human recombinant HDAC10 after 60 mins by fluorimetric assay | B | 6.16 | pIC50 | 686 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay | B | 6.16 | pIC50 | 686 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of human HDAC10 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.34 | pIC50 | 460 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.34 | pIC50 | 456 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of human HDAC10 by fluorimetric assay | B | 6.34 | pIC50 | 456 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC-10 using RHKK(Ac) as substrate by fluorescence assay | B | 6.34 | pIC50 | 456 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC-10 using RHKK(Ac) as substrate | B | 6.34 | pIC50 | 456 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 6.34 | pIC50 | 456 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC10 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.34 | pIC50 | 456 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC10 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.34 | pIC50 | 456 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 6.36 | pIC50 | 432 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.37 | pIC50 | 430 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.37 | pIC50 | 430 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 6.56 | pIC50 | 278 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of HDAC10 | B | 6.68 | pIC50 | 210 | nM | IC50 | Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529] |
| ChEMBL | Inhibition of recombinant N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 6.68 | pIC50 | 208 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of HDAC10 by in vitro deacetylation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay | B | 6.7 | pIC50 | 199.53 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| ChEMBL | Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of human HDAC10 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) by fluorescence assay | B | 7.01 | pIC50 | 97 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 7.04 | pIC50 | 91.8 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) using Ac-ArgThr- Lys(Ac)Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.1 | pIC50 | 80 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of recombinant human N-terminal FLAG-tagged HDAC10 (2 to 631 residues) expressed in baculovirus infected using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 7.11 | pIC50 | 77 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC10 after 17 hrs | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of human recombinant HDAC10 | B | 7.14 | pIC50 | 72 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863] |
| ChEMBL | Inhibition of HDAC10 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of N-terminal GST-tagged human HDAC10 (1 to 481 residues) using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | B | 7.14 | pIC50 | 72 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of recombinant HDAC10 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 7.15 | pIC50 | 70 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 7.16 | pIC50 | 68.4 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 7.19 | pIC50 | 64 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of recombinant human HDAC10 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.24 | pIC50 | 58 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC10 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.24 | pIC50 | 57.25 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of human recombinant HDAC10 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Inhibition of recombinant HDAC10 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | B | 7.32 | pIC50 | 47.5 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of human recombinant HDAC11 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay | B | 7.22 | pKi | 60 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| GtoPdb | - | - | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378] |
| ChEMBL | Inhibition of HDAC11 | B | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay | B | 7.51 | pKi | 31 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of recombinant human HDAC11 enzyme using Ac-LeuGlyLys(Ac)-AMC as substrate after 15 to 30 mins | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of human recombinant HDAC11 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2A by fluorescence assay | B | 4.13 | pIC50 | 73770 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 4.4 | pIC50 | 40000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of recombinant human HDAC11 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 4.9 | pIC50 | 12542 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| ChEMBL | Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of HDAC 11 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 cells measured after 60 mins by FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 4020-4033 [PMID:33745280] |
| ChEMBL | Inhibition of recombinant full-length human HDAC11 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 5.06 | pIC50 | 8700 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC11 after 60 mins by fluorimetric assay | B | 5.23 | pIC50 | 5840 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of recombinant human HDAC11 measured after 30 mins by fluorescence microplate reader assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC11 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of human HDAC11 by fluorescence assay | B | 6.32 | pIC50 | 480 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of His-tagged human HDAC11 expressed in Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate by fluorometric assay | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2434-2437 [PMID:27055940] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 6.44 | pIC50 | 362 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC11 by fluorimetric assay | B | 6.44 | pIC50 | 362 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.44 | pIC50 | 362 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC11 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.44 | pIC50 | 362 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human HDAC-11 using RHKK(Ac) as substrate by fluorescence assay | B | 6.44 | pIC50 | 362 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC-11 using RHKK(Ac) as substrate | B | 6.44 | pIC50 | 362 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC11 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.44 | pIC50 | 362 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of human recombinant N-terminal His-tagged HDAC11 (1 to 347 residues) using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.44 | pIC50 | 360 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 6.7 | pIC50 | 200 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2943-2945 [PMID:28501514] |
| ChEMBL | Inhibition of recombinant human HDAC11 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 6.88 | pIC50 | 133 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of human HDAC11 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of recombinant HDAC11 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of HDAC11 (unknown origin) | B | 7.29 | pIC50 | 51.3 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect S9 cells after 30 mins by fluorescence assay | B | 7.46 | pIC50 | 34.5 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant human HDAC2 | B | 7.05 | pKi | 90 | nM | Ki | Bioorg Med Chem (2020) 28: 115108-115108 [PMID:31787463] |
| ChEMBL | Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay | B | 7.38 | pKi | 42 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC2 | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay | B | 8.1 | pKi | 8 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| ChEMBL | Inhibition of human recombinant HDAC2 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of recombinant human HDAC2 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of His-tagged recombinant human HDAC2 expressed in insect cells assessed as hydrolase activity using fluorogenic AC-LGK-ac-AMC as substrate measured after 60 mins by fluorescence analysis | B | 8.38 | pKi | 4.2 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
| ChEMBL | Inhibition of human HDAC2 | B | 8.8 | pKi | 1.6 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| GtoPdb | - | - | 8.8 | pKi | 1.6 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.04 | pIC50 | 921 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC2 by fluorimetric assay | B | 6.04 | pIC50 | 921 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 6.04 | pIC50 | 921 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC-2 using RHKK(Ac) as substrate | B | 6.04 | pIC50 | 921 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC2 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.04 | pIC50 | 921 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of human HDAC2 by fluorescence assay | B | 6.04 | pIC50 | 920 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of human HDAC-2 using RHKK(Ac) as substrate by fluorescence assay | B | 6.04 | pIC50 | 920 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human recombinant full length HDAC2 using (Ac)Arg-Gly-Lys(Ac) as substrate after 60 mins by fluorescence assay | B | 6.04 | pIC50 | 920 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant HDAC2 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 6.04 | pIC50 | 920 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of HDAC2 by fluorometric assay | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (2012) 55: 9562-9575 [PMID:23116147] |
| ChEMBL | Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) by fluorimetric assay | B | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
| ChEMBL | Inhibition of C-terminal His-tagged full length human recombinant HDAC2 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis | B | 6.27 | pIC50 | 537 | nM | IC50 | ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575] |
| ChEMBL | Inhibition of HDAC 2 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | B | 6.34 | pIC50 | 454 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate-3 by fluorescence assay | B | 6.39 | pIC50 | 411 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of HDAC2 by in vitro deacetylation assay | B | 6.4 | pIC50 | 400 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of HDAC2 | B | 6.41 | pIC50 | 390 | nM | IC50 | Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529] |
| ChEMBL | Inhibition of recombinant human HDAC2 using fluorogenic substrate by fluorescence assay | B | 6.48 | pIC50 | 332.65 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of HDAC2 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 6.55 | pIC50 | 282 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of HDAC2 after 17 hrs | B | 6.55 | pIC50 | 282 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of human recombinant HDAC2 | B | 6.55 | pIC50 | 282 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2015) 96: 1-13 [PMID:25874326] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem (2015) 23: 3457-3471 [PMID:25953722] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 24 hrs measured after 35 mins by spectrofluorometric analysis | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | B | 6.59 | pIC50 | 256 | nM | IC50 | ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449] |
| ChEMBL | Inhibition of human recombinant HDAC2 by fluorimetry | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2009) 52: 2909-2922 [PMID:19419205] |
| ChEMBL | Inhibition of human HDAC2 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2021) 64: 10403-10417 [PMID:34185525] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 6.63 | pIC50 | 232 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His- tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluorometric substrate measured after 60 mins by FRET assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2021) 64: 4020-4033 [PMID:33745280] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic HDAC substrate 3 incubated for 30 mins by fluorescence based assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2019) 62: 3898-3923 [PMID:30901208] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2018) 61: 5304-5322 [PMID:29787262] |
| ChEMBL | Inhibition of full length recombinant human HDAC2 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 6.67 | pIC50 | 214 | nM | IC50 | Eur J Med Chem (2018) 143: 792-805 [PMID:29223096] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 6.67 | pIC50 | 213 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC2 after 10 mins by fluorometric assay | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem (2010) 18: 4119-4137 [PMID:20452225] |
| ChEMBL | Inhibition of full length human HDAC2 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 6.7 | pIC50 | >200 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2017) 60: 5493-5506 [PMID:28574690] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Boc-L-Lys (Ac)-AMC as substrate preincubated with compound for 5 mins measured after 35 mins by spectrofluorometric analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5025-5030 [PMID:22771007] |
| ChEMBL | Inhibition of recombinant C-terminal FLAG-tagged HDAC2 expressed in baculovirus after 10 mins by fluorimetric analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 24 hrs and measured after 60 mins by fluorescence assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.71 | pIC50 | 197 | nM | IC50 | Eur J Med Chem (2016) 108: 53-67 [PMID:26629860] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.71 | pIC50 | 197 | nM | IC50 | Eur J Med Chem (2013) 64: 273-284 [PMID:23644210] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay | B | 6.71 | pIC50 | 193 | nM | IC50 | Medchemcomm (2015) 6: 1816-1825 |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 6.73 | pIC50 | 184.7 | nM | IC50 | J Med Chem (2014) 57: 3324-3341 [PMID:24694055] |
| ChEMBL | Inhibition of recombinant human full length C-terminal Flag-tagged HDAC2 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method | B | 6.74 | pIC50 | 183 | nM | IC50 | Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257] |
| ChEMBL | Inhibition of human recombinant HDAC2 after 60 mins by fluorimetric assay | B | 6.74 | pIC50 | 182 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
| ChEMBL | Inhibition of HDAC2 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human HDAC2 preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4415-4420 [PMID:28818449] |
| ChEMBL | Inhibition of recombinant HDAC2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 6.74 | pIC50 | 180 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.75 | pIC50 | 178 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of human HDAC2 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm | B | 6.75 | pIC50 | 178 | nM | IC50 | J Med Chem (2021) 64: 14620-14646 [PMID:34582215] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 6.75 | pIC50 | 176 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.76 | pIC50 | 174.6 | nM | IC50 | Eur J Med Chem (2015) 89: 628-637 [PMID:25462271] |
| ChEMBL | Inhibition of recombinant C-terminal His-tagged full length human HDAC2 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | B | 6.76 | pIC50 | 174 | nM | IC50 | ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) measured after 30 mins by fluorescence assay | B | 6.76 | pIC50 | 173 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of HDAC2 | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) incubated for 30 mins by microplate reader assay | B | 6.78 | pIC50 | 167 | nM | IC50 | Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595] |
| ChEMBL | Inhibition of recombinant human HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 6.78 | pIC50 | 166 | nM | IC50 | Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490] |
| ChEMBL | Inhibition of HDAC2 | B | 6.79 | pIC50 | 164 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Inhibition of full length C-terminal 6x-His tagged human HDAC2 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | B | 6.79 | pIC50 | 164 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of human recombinant HDAC2 | B | 6.79 | pIC50 | 163.6 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.81 | pIC50 | 156 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) after 30 mins by fluorescence assay | B | 6.82 | pIC50 | 153.1 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| ChEMBL | Inhibition of human HDAC2 after 40 mins by fluorescence analysis | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4457-4460 [PMID:26376355] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 6.83 | pIC50 | 149 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay | B | 6.84 | pIC50 | 146 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462] |
| ChEMBL | Inhibition of recombinant human full-length HDAC2 expressed in baculovirus expression system using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 6.85 | pIC50 | 140 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human HDAC2 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 6.87 | pIC50 | 135 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 6.89 | pIC50 | 128.9 | nM | IC50 | J Med Chem (2020) 63: 12083-12099 [PMID:33021789] |
| ChEMBL | Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay | B | 6.92 | pIC50 | 120.5 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 6.92 | pIC50 | 120 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of recombinant human full length HDAC2 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
| ChEMBL | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2016) 122: 92-101 [PMID:27344487] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 6.93 | pIC50 | 118 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | B | 6.95 | pIC50 | 112.5 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of recombinant human full length C-terminal GST-fusion tagged HDAC2 expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry | B | 6.97 | pIC50 | 107 | nM | IC50 | Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis | B | 7 | pIC50 | 100.9 | nM | IC50 | J Med Chem (2013) 56: 3645-3655 [PMID:23570542] |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7 | pIC50 | 100.9 | nM | IC50 | US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015) |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7 | pIC50 | 100.9 | nM | IC50 | US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016) |
| ChEMBL | Inhibition of human recombinant HDAC2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC after 60 mins | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| ChEMBL | Inhibition of HDAC2 in human HeLa cells | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2009) 44: 1900-1912 [PMID:19084294] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Fluor de Lys Green as substrate incubated for 30 mins by fluorescence assay | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of HDAC2 in human HeLa cells using KI-104 as substrate after 40 mins by fluorescence analysis | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) by ELISA-based assay | B | 7.02 | pIC50 | 96 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461] |
| ChEMBL | Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | B | 7.02 | pIC50 | 96 | nM | IC50 | ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317] |
| ChEMBL | Inhibition of HDAC2 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | B | 7.02 | pIC50 | 96 | nM | IC50 | Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330] |
| ChEMBL | Inhibition of HADC2 (unknown origin) | B | 7.02 | pIC50 | 96 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of full length human C-terminal His-tagged HDAC2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 7.03 | pIC50 | 93.6 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of human recombinant full-length C-terminal GST-tagged HDAC2 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.04 | pIC50 | 91.6 | nM | IC50 | Eur J Med Chem (2017) 141: 596-602 [PMID:29102179] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to 488 residues) expressed in Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111] |
| ChEMBL | Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 7.05 | pIC50 | 89.23 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
| ChEMBL | Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay | B | 7.07 | pIC50 | 85.8 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| ChEMBL | Inhibition of C-terminal FLAG tagged HDAC2 | B | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459] |
| ChEMBL | Inhibition of HDAC2 | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of HDAC2 | B | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| ChEMBL | Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of human full-length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.09 | pIC50 | 81.28 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of C-terminal GST-tagged human recombinant HDAC2 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis | B | 7.09 | pIC50 | 81 | nM | IC50 | Bioorg Med Chem (2016) 24: 1446-1454 [PMID:26907204] |
| ChEMBL | Inhibition of HDAC2 in human HeLa cells after 72 hrs by ELISA | B | 7.09 | pIC50 | 81 | nM | IC50 | Eur J Med Chem (2018) 146: 79-92 [PMID:29396364] |
| ChEMBL | Inhibition of human recombinant HDAC2 preincubated for 1 hr with substrate by protease coupled end-point assay | B | 7.12 | pIC50 | 76 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3142-3145 [PMID:20392638] |
| ChEMBL | Inhibition of Histone deacetylase 2 (HDAC2) activity of HeLa nuclear extracts | B | 7.14 | pIC50 | 73 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179] |
| ChEMBL | Inhibition of human recombinant HDAC2 preincubated for 24 hrs followed by 1 hr reaction with substrate by protease coupled end-point assay | B | 7.14 | pIC50 | 72 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3142-3145 [PMID:20392638] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC2 (1 to end residues) expressed in sf9 insect cells using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2020) 192: 112189-112189 [PMID:32151834] |
| ChEMBL | Inhibition of full length HDAC2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | B | 7.18 | pIC50 | 66 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2601-2605 [PMID:21334896] |
| ChEMBL | Inhibition of recombinant human HDAC2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.18 | pIC50 | 66 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.25 | pIC50 | 56 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of human recombinant HDAC2 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2015) 58: 4812-4821 [PMID:25974739] |
| ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.29 | pIC50 | 51 | nM | IC50 | Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452] |
| ChEMBL | Inhibition of HDAC2 in HeLa cell lysates | B | 7.3 | pIC50 | >=50 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6261-6265 [PMID:17892933] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| ChEMBL | Inhibition of HDAC2 | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of human full-length recombinant HDAC2 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127537-127537 [PMID:32916298] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 15 to 30 mins | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2018) 61: 3779-3798 [PMID:29039662] |
| ChEMBL | Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of C-terminal His-tagged full length human HDAC2 expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| ChEMBL | Inhibition of human HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.57 | pIC50 | 27 | nM | IC50 | Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | B | 7.59 | pIC50 | 26 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of human recombinant HDAC2 using fluor de Lys as substrate by fluorometric analysis | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2010) 53: 8663-8678 [PMID:21080647] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His tagged HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs | B | 7.62 | pIC50 | 23.8 | nM | IC50 | J Med Chem (2022) 65: 4156-4181 [PMID:35175762] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using Ac-Leu-GlyLys(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by fluorescence analysis | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2017) 25: 4123-4132 [PMID:28629630] |
| ChEMBL | Inhibition of human recombinant full-length HDAC2 using fluorophore conjugated substrate by fluorescence assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2011) 54: 5576-5582 [PMID:21721525] |
| ChEMBL | Inhibition of human recombinant HDAC2 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2021) 213: 113173-113173 [PMID:33493830] |
| ChEMBL | Inhibition of C-terminal 6XHis-tagged human recombinant full length HDAC2 (1 to 488 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2022) 65: 3667-3683 [PMID:35152694] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of human recombinant HDAC2 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | B | 7.99 | pIC50 | 10.2 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1265-1271 [PMID:26804233] |
| ChEMBL | Inhibition of HDAC2 (unknown origin)-mediated deacetylation preincubated for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2013) 56: 7997-8007 [PMID:24074025] |
| ChEMBL | Inhibition of human recombinant HDAC2 after 30 mins by fluorometric assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2012) 55: 3777-3791 [PMID:22439863] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC3 | B | 7.54 | pKi | 29 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of human recombinant HDAC3 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of human C-terminal His-tagged HDAC3 (1 to 428 residues)/human N-terminal GST-tagged NcoR2 (395 to 489 residues) expressed in sf9 cells using acetyl-Lys(Ac)-AMC as substrate | B | 8.1 | pKi | 8 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC3 | B | 8.3 | pKi | 5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human HDAC3 using fluorogenic HDAC substrate after 30 mins by fluorescence analysis | B | 6.29 | pIC50 | 517 | nM | IC50 | Bioorg Med Chem (2018) 26: 5718-5729 [PMID:30385227] |
| ChEMBL | Inhibition of human full-length recombinant HDAC3 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 6.34 | pIC50 | 460 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of human recombinant HDAC3 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 6.46 | pIC50 | 350 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of human HDAC3 complexed with NCOR2 using fluorogenic tetrapeptide RHKKAc as susbtrate | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC3 by fluorimetric assay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC3 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay | B | 6.49 | pIC50 | 323 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC 3 in human HeLa nuclear extract using HDAC substrate-3 measured after 60 mins by fluorometric analysis | B | 6.58 | pIC50 | 261 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of human HDAC3 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay | B | 6.6 | pIC50 | 250 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of full length His6-tagged GST-fused recombinant human HDAC3 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.63 | pIC50 | 232.08 | nM | IC50 | Eur J Med Chem (2016) 112: 81-90 [PMID:26890114] |
| ChEMBL | Inhibition of HDAC3 | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529] |
| ChEMBL | Inhibition of HDAC3 by in vitro deacetylation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of human recombinant HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate incubated for 24 hrs measured after 30 mins by microplate reader based spectrophotometric analysis | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem (2020) 28: 115639-115639 [PMID:32773090] |
| ChEMBL | Inhibition of human recombinant HDAC3 after 60 mins by fluorimetric assay | B | 6.74 | pIC50 | 182 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of full length recombinant human GST fused His6-tagged HDAC3 expressed in baculovirus infected High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate measured after 24 hrs | B | 6.74 | pIC50 | 181.05 | nM | IC50 | Eur J Med Chem (2017) 128: 293-299 [PMID:28213282] |
| ChEMBL | Inhibition of human recombinant HDAC3 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem (2015) 23: 7597-7606 [PMID:26613635] |
| ChEMBL | Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4844-4846 [PMID:21745740] |
| ChEMBL | Inhibition of human recombinant HDAC3 expressed in High5 insect cells using Ac-Lys-Tyr-Lys(-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem (2013) 21: 3240-3244 [PMID:23602523] |
| ChEMBL | Inhibition of recombinant His6-tagged GST-fused human HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs | B | 6.8 | pIC50 | 158.17 | nM | IC50 | Bioorg Med Chem (2015) 23: 5881-5890 [PMID:26211462] |
| ChEMBL | Inhibition of human recombinant full length HDAC3 using (Ac)-Lys-Tyr-Lys(-acetyl)-AMC substrate after 30 mins | B | 6.8 | pIC50 | 158.17 | nM | IC50 | Bioorg Med Chem (2014) 22: 6146-6155 [PMID:25261927] |
| ChEMBL | Inhibition of human recombinant HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | B | 6.82 | pIC50 | 153 | nM | IC50 | Eur J Med Chem (2019) 168: 515-526 [PMID:30851694] |
| ChEMBL | Inhibition of human HDAC3 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 6.82 | pIC50 | 153 | nM | IC50 | J Nat Prod (2019) 82: 1442-1450 [PMID:31120744] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 6.82 | pIC50 | 153 | nM | IC50 | Eur J Med Chem (2018) 144: 398-409 [PMID:29288941] |
| ChEMBL | Inhibition of HDAC3 after 10 mins by fluorometric assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2010) 18: 4119-4137 [PMID:20452225] |
| ChEMBL | Inhibition of human recombinant HDAC3 using fluor de Lys as substrate by fluorometric analysis | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2010) 53: 8663-8678 [PMID:21080647] |
| ChEMBL | Ex vivo inhibition of human HDAC3 in human Caco-2 cells by fluorometric cellular activity assay | B | 6.83 | pIC50 | 147 | nM | IC50 | J Med Chem (2010) 53: 1937-1950 [PMID:20143840] |
| ChEMBL | Inhibition of HDAC3 after 30 mins by Fluor de Lys fluorescence assay | B | 6.84 | pIC50 | 146 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6139-6142 [PMID:21889343] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) by fluorimetric assay | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
| ChEMBL | Inhibition of human recombinant His6-tagged and GST-fuses HDAC3 expressed in insect High5 cells using Ac-Lys-Tyr-Lys(e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4540-4545 [PMID:22738629] |
| ChEMBL | Inhibition of HDAC3 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | B | 6.87 | pIC50 | 136 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7084-7086 [PMID:23089527] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 6.88 | pIC50 | 132 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay | B | 6.9 | pIC50 | 126 | nM | IC50 | Medchemcomm (2015) 6: 1816-1825 |
| ChEMBL | Inhibition of recombinant human HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2018) 26: 4706-4715 [PMID:30115492] |
| ChEMBL | Inhibition of human HDAC3 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of C-terminal His-tagged full length human recombinant HDAC3 co-expressed with NcoR2 in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575] |
| ChEMBL | Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2013) 21: 6981-6995 [PMID:24095018] |
| ChEMBL | Inhibition of human HDAC3 assessed as target activity using fluorogenic substrate ZMAL for 90 min by microplate reader at 355nm | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2021) 64: 14620-14646 [PMID:34582215] |
| ChEMBL | Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate-3 by fluorescence assay | B | 6.97 | pIC50 | 107 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of full length C-terminal 6x-His tagged human HDAC3 using Arg-His-Lys-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | B | 6.97 | pIC50 | 106 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of full length FLAG-tagged recombinant HDAC3 (unknown origin) transfected in human HeLa cells assessed as deacetylation of [3H]-acetylated histones after 2 hrs by scintillation counting analysis | B | 6.97 | pIC50 | 106 | nM | IC50 | J Med Chem (2013) 56: 7201-7211 [PMID:23964961] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of HDAC3 | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.05 | pIC50 | 90.1 | nM | IC50 | J Med Chem (2014) 57: 3324-3341 [PMID:24694055] |
| ChEMBL | Inhibition of human recombinant HDAC3 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2021) 64: 10403-10417 [PMID:34185525] |
| ChEMBL | Inhibition of recombinant HDAC3 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 7.15 | pIC50 | 70 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of human recombinant HDAC3 | B | 7.17 | pIC50 | 67.1 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111] |
| ChEMBL | Inhibition of recombinant HDAC3 (unknown origin) measured after 30 mins by fluorescence assay | B | 7.21 | pIC50 | 62 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of full length human recombinant HDAC3 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Ac)-AMC as substrate after 30 mins by fluorescence assay | B | 7.23 | pIC50 | 58.5 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of HDAC3 | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| ChEMBL | Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells | B | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of C-terminal FLAG tagged HDAC3 | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459] |
| ChEMBL | Inhibition of HDAC3 in HEK293 cells | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of HDAC3 | B | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.25 | pIC50 | 56.8 | nM | IC50 | Eur J Med Chem (2015) 89: 628-637 [PMID:25462271] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.26 | pIC50 | 55 | nM | IC50 | Eur J Med Chem (2013) 64: 273-284 [PMID:23644210] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.26 | pIC50 | 55 | nM | IC50 | Eur J Med Chem (2016) 108: 53-67 [PMID:26629860] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis | B | 7.28 | pIC50 | 52.99 | nM | IC50 | Bioorg Med Chem (2015) 23: 4728-4736 [PMID:26100440] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | B | 7.29 | pIC50 | 51 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of HDAC3 | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC3 expressed in baculovirus insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.39 | pIC50 | 41 | nM | IC50 | Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of human recombinant HDAC3 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2015) 58: 4812-4821 [PMID:25974739] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) by fluorescence based assay | B | 7.4 | pIC50 | 39.6 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of Flag tagged human recombinant HDAC3 expressed in Sf21 cells coexpressing SMRT DAD domain | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2010) 53: 8546-8555 [PMID:21080629] |
| ChEMBL | Inhibition of HDAC3 | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.46 | pIC50 | 35 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of human recombinant HDAC3 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Fluorogenic Inhibition Assay: Boc-Lys(Ac)-7-amino-4-methylcoumarin (Boc-Lys(Ac)-AMC) was used as substrate for the HDAC assays. Substrate solution was prepared as follow: Boc(Lys-Ac)-AMC was dissolved in DMSO and diluted with HDAC buffer (15 mM Tris-HCl [pH 8.1], 250 μM EDTA, 250 mM NaCl, 10% glycerol) to give 1 mM solutions containing 1.7% DMSO. Trypsin was used to stop the reaction, releasing free AMC. The trypsin solution was prepared as follow: trypsin was dissolved in HDAC buffer to give a concentration of 10 mg/mL. Release of AMC was monitored by measuring the fluorescence at 460 nm (lex=390 nm) with a microplate reader (SpectraMax Gemini) at 37° C. The AMC signals were recorded against a blank with buffer, substrate and trypsin but without the enzyme. All experiments were carried out at least in triplicate. For HDAC inhibition assays, inhibitor diluted in 50 μL of HDAC buffer was mixed with 10 μL of diluted enzyme solution in HDAC buffer at room temperature. The HDAC reaction was started by adding 40 μL of substrate solution in HDAC buffer followed by 30 min of incubation with stirring at 37° C. The reaction was stopped by adding 100 μL, of trypsin solution. After a 10 min incubation with stirring at 37° C., the release of AMC was monitored by measuring the fluorescence. | B | 7.47 | pIC50 | 33.8 | nM | IC50 | US-9428447-B2. Bis-(aryl/heteroaryl)-methylene compounds, pharmaceutical compositions containing same and their use for treating cancer (2016) |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.48 | pIC50 | 33.1 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC3 | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
| ChEMBL | Inhibition of recombinant full length HDAC3 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of human recombinant full-length C-terminal GST-tagged HDAC3 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.53 | pIC50 | 29.7 | nM | IC50 | Eur J Med Chem (2017) 141: 596-602 [PMID:29102179] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 7.53 | pIC50 | 29.5 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) after 30 mins by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| ChEMBL | Inhibition of recombinant human FLAG-tagged HDAC3 expressed in human HEK293F cells co-expressing His6-tagged SMRT (1 to 899 residues) using Fluor-de-lys substrate as substrate incubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.54 | pIC50 | 29 | nM | IC50 | ACS Med Chem Lett (2021) 12: 540-547 [PMID:33854701] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) incubated for 60 mins using microplate reader analysis | B | 7.55 | pIC50 | 28.1 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | B | 7.55 | pIC50 | 28 | nM | IC50 | ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449] |
| ChEMBL | Inhibition of human C-terminal His tagged HDAC3 (1 to 428 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs | B | 7.56 | pIC50 | 27.8 | nM | IC50 | J Med Chem (2022) 65: 4156-4181 [PMID:35175762] |
| ChEMBL | Inhibition of recombinant human HDAC3 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 7.59 | pIC50 | 26 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of human recombinant full-length HDAC3 using fluorophore conjugated substrate by fluorescence assay | B | 7.66 | pIC50 | 21.8 | nM | IC50 | J Med Chem (2011) 54: 5576-5582 [PMID:21721525] |
| ChEMBL | Inhibition of human recombinant HDAC3 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate by fluorescence assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1265-1271 [PMID:26804233] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) by ELISA-based assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461] |
| ChEMBL | Inhibition of HADC3 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2019) 183: 111691-111691 [PMID:31536895] |
| ChEMBL | Inhibition of HDAC3 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330] |
| ChEMBL | Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | B | 7.7 | pIC50 | 20 | nM | IC50 | ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317] |
| ChEMBL | Inhibition of HDAC3 in human Jurkat cells extract after 30 mins by immunoprecipitation assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3122-3126 [PMID:27177826] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.72 | pIC50 | 19.1 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of HDAC3 after 17 hrs | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of human recombinant HDAC3 | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863] |
| ChEMBL | Inhibition of HDAC3 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) incubated for 30 mins by microplate reader assay | B | 7.9 | pIC50 | 12.6 | nM | IC50 | Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595] |
| ChEMBL | Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay | B | 8.18 | pIC50 | 6.57 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of human KDAC3 | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
| histone deacetylase 3/Histone deacetylase 3/NCoR1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038484] [GtoPdb: 2617] [UniProtKB: O15379, O75376] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant human HDAC3/NcoR1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of recombinant human HDAC3/NCOR1 complex expressed in insect cells assessed as residual enzyme activity preincubated for 1 hr followed by addition of fluorogenic Ac-LGK-ac-AMC as substrate for 30 mins by fluorescence analysis | B | 8 | pKi | 9.9 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of recombinant human GST-fused HDAC3/NCOR1 (397 to 503 residues) expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.27 | pIC50 | 53.89 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of human recombinant HDAC3/GST tagged NCOR1 (397 to 503 residues) expressed in insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of human recombinant HDAC3/GST-tagged NCOR1 DAD (397 to 503 residues) expressed in baculovirus expression system after 30 mins by fluorescence assay | B | 8.01 | pIC50 | 9.8 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] | ||||||||
| ChEMBL | Inhibition of human recombinant HDAC3/NCoR2 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 30 mins by fluorescence assay | B | 7.66 | pKi | 22 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| ChEMBL | Inhibition of human recombinant HDAC3/NCoR2 using Ac-Leu-Gly-Lys (Ac)-AMC substrate incubated for 45 mins by fluorescence assay based continuous assay protocol | B | 8.27 | pKi | 5.42 | nM | Ki | Medchemcomm (2014) 5: 1849-1855 |
| GtoPdb | - | - | 8.3 | pKi | 5 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of human HDAC-3/NCOR2 using RHKK(Ac) as substrate by fluorescence assay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of full length human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/human recombinant N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human HDAC3/NCOR2 using RHKK(Ac) as substrate by fluorimetric analysis | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC-3/NCOR-2 using RHKK(Ac) as substrate | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 6.84 | pIC50 | 144.7 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
| ChEMBL | Inhibition of human full length C-terminal His-tagged HDAC3/N-terminal GST-tagged human NCOR2 (395 to 489 residues) expressed in baculovirus expression system using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2018) 26: 4428-4440 [PMID:30078609] |
| ChEMBL | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method | B | 6.98 | pIC50 | 105 | nM | IC50 | Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257] |
| ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using fluorometric substrate measured after 60 mins by FRET assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2021) 64: 4020-4033 [PMID:33745280] |
| ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 7.05 | pIC50 | 89.7 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells measured after 30 mins by fluorescence microplate reader assay | B | 7.05 | pIC50 | 89.7 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC3 (1 to 428 residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) co-expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.08 | pIC50 | 83 | nM | IC50 | Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490] |
| ChEMBL | Inhibition of C-terminal His-tagged/N-terminal GST-tagged full length recombinant human HDAC3/NcoR2 expressed in baculovirus infected Sf9 insect cells using KI 177 as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 7.14 | pIC50 | 72.8 | nM | IC50 | Eur J Med Chem (2018) 143: 792-805 [PMID:29223096] |
| ChEMBL | Inhibition of full length human C-terminal His-tagged HDAC3/human N-terminal GST-agged NCOR2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 7.19 | pIC50 | 63.9 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of recombinant C-terminal His-tagged full length human HDAC3/NcoR2 complex expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | B | 7.25 | pIC50 | 56 | nM | IC50 | ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139] |
| ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.31 | pIC50 | 49 | nM | IC50 | Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452] |
| ChEMBL | Inhibition of recombinant HDAC3/NCoR2 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 7.37 | pIC50 | 43 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of recombinant human HDAC3-NCoR2 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC3-NCoR2 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.39 | pIC50 | 41 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of full length HDAC3/NCoR2 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2601-2605 [PMID:21334896] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC3 (1 to 428 end residues)/N-terminal GST-tagged recombinant human NCoR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of human recombinant C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residus) expressed in baculovirus infected Sf9 insect cells using fluor de lys SIRT1 as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC3/NCoR2 using fluorophore-conjugated substrate Boc-L-Lys(Ac)-AMC | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in insect cells using Boc-l-Lys(Ac)-AMC as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of C-terminal His-tagged human recombinant full length HDAC3 (1 to 428 residues)/N-terminal GST-tagged human recombinant NCOR2 (395 to 489 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release using fluorogenic HDAC substrate 3 measured every 5 mins by fluorescence based analysis | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC3/NcoR2 by fluorescence polarization assay | B | 7.73 | pIC50 | 18.8 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of full length human recombinant C-terminal His-tagged HDAC3/NcoR2 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-Ac)-AMC as substrate measured after 90 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2017) 60: 5493-5506 [PMID:28574690] |
| ChEMBL | Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(epsilon-acetyl)-AMC as substrate incubated for 90 mins by fluorescence assay | B | 8.01 | pIC50 | 9.7 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay | B | 4.52 | pKi | 30100 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant human HDAC4 | B | 4.55 | pKi | 28400 | nM | Ki | Bioorg Med Chem (2020) 28: 115108-115108 [PMID:31787463] |
| ChEMBL | Competitive inhibition of HDAC4 using KI-104 as substrate by fluorescence assay | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC4 | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of GST tagged human recombinant HDAC4 (H86 to 31G) expressed in Baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC4 (612 to end residues) expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | B | 4.12 | pIC50 | 76000 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 4.12 | pIC50 | 76000 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 4.12 | pIC50 | 76000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 4.13 | pIC50 | 74000 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of HDAC4 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of human HDAC4 by fluorescence assay | B | 4.32 | pIC50 | 48300 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-fusion tagged/C-terminal GST-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry | B | 4.32 | pIC50 | 47800 | nM | IC50 | Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-fused and C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 90 mins by fluorescence assay | B | 4.37 | pIC50 | 42200 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| ChEMBL | Inhibition of human recombinant HDAC4 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 4.39 | pIC50 | 41000 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2A by fluorescence assay | B | 4.43 | pIC50 | 37090 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 4.48 | pIC50 | >33330 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus expression system using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.48 | pIC50 | 33040 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) after 60 mins by fluorescence assay | B | 4.48 | pIC50 | >33000 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of N-terminal GST-tagged and C-terminal His-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic assay | B | 4.51 | pIC50 | 30710 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of N-terminal GST-tagged/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC4 (612-1034) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) by fluorescence based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of HDAC4 using Boc-Lys(TFA)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2011) 46: 4042-4049 [PMID:21712146] |
| ChEMBL | Inhibition of HDAC4 by fluorometric assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 9562-9575 [PMID:23116147] |
| ChEMBL | Inhibition of recombinant full length human HDAC4 expressed in sf9 insect cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of HDAC4 in human Jurkat E6.1 cells using Boc-Lys-TFA as substrate incubated for 2 hrs prior to substrate addition measured after 3 hrs by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of HDAC4 expressed in Escherichia coli | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of HDAC 4 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of His-tagged HDAC4 catalytic domain expressed in Escherichia coli | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459] |
| ChEMBL | Inhibition of human recombinant HDAC4 using non-histone trifluoroacetyl lysine substrate pre-incubated at room temperature for 15 mins before substrate addition by fluorimetric assay | B | 5.06 | pIC50 | 8800 | nM | IC50 | J Med Chem (2014) 57: 6259-6265 [PMID:24972008] |
| ChEMBL | Inhibition of human recombinant HDAC4 using (S)-[5-Acetylamino-1-(2-oxo-4-trifluorometyl-2Hchromen-7-ylcarbamoyl)pentl]carbami acid tert-Butyl Ester as substrate after 1 hr by fluorescent activity assay | B | 5.11 | pIC50 | 7800 | nM | IC50 | ACS Med Chem Lett (2014) 5: 973-978 [PMID:25221651] |
| ChEMBL | Inhibition of human recombinant HDAC4 after 15 mins by fluorimetric assay | B | 5.21 | pIC50 | 6200 | nM | IC50 | J Med Chem (2010) 53: 4654-4667 [PMID:20491440] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of recombinant human HDAC4 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 5.67 | pIC50 | 2139 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged/C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in baculovirus infected Sf21 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC4 (627 to end residues) expressed in baculovirus infected Sf9 insect cells using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant human full length HDAC4 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
| ChEMBL | Inhibition of human recombinant HDAC4 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay | B | 6 | pIC50 | >1000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375] |
| ChEMBL | Inhibition of HDAC4 H976Y mutant expressed in Escherichia coli | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of HDAC4 gain-of-function phenotype expressed in Escherichia coli | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of human HDAC4 by fluorimetric assay | B | 6.31 | pIC50 | 493 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC-4 using RHKK(Ac) as substrate | B | 6.31 | pIC50 | 493 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC-4 using RHKK(Ac) as substrate by fluorescence assay | B | 6.31 | pIC50 | 493 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC4 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.31 | pIC50 | 493 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human recombinant HDAC4 using AMC-K(TFA)GL as substrate by fluorescence based assay | B | 6.31 | pIC50 | 490 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of human recombinant C-terminal His-tagged, N-terminal GST-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of full length His6-tagged GST-fused recombinant human HDAC4 expressed in High5 insect cells using Ac-Lys-Tyr-Lys (e-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | B | 6.45 | pIC50 | 353.78 | nM | IC50 | Eur J Med Chem (2016) 112: 81-90 [PMID:26890114] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.47 | pIC50 | 340 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC4 by in vitro deacetylation assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of human HDAC4 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of human HDAC4 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 6.7 | pIC50 | >200 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of human HDAC4 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.95 | pIC50 | 113 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of human recombinant HDAC4 | B | 7 | pIC50 | 100.9 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of human recombinant HDAC4 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay | B | 7 | pIC50 | >100 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of HDAC4 in human HeLa cells after 72 hrs by ELISA | B | 7.04 | pIC50 | 91.1 | nM | IC50 | Eur J Med Chem (2018) 146: 79-92 [PMID:29396364] |
| ChEMBL | Inhibition of recombinant HDAC4 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | B | 7.2 | pIC50 | 63.2 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 7.27 | pIC50 | 54.3 | nM | IC50 | Eur J Med Chem (2021) 226: 113870-113870 [PMID:34610548] |
| ChEMBL | Inhibition of HDAC4 in human Jurkat E6.1 cells using Boc-Lys-Ac as substrate incubated for 2 hrs prior to substrate addition measured after 3 hrs by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of HDAC4 | B | 9 | pIC50 | >1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| GtoPdb | - | - | 5.44 | pKi | 3600 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human HDAC5 | B | 5.44 | pKi | 3600 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Competitive inhibition of HDAC5 using KI-104 as substrate by fluorescence assay | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC5 | B | 7.48 | pKi | 33 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 4.38 | pIC50 | 41500 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of HDAC5 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate by fluorescence assay | B | 4.57 | pIC50 | 27200 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 4.57 | pIC50 | 27200 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC fluorogenic acetylated peptide substrate by fluorometric assay | B | 4.57 | pIC50 | 27000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of human HDAC5 by fluorescence assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2A by fluorescence assay | B | 4.73 | pIC50 | 18440 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of recombinant human HDAC5 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 4.82 | pIC50 | 15000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 4.86 | pIC50 | 13800 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) after 60 mins by fluorescence assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus infected Sf9 insect cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.98 | pIC50 | 10510 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC5 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of wild type His-tagged HDAC5 catalytic domain T678-L1122 expressed in Escherichia coli | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of N-terminal GST-tagged human recombinant full length HDAC5 expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 5.06 | pIC50 | 8750 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of human recombinant HDAC5 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 5.34 | pIC50 | 4600 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant HDAC5 using fluor de Lys as substrate by fluorometric analysis | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2010) 53: 8663-8678 [PMID:21080647] |
| ChEMBL | Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay | B | 5.59 | pIC50 | 2580 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of human recombinant HDAC5 after 60 mins by fluorimetric assay | B | 5.61 | pIC50 | 2480 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of HDAC 5 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | B | 5.66 | pIC50 | 2180 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC5 (620-1122) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC5 (656 to 1122 residues) expressed in baculovirus-infected insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC5 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal GST-tagged HDAC5 expressed in baculovirus infected Sf9 insect cells using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of HDAC5 by in vitro deacetylation assay | B | 6.4 | pIC50 | 400 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of human recombinant HDAC5 using AMC-K(TFA)GL as substrate by fluorescence based assay | B | 6.42 | pIC50 | 380 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.42 | pIC50 | 380 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human HDAC-5 using RHKK(Ac) as substrate | B | 6.42 | pIC50 | 378 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC-5 using RHKK(Ac) as substrate by fluorescence assay | B | 6.42 | pIC50 | 378 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC5 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.42 | pIC50 | 378 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human HDAC5 by fluorimetric assay | B | 6.42 | pIC50 | 378 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC5 using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 6.7 | pIC50 | >200 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of human HDAC5 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of human recombinant HDAC5 | B | 6.97 | pIC50 | 107.3 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of HDAC5 | B | 9 | pIC50 | >1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC6 using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | B | 6.52 | pKd | 300 | nM | Kd | Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579] |
| ChEMBL | Inhibition of HDAC7 | B | 6.9 | pKi | 126 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells assessed as inhibitory constant using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay | B | 7.46 | pKi | <35 | nM | Ki | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Competitive inhibition of HDAC6 using KI-104 as substrate by fluorescence assay | B | 7.54 | pKi | 29 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of human recombinant HDAC6 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of recombinant human HDAC6 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins | B | 7.66 | pKi | 22 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of HDAC6 | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2008) 51: 2898-2906 [PMID:18412327] |
| ChEMBL | Inhibition of recombinant human HDAC6 | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2020) 28: 115108-115108 [PMID:31787463] |
| ChEMBL | Inhibition of HDAC6 | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of His-tagged recombinant human HDAC6 expressed in insect cells assessed as hydrolase activity using fluorogenic AC-LGK-ac-AMC as substrate measured after 60 mins by fluorescence analysis | B | 7.75 | pKi | 17.7 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
| ChEMBL | Inhibition of human HDAC6 | B | 8.8 | pKi | 1.6 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| GtoPdb | - | - | 8.8 | pKi | 1.6 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (2021) 64: 2691-2704 [PMID:33576627] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Z-MAL as substrate after 1 hr by fluorescent activity assay | B | 5.25 | pIC50 | 5600 | nM | IC50 | ACS Med Chem Lett (2014) 5: 973-978 [PMID:25221651] |
| ChEMBL | Inhibition of HDAC6 in human LNCAP cells assessed as tubulin acetylation by Western blot analysis | B | 5.64 | pIC50 | 2310 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4826-4830 [PMID:25240614] |
| ChEMBL | Inhibition of recombinant human N-terminal GST tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys (Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 6.07 | pIC50 | 860 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
| ChEMBL | Inhibition of HDAC6 | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6588-6590 [PMID:19854643] |
| ChEMBL | Fluorogenic Inhibition Assay: Boc-Lys(Ac)-7-amino-4-methylcoumarin (Boc-Lys(Ac)-AMC) was used as substrate for the HDAC assays. Substrate solution was prepared as follow: Boc(Lys-Ac)-AMC was dissolved in DMSO and diluted with HDAC buffer (15 mM Tris-HCl [pH 8.1], 250 μM EDTA, 250 mM NaCl, 10% glycerol) to give 1 mM solutions containing 1.7% DMSO. Trypsin was used to stop the reaction, releasing free AMC. The trypsin solution was prepared as follow: trypsin was dissolved in HDAC buffer to give a concentration of 10 mg/mL. Release of AMC was monitored by measuring the fluorescence at 460 nm (lex=390 nm) with a microplate reader (SpectraMax Gemini) at 37° C. The AMC signals were recorded against a blank with buffer, substrate and trypsin but without the enzyme. All experiments were carried out at least in triplicate. For HDAC inhibition assays, inhibitor diluted in 50 μL of HDAC buffer was mixed with 10 μL of diluted enzyme solution in HDAC buffer at room temperature. The HDAC reaction was started by adding 40 μL of substrate solution in HDAC buffer followed by 30 min of incubation with stirring at 37° C. The reaction was stopped by adding 100 μL, of trypsin solution. After a 10 min incubation with stirring at 37° C., the release of AMC was monitored by measuring the fluorescence. | B | 6.24 | pIC50 | 580 | nM | IC50 | US-9428447-B2. Bis-(aryl/heteroaryl)-methylene compounds, pharmaceutical compositions containing same and their use for treating cancer (2016) |
| ChEMBL | Inhibition of human HDAC6 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of HDAC6 after 10 mins by fluorometric assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem (2010) 18: 4119-4137 [PMID:20452225] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Boc-Lys(Ac)-AMC as substrate after 30 mins by fluorescence assay | B | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem (2015) 23: 7597-7606 [PMID:26613635] |
| ChEMBL | Inhibition of human full-length recombinant HDAC6 preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of HDAC6 CD2 (unknown origin) expressed in HEK293 cells cotransfected with nano-luciferase incubated for 2 hrs followed by NanoBRET NanoGlo Substrate addition by NanoBRET assay | B | 6.62 | pIC50 | 241 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate-3 by fluorescence assay | B | 6.65 | pIC50 | 226 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of HDAC6 by fluorometric assay | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2012) 55: 9562-9575 [PMID:23116147] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Boc-lys(Ac)-AMC as substrate preincubated for 20 mins with substrate measured after 60 mins by fluorescence analysis | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2012) 55: 1731-1750 [PMID:22280363] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys (acetyl)-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by UV-vis spectrophotometer analysis | B | 6.69 | pIC50 | 202.11 | nM | IC50 | Bioorg Med Chem (2015) 23: 4728-4736 [PMID:26100440] |
| ChEMBL | Inhibition of human recombinant N-terminal histidine-tagged HDAC6 expressed in baculovirus by fluorimetry | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 336-340 [PMID:19084395] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC6 in presence of DTT | B | 6.71 | pIC50 | 196 | nM | IC50 | J Med Chem (2007) 50: 5720-5726 [PMID:17958342] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cell nuclear extract after 30 mins by fluorescence microplate reader | B | 6.71 | pIC50 | 195 | nM | IC50 | J Med Chem (2011) 54: 2823-2838 [PMID:21476600] |
| ChEMBL | Inhibition of full length His6-tagged GST-fused recombinant human HDAC6 expressed in High5 insect cells using Boc-Lys (e-acetyl)-AMC as substrate after 3 hrs by fluorescence assay | B | 6.75 | pIC50 | 179.62 | nM | IC50 | Eur J Med Chem (2016) 112: 81-90 [PMID:26890114] |
| ChEMBL | Inhibition of human HDAC6 by fluorescence assay | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of HDAC6 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Fluor-de-lys as substrate measured after 60 mins by fluorescence assay | B | 6.81 | pIC50 | 154 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys(eacety1)-AMC as substrate incubated for 3 hrs measured after 30 mins by microplate reader based spectrophotometric analysis | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2020) 28: 115639-115639 [PMID:32773090] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis | B | 6.84 | pIC50 | 144 | nM | IC50 | J Med Chem (2013) 56: 3492-3506 [PMID:23547652] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacYGC as substrate after 60 mins by SAMDI mass spectrometric analysis | B | 6.84 | pIC50 | 144 | nM | IC50 | J Med Chem (2013) 56: 9969-9981 [PMID:24304348] |
| ChEMBL | Inhibition of His-tagged HDAC6 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | B | 6.84 | pIC50 | 144 | nM | IC50 | Eur J Med Chem (2015) 96: 340-359 [PMID:25899338] |
| ChEMBL | Inhibition of Nanoluc-fused HDAC6 CD2 (unknown origin) expressed in HEK293 cells incubated for 2 hrs by NANOBRET assay | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of recombinant human HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem (2018) 26: 4706-4715 [PMID:30115492] |
| ChEMBL | Inhibition of human recombinant His6-tagged and GST-fuses HDAC6 expressed in insect High5 cells using Boc-Lys(eacetyl)- AMC as substrate after 3 hrs by fluorescence assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4540-4545 [PMID:22738629] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 30 mins by fluorescence assay | B | 6.93 | pIC50 | 118 | nM | IC50 | ACS Med Chem Lett (2013) 4: 235-238 [PMID:23493449] |
| ChEMBL | Inhibition of human recombinant HDAC6 | B | 6.96 | pIC50 | 110.6 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of recombinant human full length HDAC6 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
| ChEMBL | Inhibition of full length recombinant human HDAC6 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2016) 122: 92-101 [PMID:27344487] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) incubated for 30 mins by microplate reader assay | B | 6.96 | pIC50 | 109 | nM | IC50 | Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595] |
| ChEMBL | Inhibition of N-terminal GST-tagged recombinant human HDAC6 expressed in baculovirus infected Sf9 insect cells using Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2017) 60: 5493-5506 [PMID:28574690] |
| ChEMBL | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells Z-(Ac)Lys-AMC as substrate measured after 90 mins by fluorescence assay | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2017) 60: 5334-5348 [PMID:28581289] |
| ChEMBL | Inhibition of full length recombinant human GST fused His6-tagged HDAC6 expressed in baculovirus infected High5 cells using Boc-Lys(epsilon-acetyl)-AMC as substrate measured after 3 hrs | B | 6.98 | pIC50 | 105.1 | nM | IC50 | Eur J Med Chem (2017) 128: 293-299 [PMID:28213282] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic ZMAL as substrate incubated for 90 mins by fluorescence assay | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (2019) 62: 1138-1166 [PMID:30645113] |
| ChEMBL | Inhibition of human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells ZMAL as substrate incubated for 90 mins by fluorescence assay | B | 6.99 | pIC50 | 102 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| ChEMBL | Inhibition of full length recombinant GST-tagged N-terminal human HDAC6 expressed in baculovirus infected Sf9 insect cells using ZMAL (Z-Lys(Ac)-AMC) as substrate incubated for 90 mins by fluorescence based assay | B | 6.99 | pIC50 | 102 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1336-1340 [PMID:31531206] |
| ChEMBL | Inhibition of human HDAC6 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of recombinant HDAC6 (unknown origin) using Fluor-de-Lys-SIRT1 as substrate by fluorescence assay | B | 7 | pIC50 | 100 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of Histone deacetylase 6 (HDAC6) of HeLa nuclear extracts | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition by fluorescence assay | B | 7.01 | pIC50 | 98 | nM | IC50 | Medchemcomm (2015) 6: 1816-1825 |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorogenic Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | B | 7.04 | pIC50 | 91 | nM | IC50 | J Med Chem (2018) 61: 5304-5322 [PMID:29787262] |
| ChEMBL | Inhibition of HDAC6 | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2019) 62: 3898-3923 [PMID:30901208] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in High5 insect cells using Boc-Lys (-acetyl)-AM) as substrate after 24 hrs by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem (2013) 21: 3240-3244 [PMID:23602523] |
| ChEMBL | Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of HDAC6 | B | 7.07 | pIC50 | 85.5 | nM | IC50 | J Med Chem (2010) 53: 6100-6111 [PMID:20669972] |
| ChEMBL | Inhibition of HDAC6 from human HeLa cells nuclear extract by cell free fluorimetric assay | B | 7.07 | pIC50 | 85.5 | nM | IC50 | J Med Chem (2009) 52: 456-468 [PMID:19093884] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate by fluorometric analysis | B | 7.07 | pIC50 | 85 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7067-7070 [PMID:20947351] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 7.08 | pIC50 | 83 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 7.09 | pIC50 | 82 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of recombinant His6-tagged GST-fused human HDAC6 expressed in baculovirus infected insect High5 cells using Boc-Lys-(epsilon-acetyl)-AMC as substrate after 3 hrs | B | 7.1 | pIC50 | 78.98 | nM | IC50 | Bioorg Med Chem (2015) 23: 5881-5890 [PMID:26211462] |
| ChEMBL | Inhibition of human recombinant full length HDAC6 using (Boc-Lys (-acetyl)-AMC substrate after 30 mins | B | 7.1 | pIC50 | 78.98 | nM | IC50 | Bioorg Med Chem (2014) 22: 6146-6155 [PMID:25261927] |
| ChEMBL | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | B | 7.11 | pIC50 | 78.3 | nM | IC50 | J Med Chem (2020) 63: 5501-5525 [PMID:32321249] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | B | 7.12 | pIC50 | 76 | nM | IC50 | J Med Chem (2015) 58: 9214-9227 [PMID:26555243] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) incubated for 60 mins by microplate reader analysis | B | 7.12 | pIC50 | 75.9 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of recombinant C-terminal FLAG-tagged full length human HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.13 | pIC50 | 74 | nM | IC50 | Eur J Med Chem (2020) 188: 111991-111991 [PMID:31883490] |
| ChEMBL | Inhibition of HDAC6 using Fluor-de-Lys as substrate compound pretreated for 30 mins before substrate addition by fluorescence assay | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7084-7086 [PMID:23089527] |
| ChEMBL | Inhibition of HDAC6 after 30 mins by Fluor de Lys fluorescence assay | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6139-6142 [PMID:21889343] |
| ChEMBL | Inhibition of recombinant human HDAC6 using fluorogenic substrate by fluorescence assay | B | 7.14 | pIC50 | 72.34 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 pre-incubated for 30 mins followed by HDAC developer addition and measured after 15 mins by fluorogenic assay | B | 7.15 | pIC50 | 70.83 | nM | IC50 | Bioorg Med Chem (2019) 27: 3408-3420 [PMID:31235266] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4457-4460 [PMID:26376355] |
| ChEMBL | Inhibition of recombinant human HDAC6 | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 375-379 [PMID:26706171] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect high5 cells using Boc-Lys (epsilon-acetyl)-AM) as substrate after 3 to 24 hrs by fluorescence assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2013) 21: 6981-6995 [PMID:24095018] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | B | 7.19 | pIC50 | 65 | nM | IC50 | Eur J Med Chem (2019) 168: 515-526 [PMID:30851694] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.19 | pIC50 | 65 | nM | IC50 | Eur J Med Chem (2018) 144: 398-409 [PMID:29288941] |
| ChEMBL | Inhibition of human HDAC6 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 7.19 | pIC50 | 65 | nM | IC50 | J Nat Prod (2019) 82: 1442-1450 [PMID:31120744] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.2 | pIC50 | 63 | nM | IC50 | J Med Chem (2014) 57: 3324-3341 [PMID:24694055] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in Sf9 cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2018) 26: 4428-4440 [PMID:30078609] |
| ChEMBL | Inhibition of human recombinant HDAC6 pre-incubated at room temperature for 15 min before substrate addition by fluorimetric assay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2014) 57: 6259-6265 [PMID:24972008] |
| ChEMBL | Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using Z-(Ac)-Lys-AMC as substrate incubated for 40 mins by fluorescence based assay | B | 7.23 | pIC50 | 59.3 | nM | IC50 | Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778] |
| ChEMBL | Inhibition of human recombinant full-length HDAC6 using fluorophore conjugated substrate by fluorescence assay | B | 7.24 | pIC50 | 57.3 | nM | IC50 | J Med Chem (2011) 54: 5576-5582 [PMID:21721525] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac)AMC as substrate | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2015) 58: 2809-2820 [PMID:25734520] |
| ChEMBL | Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2016) 59: 1545-1555 [PMID:26653328] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in HEK293 cells | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (2009) 52: 2265-2279 [PMID:19301902] |
| ChEMBL | Inhibition of human recombinant HDAC6 assessed as fluorescence using fluorogenic substrate ZMAL incubated for 90 min by microplate reader | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2021) 64: 14620-14646 [PMID:34582215] |
| ChEMBL | Inhibition of N-terminal GST-tagged full length human recombinant HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2021) 211: 113065-113065 [PMID:33360801] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) by fluorimetric assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.3 | pIC50 | 50 | nM | IC50 | Medchemcomm (2014) 5: 342-351 |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate measured after 30 mins by fluorescence assay | B | 7.33 | pIC50 | 46.48 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of HDAC6 | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| ChEMBL | Inhibition of HDAC6 at 10 uM | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of HDAC6 in HEK293 cells | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1814-1819 [PMID:18308563] |
| ChEMBL | Inhibition of C-terminal FLAG-tagged HDAC6 expressed in mammalian cells | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of C-terminal FLAG tagged HDAC6 | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Cbz-(Ac)Lys-AMC as substrate preincubated for 90 mins followed by trypsin addition measured after 20 mins by fluorescence assay | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2016) 59: 2423-2435 [PMID:26937828] |
| ChEMBL | Inhibition of human recombinant HDAC6 using ZMAL (Z-(Ac)Lys-AMC fluorogenic substrate incubated for 90 mins by fluorescence method | B | 7.38 | pIC50 | 41.9 | nM | IC50 | ACS Med Chem Lett (2019) 10: 671-676 [PMID:30996816] |
| ChEMBL | Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 7.4 | pIC50 | 39.9 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | B | 7.41 | pIC50 | 38.9 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| ChEMBL | Inhibition of full length His-tagged human recombinant HDAC6 expressed in baculovirus system using fluor de Lys as substrate by fluorometric analysis | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2013) 66: 56-68 [PMID:23792316] |
| ChEMBL | Inhibition of HDAC6 | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Fluor de Lys Assay: Fluor de Lys is a fluorescence based HDAC activity assay comprising a combination of fluorogenic Histone deAcetylase Lysyl substrate and a developer. The kit is a highly sensitive and convenient alternative to radiolabeled, acetylated histones or peptide/HPLC methods for the assay of histone deacetylases. This assay is based on the ability of HeLa nuclear extract, which is enriched in HDAC activity, to mediate the deacetylation of the acetylated lysine side chain of the Fluor de Lys substrate. The assay procedure requires two steps. First, incubation of the HeLa nuclear extract with the Fluor de Lys substrate results in substrate deacetylation and thus sensitizes it to the second step. In the second step, treatment of the deacetylated substrate with the Fluor de Lys developer produces a fluorophore. The substrate-developer reaction, under normal circumstances goes to completion in less than 1 min at 25 C. | B | 7.42 | pIC50 | 38 | nM | IC50 | US-8871728-B2. Non-peptide macrocyclic histone deacetylese (HDAC) inhibitors and methods of making and using thereof (2014) |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2016) 59: 8967-9004 [PMID:27606546] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
| ChEMBL | Inhibition of recombinant human full length C-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using ZMAL as substrate incubated for 90 mins by fluorometric method | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem (2019) 27: 115039-115039 [PMID:31420257] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 60 mins by fluorimetric assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay | B | 7.46 | pIC50 | 34.3 | nM | IC50 | Medchemcomm (2019) 10: 1109-1115 [PMID:31391882] |
| ChEMBL | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate 3 preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem (2020) 28: 115345-115345 [PMID:32061484] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect High5 cells using Boc-Lys(epsilon-acetyl)-AMC as substrate by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4844-4846 [PMID:21745740] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (2013) 56: 5782-5796 [PMID:23786452] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cells after 72 hrs by ELISA | B | 7.48 | pIC50 | 33.4 | nM | IC50 | Eur J Med Chem (2018) 146: 79-92 [PMID:29396364] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 7.48 | pIC50 | 33.1 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127638-127638 [PMID:33132117] |
| ChEMBL | Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | B | 7.48 | pIC50 | 33 | nM | IC50 | ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2021) 47: 128207-128207 [PMID:34146703] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) by ELISA-based assay | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay | B | 7.48 | pIC50 | 33 | nM | IC50 | ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375] |
| ChEMBL | Inhibition of HDAC6 in human HeLa-S3 cell lysates preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 40 mins by fluorimetric method | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330] |
| ChEMBL | Inhibition of HADC6 (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of recombinant full length human HDAC6 expressed in Baculovirus infected insect Sf9 cells incubated for 30 mins measured by fluorescence assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Medchemcomm (2014) 5: 1887-1891 |
| ChEMBL | Inhibition of recombinant human HDAC6 using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells preincubated with enzyme followed by flour de lys-green substrate addition measured after 1 hr by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4415-4420 [PMID:28818449] |
| ChEMBL | Inhibition of human recombinant HDAC6 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 7.52 | pIC50 | 30 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127537-127537 [PMID:32916298] |
| ChEMBL | Inhibition of human recombinant HDAC6 using fluor de Lys as substrate by fluorometric analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2010) 53: 8663-8678 [PMID:21080647] |
| ChEMBL | Inhibition of human recombinant full length HDAC6 after 60 mins by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Tosyl-Gly-ProLys(Ac)-AMC as substrate measured after 60 mins by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2021) 64: 10403-10417 [PMID:34185525] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Fluor de Lys-Green as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2018) 143: 320-333 [PMID:29202397] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2013) 64: 273-284 [PMID:23644210] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 15 mins by fluorogenic assay | B | 7.53 | pIC50 | 29.7 | nM | IC50 | J Med Chem (2015) 58: 4550-4572 [PMID:25993269] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2016) 108: 53-67 [PMID:26629860] |
| ChEMBL | Inhibition of human HDAC-6 using RHKK(Ac) as substrate by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate incubated for 90 mins by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human HDAC6 using RHKK(Ac) as substrate by fluorimetric analysis | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC-6 using RHKK(Ac) as substrate | B | 7.54 | pIC50 | 28.9 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC6 by fluorimetric assay | B | 7.54 | pIC50 | 28.6 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human HDAC6 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.54 | pIC50 | 28.6 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorogenic tetrapeptide RHKK(Ac) substrate by fluorescence assay | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2638-2645 [PMID:31400938] |
| ChEMBL | Inhibition of human recombinant HDAC6 by fluorimetry | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2009) 52: 2909-2922 [PMID:19419205] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2022) 65: 3667-3683 [PMID:35152694] |
| ChEMBL | Inhibition of human HDAC6 pre-incubated for 5 mins before substrate addition and measured after 30 mins by fluorescence based assay | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2021) 64: 1116-1126 [PMID:33356256] |
| ChEMBL | Inhibition of recombinant full length HDAC6 (unknown origin) using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3283-3287 [PMID:23622981] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2012) 55: 1465-1477 [PMID:22260166] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-LeuGlyLy-s(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence microtiter plate reader assay | B | 7.57 | pIC50 | 26.9 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC6 | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
| ChEMBL | Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay | B | 7.59 | pIC50 | 25.6 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC6 | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in HEK293 cells | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2010) 53: 8546-8555 [PMID:21080629] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of recombinant human HDAC6 using fluorogenic HDAC substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by fluorescence analysis | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2018) 26: 5718-5729 [PMID:30385227] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.61 | pIC50 | 24.4 | nM | IC50 | Eur J Med Chem (2015) 89: 628-637 [PMID:25462271] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | B | 7.62 | pIC50 | 24.25 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of human recombinant full-length HDAC6 expressed in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate after 30 mins by fluorescence assay | B | 7.62 | pIC50 | 24.2 | nM | IC50 | Eur J Med Chem (2017) 141: 596-602 [PMID:29102179] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry | B | 7.62 | pIC50 | 24 | nM | IC50 | Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.64 | pIC50 | 23 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged full length human HDAC6 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139] |
| ChEMBL | Displacement of fluorescent 5-(3-(3-(4-((4-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)phenylamino)methyl)-1H-1,2,3-triazol-1-yl)propyl)thioureido)-2-(3-hydroxy-6-oxo-6H-xanthen-9-yl)benzoic acid from human HDAC6 by fluorescence polarization assay | B | 7.67 | pIC50 | 21.6 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2809-2812 [PMID:18430569] |
| ChEMBL | Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay | B | 7.67 | pIC50 | 21.5 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of recombinant human full length C-terminal flag-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | B | 7.68 | pIC50 | 21 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| ChEMBL | Inhibition of recombinant HDAC6 (unknown origin) measured after 30 mins by fluorescence assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of human recombinant HDAC6 expressed in Baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of human HDAC6 after 30 mins by microplate reader analysis | B | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127023-127023 [PMID:32067866] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 7.69 | pIC50 | 20.2 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of N-terminal GST tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected insect cells using RHKKAc as substrate in presence of ATP | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2017) 60: 8336-8357 [PMID:28953386] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHKK(Ac)) as substrate by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2018) 158: 593-619 [PMID:30243158] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Arg-His-Lys-Lys(Ac) as substrate after 2 hrs by fluorescence analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1357-1362 [PMID:29545103] |
| ChEMBL | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2016) 59: 8233-8262 [PMID:27541357] |
| ChEMBL | Inhibition of HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | B | 7.7 | pIC50 | 19.8 | nM | IC50 | Eur J Med Chem (2011) 46: 4042-4049 [PMID:21712146] |
| ChEMBL | Inhibition of human HDAC6 using Arg-His-Lys-Lys (Ac) as substrate incubated for 2 hrs by fluorescence assay | B | 7.7 | pIC50 | 19.8 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
| ChEMBL | Inhibition of recombiant human HDAC6 using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence microplate reader assay | B | 7.7 | pIC50 | 19.8 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7.71 | pIC50 | 19.4 | nM | IC50 | US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016) |
| ChEMBL | Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). | B | 7.71 | pIC50 | 19.4 | nM | IC50 | US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015) |
| ChEMBL | Inhibition of recombinant HDAC6 (unknown origin) after 10 mins by fluorimetric analysis | B | 7.71 | pIC50 | 19.4 | nM | IC50 | J Med Chem (2013) 56: 3645-3655 [PMID:23570542] |
| ChEMBL | Inhibition of recombinant HDAC6 expressed in HEK293 cells | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2008) 51: 3985-4001 [PMID:18558669] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) assessed as release of 7-amino-4-methylcoumarin incubated in room temperature for 15 min measured by Spectra max microtitre plate reader | B | 7.73 | pIC50 | 18.5 | nM | IC50 | J Med Chem (2021) 64: 16573-16597 [PMID:34783558] |
| ChEMBL | Inhibition of human recombinant HDAC6 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.74 | pIC50 | 18 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cells nuclear extract using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 7.74 | pIC50 | 18 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of recombinant HDAC6 using Ac-Lys(Ac)-AMC as substrate after 30 mins by fluorescence analysis | B | 7.74 | pIC50 | 18 | nM | IC50 | ACS Med Chem Lett (2012) 3: 505-508 [PMID:24900500] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 7.76 | pIC50 | 17.4 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) by fluorescence based assay | B | 7.76 | pIC50 | 17.2 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) after 30 mins by fluorescence assay | B | 7.79 | pIC50 | 16.3 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| ChEMBL | Inhibition of full length human N-terminal FLAG-tagged HDAC6 (1 to 1215 residues) expressed in HEK293 cells preincubated for 15 mins followed by acetyl-Gly-Ala-[acetyl-Lys]-AMC substrate addition measured after 30 mins by fluorimetric method | B | 7.8 | pIC50 | 16 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1301-1305 [PMID:30613344] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence assay | B | 7.82 | pIC50 | 15.1 | nM | IC50 | Eur J Med Chem (2021) 226: 113870-113870 [PMID:34610548] |
| ChEMBL | Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of recombinant full length HDAC6 (unknown origin) using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using substrate after 30 mins by fluorometric analysis | B | 7.84 | pIC50 | 14.5 | nM | IC50 | Eur J Med Chem (2017) 133: 11-23 [PMID:28371677] |
| ChEMBL | Inhibition of HDAC6 after 17 hrs | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of human recombinant HDAC6 incubated for 15 mins by fluorogenic assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem (2021) 40: 116185-116185 [PMID:33965842] |
| ChEMBL | Inhibition of HDAC6 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of human recombinant HDAC6 | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3023-3026 [PMID:19419863] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST tagged HDAC6 (1 to 1215 residues) expressed in baculovirus-infected Sf9 cells using Ac-peptide as substrate incubated for 4 hrs | B | 7.87 | pIC50 | 13.5 | nM | IC50 | J Med Chem (2022) 65: 4156-4181 [PMID:35175762] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844] |
| ChEMBL | Inhibition of N-terminal GST-tagged full length human HDAC6 expressed in baculovirus-infected Sf9 cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorescence based assay | B | 7.9 | pIC50 | 12.6 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 cells using fluorogenic HDAC substrate 3 measured after 30 mins by fluorescence based assay | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 744-749 [PMID:28131715] |
| ChEMBL | Inhibition of human recombinant HDAC6 using MAZ1600 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2015) 58: 4812-4821 [PMID:25974739] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | B | 7.97 | pIC50 | 10.8 | nM | IC50 | Bioorg Med Chem (2017) 25: 27-37 [PMID:27769671] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2021) 224: 113672-113672 [PMID:34237620] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 8.03 | pIC50 | 9.4 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of HDAC6 | B | 8.03 | pIC50 | 9.3 | nM | IC50 | Eur J Med Chem (2010) 45: 4331-4338 [PMID:20637529] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | B | 8.04 | pIC50 | 9.2 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| ChEMBL | Inhibition of N-terminal GST-tagged human HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 8.04 | pIC50 | 9.1 | nM | IC50 | Eur J Med Chem (2018) 143: 792-805 [PMID:29223096] |
| ChEMBL | Inhibition of HDAC6 by in vitro deacetylation assay | B | 8.05 | pIC50 | 9 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) preincubated for 10 mins followed by Ac-Leu-GlyLys(Ac)-AMC substrate addition measured after 30 mins by fluorescence based assay | B | 8.06 | pIC50 | 8.8 | nM | IC50 | Bioorg Med Chem (2018) 26: 747-757 [PMID:29317150] |
| ChEMBL | Inhibition of recombinant human His-tagged HDAC6 expressed in baculovirus infected insect cells using Boc Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 8.1 | pIC50 | 7.9 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 8.11 | pIC50 | 7.76 | nM | IC50 | Eur J Med Chem (2017) 134: 281-292 [PMID:28419930] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using acetylated peptide substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence analysis | B | 8.11 | pIC50 | 7.7 | nM | IC50 | Bioorg Med Chem (2017) 25: 4100-4109 [PMID:28601509] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate pretreated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem (2018) 26: 3958-3966 [PMID:29954683] |
| ChEMBL | Inhibition of recombinant human HDAC6 using Ac-GAK(Ac)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay | B | 8.24 | pIC50 | 5.8 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using Boc-Lys(Ac)-pNA as substrate preincubated for 20 mins followed by substrate addition and further incubated for 90 mins by fluorescence assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2020) 63: 6959-6978 [PMID:32551649] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorometric assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2012) 55: 3777-3791 [PMID:22439863] |
| ChEMBL | Inhibition of full length human N-terminal GST-tagged HDAC6 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of recombinant human full length HDAC6 expressed in baculovirus infected Sf9 insect cells using p53 (379 to 382 residues) derived RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 2 hrs by fluorescence assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1031-1036 [PMID:29057046] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.57 | pIC50 | 2.71 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of HDAC6 (unknown origin) after 60 mins by fluorescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of human KDAC6 | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
| ChEMBL | Inhibition of HDAC6 in human A549 cells assessed as tubulin acetylation after 17 to 18 hrs by cytoblot assay | B | 5.99 | pEC50 | 1030 | nM | EC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC6 in human A549 cells assessed as induction of tubulin acetylation after 17 to 18 hrs by ELISA | B | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2015) 58: 2809-2820 [PMID:25734520] |
| ChEMBL | Inhibition of HDAC6 in human MCF7 cells assessed as increase in acetylated alpha-tubulin at Lys40 residue incubated for 3 hrs by ELISA | B | 6.37 | pEC50 | 430 | nM | EC50 | J Med Chem (2018) 61: 1552-1575 [PMID:29360358] |
| ChEMBL | Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay | B | 6.4 | pEC50 | 399.25 | nM | EC50 | J Med Chem (2016) 59: 5488-5504 [PMID:27186676] |
| ChEMBL | Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA | B | 7.66 | pEC50 | 21.7 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 154-159 [PMID:26611919] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC7 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay | B | 4.44 | pKd | 36000 | nM | Kd | Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579] |
| ChEMBL | Competitive inhibition of HDAC7 using KI-104 as substrate by fluorescence assay | B | 6.89 | pKi | 129 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 4.38 | pIC50 | 41800 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of human recombinant HDAC7 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 4.39 | pIC50 | 41000 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.4 | pIC50 | >40000 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of human recombinant HDAC7 after 60 mins by fluorimetric assay | B | 4.41 | pIC50 | 38900 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of human recombinant HDAC7 incubated for 10 mins prior to substrate addition measured after 60 mins by spectrophotometric analysis | B | 4.41 | pIC50 | 38900 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3295-3299 [PMID:23601706] |
| ChEMBL | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus-infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic assay | B | 4.45 | pIC50 | 35160 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 4.48 | pIC50 | >33330 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) after 60 mins by fluorescence assay | B | 4.48 | pIC50 | >33000 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of HDAC7 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 4.53 | pIC50 | 29760 | nM | IC50 | Medchemcomm (2014) 5: 342-351 |
| ChEMBL | Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2A by fluorescence assay | B | 4.53 | pIC50 | 29290 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of recombinant human HDAC7 using Fluor-de-Lys as substrate after 30 mins by spectrophotometry | B | 4.68 | pIC50 | 21000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of HDAC7 expressed in Escherichia coli | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of human recombinant N-terminal FLAG-tagged HDAC7 (438-915) expressed in baculovirus after 10 mins by fluorimetric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5684-5688 [PMID:19699639] |
| ChEMBL | Inhibition of wild type His-tagged HDAC7 catalytic domain T515-L952 expressed in Escherichia coli | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of recombinant human HDAC7 using Ac-LGK(TFA)-AMC as substrate pre-incubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 5.02 | pIC50 | 9600 | nM | IC50 | J Med Chem (2021) 64: 2186-2204 [PMID:33570940] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 5.09 | pIC50 | 8200 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay | B | 5.21 | pIC50 | 6110 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of human HDAC7 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 5.61 | pIC50 | 2480 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) using AcLeu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC7 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 6.1 | pIC50 | 800 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC7 by in vitro deacetylation assay | B | 6.3 | pIC50 | 500 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of human HDAC-7 using RHKK(Ac) as substrate by fluorescence assay | B | 6.46 | pIC50 | 344 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC-7 using RHKK(Ac) as substrate | B | 6.46 | pIC50 | 344 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC7 by fluorimetric assay | B | 6.46 | pIC50 | 344 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human N-terminal GST tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 6.7 | pIC50 | >200 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of human recombinant HDAC7 | B | 6.99 | pIC50 | 102.4 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of recombinant HDAC7 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | B | 7.12 | pIC50 | 75.2 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of human HDAC7 using fluorogenic tetrapeptide RHKKAc as substrate | B | 7.46 | pIC50 | 34.4 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.47 | pIC50 | 34 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 7.67 | pIC50 | 21.6 | nM | IC50 | J Med Chem (2019) 62: 3171-3183 [PMID:30418766] |
| ChEMBL | Inhibition of HDAC7 | B | 9 | pIC50 | >1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| Histone deacetylase 8 in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797017] [UniProtKB: A5H660] | ||||||||
| ChEMBL | Inhibition of recombinant Schistosoma mansoni HDAC8 expressed in Escherichia coli using Fluor de Lys as substrate preincubated for 90 mins followed by BML-KI176 addition measured after 45 mins by fluorescence assay | B | 5.81 | pIC50 | 1560 | nM | IC50 | J Med Chem (2016) 59: 2423-2435 [PMID:26937828] |
| ChEMBL | Inhibition of Schistosoma mansoni HDAC8 using Fluor de Lys as substrate incubated for 90 mins by fluorescence method | B | 5.81 | pIC50 | 1560 | nM | IC50 | Eur J Med Chem (2021) 225: 113745-113745 [PMID:34392190] |
| ChEMBL | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | Bioorg Med Chem (2017) 25: 2105-2132 [PMID:28259528] |
| ChEMBL | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | B | 6.23 | pIC50 | 590 | nM | IC50 | Bioorg Med Chem (2017) 25: 2105-2132 [PMID:28259528] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-L-Lys(trifluoroacetyl)-MCA as substrate by fluorogenic enzymatic assay | B | 5.54 | pKd | 2900 | nM | Kd | Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579] |
| ChEMBL | Binding affinity to human recombinant HDAC8 by fluorescence assay | B | 6.24 | pKd | 580 | nM | Kd | Medchemcomm (2015) 6: 613-618 [PMID:26005563] |
| ChEMBL | Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins measured after 15 mins by microplate reader based fluorescence assay | B | 4.8 | pKi | 15700 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of recombinant human HDAC8 | B | 5.27 | pKi | 5330 | nM | Ki | Bioorg Med Chem (2020) 28: 115108-115108 [PMID:31787463] |
| ChEMBL | Inhibition of recombinant human HDAC8 enzyme using Ac-LeuGlyLys (tfa)-AMC as substrate after 15 to 30 mins | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (2013) 56: 6512-6520 [PMID:23865683] |
| ChEMBL | Inhibition of human recombinant HDAC8 using [Ac-Leu-Gly-Lys(Ac)-AMC substrate incubated for 15 to 30 mins | B | 6.15 | pKi | 700 | nM | Ki | J Med Chem (2014) 57: 9644-9657 [PMID:25380299] |
| ChEMBL | Inhibition of C-terminal His-tagged human recombinant full-length HDAC8 expressed in baculovirus expression system assessed as reduction in 7-amino-4-methylcoumarin by fluorescence based assay | B | 6.32 | pKi | 480 | nM | Ki | Eur J Med Chem (2017) 141: 188-196 [PMID:29031066] |
| ChEMBL | Activity of human HDAC8 | B | 6.32 | pKi | 480 | nM | Ki | Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Inhibition of human recombinant HDAC8 by Michaelis-Menten equation analysis | B | 6.32 | pKi | 480 | nM | Ki | ACS Med Chem Lett (2013) 4: 757-761 [PMID:24900743] |
| ChEMBL | Inhibition of human recombinant HDAC8 using fluorescent acetylated substrate | B | 6.4 | pKi | 396 | nM | Ki | J Med Chem (2009) 52: 7003-7013 [PMID:19886628] |
| ChEMBL | Inhibition of recombinant human HDAC8 expressed in Escherichia coli assessed as hydrolase activity using fluorogenic AC-LGK-tfa-AMC as substrate measured after 60 mins by fluorescence analysis | B | 6.64 | pKi | 230 | nM | Ki | Medchemcomm (2016) 7: 464-470 |
| ChEMBL | Inhibition of HDAC8 | B | 6.69 | pKi | 205 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| GtoPdb | - | - | 6.69 | pKi | 205 | nM | Ki |
Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378]; Nat Chem Biol (2010) 6: 238-243 [PMID:20139990] |
| ChEMBL | Competitive inhibition of HDAC8 using KI-104 as substrate by fluorescence assay | B | 6.76 | pKi | 173 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of recombinant human C-terminal His-fusion tagged/N-terminal Strep-2 tagged HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorescence assay | B | 4.92 | pIC50 | 11900 | nM | IC50 | J Med Chem (2019) 62: 11260-11279 [PMID:31762274] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence-based assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2016) 109: 350-359 [PMID:26814680] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) pre-incubated for 5 mins before fluorogenic substrate Boc-Lys (acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC addition and measured after 30 mins by fluorescence based assay | B | 5.02 | pIC50 | 9590 | nM | IC50 | J Med Chem (2020) 63: 4701-4715 [PMID:32267687] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using substrate after 30 mins by fluorometric analysis | B | 5.13 | pIC50 | 7468.5 | nM | IC50 | Eur J Med Chem (2017) 133: 11-23 [PMID:28371677] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells after 30 mins by fluorescence assay | B | 5.14 | pIC50 | 7300 | nM | IC50 | ACS Med Chem Lett (2018) 9: 34-38 [PMID:29348808] |
| ChEMBL | Inhibition of GST tagged full length human recombinant HDAC8 (H90 to 30H) expressed in Baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (2017) 60: 7965-7983 [PMID:28885834] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 5.25 | pIC50 | 5600 | nM | IC50 | J Med Chem (2019) 62: 3898-3923 [PMID:30901208] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorogenic substrate incubated for 30 mins by fluorescence based assay | B | 5.29 | pIC50 | 5120 | nM | IC50 | J Med Chem (2022) 65: 3667-3683 [PMID:35152694] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127638-127638 [PMID:33132117] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorogenic Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence-based assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2018) 61: 5304-5322 [PMID:29787262] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Boc-Lys(trifluoroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | Eur J Med Chem (2018) 150: 282-291 [PMID:29533873] |
| ChEMBL | Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay | B | 5.31 | pIC50 | 4890 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of human recombinant HDAC8 after 60 mins by fluorimetric assay | B | 5.31 | pIC50 | 4890 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2638-2645 [PMID:31400938] |
| ChEMBL | Inhibition of recombinant HDAC8 (unknown origin) measured after 30 mins by fluorescence assay | B | 5.37 | pIC50 | 4300 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) after 30 mins by fluorescence assay | B | 5.4 | pIC50 | 3970 | nM | IC50 | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| ChEMBL | Inhibition of C-terminal His-tagged human recombinant HDAC8 expressed in Sf9 cells after 30 mins by microtiter plate reader analysis | B | 5.43 | pIC50 | 3700 | nM | IC50 | Bioorg Med Chem (2016) 24: 1446-1454 [PMID:26907204] |
| ChEMBL | Inhibition of C-terminal His-tagged recombinant human HDAC8 (1 to 377 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay | B | 5.47 | pIC50 | 3400.1 | nM | IC50 | Eur J Med Chem (2018) 143: 792-805 [PMID:29223096] |
| ChEMBL | Inhibition of human HDAC8 using Boc-Lys(TFA)-AMC as substrate incubated 30 mins before substrate addition measured after 30 mins post substrate addition by fluorescence assay | B | 5.48 | pIC50 | 3295.01 | nM | IC50 | Eur J Med Chem (2011) 46: 4042-4049 [PMID:21712146] |
| ChEMBL | Inhibition of human recombinant HDAC8 after 30 mins by fluorescence assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2013) 56: 5782-5796 [PMID:23786452] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 5.55 | pIC50 | 2800 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate class 2A preincubated for 30 mins followed by substrate addition and measured after 15 mins by fluorogenic assay | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem (2020) 28: 115345-115345 [PMID:32061484] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) in using Boc-Lys(acetyl)-AMC or Boc-Lys (triflouroacetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 5.56 | pIC50 | 2736.9 | nM | IC50 | J Med Chem (2020) 63: 12083-12099 [PMID:33021789] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using (FAM)-labeled acetylated peptide as substrate measured after 17 hrs by fluorescence assay | B | 5.64 | pIC50 | 2290 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of HDAC8 assessed as blockade of decorboxylation of carboxyfluorescein labeled acetylated peptide substrate after 17 hrs | B | 5.64 | pIC50 | 2290 | nM | IC50 | J Med Chem (2010) 53: 1347-1356 [PMID:20055418] |
| ChEMBL | Inhibition of recombinant human C-terminal His-fusion tagged/N-terminal Strep2 tagged HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 90 mins by fluorimetry | B | 5.65 | pIC50 | 2260 | nM | IC50 | Eur J Med Chem (2021) 211: 113095-113095 [PMID:33360560] |
| ChEMBL | Inhibition of HDAC8 | B | 5.66 | pIC50 | 2185 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6588-6590 [PMID:19854643] |
| ChEMBL | Inhibition of full length recombinant human C-terminal His-tagged HDAC8 expressed in baculovirus infected sf9 cells using Boc-Lys-(TFA)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 5.67 | pIC50 | 2139 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of HDAC8 in human HeLa cells nuclear extract using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry | B | 5.7 | pIC50 | 2000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127128-127128 [PMID:32247729] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 30 mins by spectrophotometry | B | 5.7 | pIC50 | 2000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 703-707 [PMID:21984958] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorophore-conjugated substrate by fluorescence assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 929-932 [PMID:27774131] |
| ChEMBL | Inhibition of HDAC8 | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem (2010) 18: 4103-4110 [PMID:20472442] |
| ChEMBL | Inhibition of HDAC8 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | B | 5.7 | pIC50 | 1989 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3283-3287 [PMID:23622981] |
| ChEMBL | Inhibition of HDAC8 in human HeLa cell nuclear extract using Fluor de Lys as substrate after 15 mins by fluorometric analysis | B | 5.7 | pIC50 | 1989 | nM | IC50 | J Med Chem (2012) 55: 1465-1477 [PMID:22260166] |
| ChEMBL | Inhibition of human HDAC8 using Z-L-Lys(eta-trifluoroacetyl)-AMC as substrate after 90 mins by fluorescence analysis | B | 5.72 | pIC50 | 1890 | nM | IC50 | J Med Chem (2016) 59: 1545-1555 [PMID:26653328] |
| ChEMBL | Inhibition of HDAC8 from human HeLa cells nuclear extract by cell free fluorimetric assay | B | 5.73 | pIC50 | 1860 | nM | IC50 | J Med Chem (2009) 52: 456-468 [PMID:19093884] |
| ChEMBL | Inhibition of HDAC8 | B | 5.73 | pIC50 | 1860 | nM | IC50 | J Med Chem (2010) 53: 6100-6111 [PMID:20669972] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of HDAC8 expressed in Escherichia coli | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2008) 51: 2350-2353 [PMID:18370373] |
| ChEMBL | Inhibition of human recombinant HDAC8 by fluorimetry | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2009) 52: 2909-2922 [PMID:19419205] |
| ChEMBL | Inhibition of His-tagged HDAC8 catalytic domain expressed in Escherichia coli | B | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3081-3084 [PMID:19410459] |
| ChEMBL | Inhibition of C-terminal His-tagged HDAC8 expressed in Escherichia coli | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2009) 52: 3453-3456 [PMID:19441846] |
| ChEMBL | Inhibition of recombinant HDAC8 (unknown origin) using fluorogenic substrate Boc-Lys (acetyl)-AMC after 20 mins by homogeneous fluorescence release assay | B | 5.77 | pIC50 | 1680 | nM | IC50 | Eur J Med Chem (2015) 96: 1-13 [PMID:25874326] |
| ChEMBL | Inhibition of recombinant HDAC8 (unknown origin) incubated for 10 mins using Boc-Lys(acetyl)-AMC fluorogenic substrate by homogeneous fluorescence release assay | B | 5.77 | pIC50 | 1680 | nM | IC50 | Bioorg Med Chem (2015) 23: 3457-3471 [PMID:25953722] |
| ChEMBL | Inhibition of HDAC8 after 45 mins by microplate fluorometric analysis | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2012) 20: 5738-5744 [PMID:22967811] |
| ChEMBL | Inhibition of HDAC8 | B | 5.82 | pIC50 | 1524 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Inhibition of full length C-terminal 6x-His tagged human HDAC8 using Arg-His-Lys(Ac)-Lys(Ac) substrate incubated for 2 hrs by fluorescence assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5450-5454 [PMID:25454270] |
| ChEMBL | Inhibition of HDAC8 by fluorometric assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2012) 55: 9562-9575 [PMID:23116147] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) expressed in Escherichia coli using Boc-Lys (acetyl)-AMC as substrate incubated for 5 min prior to substrate addition measured after 30 min by fluorescence assay | B | 5.83 | pIC50 | 1480 | nM | IC50 | Med Chem Res (2012) 21: 152-156 |
| ChEMBL | Inhibition of HDAC8 expressed in Escherichia coli assessed as Boc-Lys (acetyl)-AMC substrate hydrolysis by fluorimetric assay | B | 5.83 | pIC50 | 1480 | nM | IC50 | Bioorg Med Chem (2010) 18: 1761-1772 [PMID:20171895] |
| ChEMBL | Inhibition of recombinant human full length GST-tagged HDAC8 expressed in Escherichia coli DH5alpha (DE3) assessed as inhibition of deacetylation activity using Fluor-de-Lys as substrate measured after 15 mins by fluorimetric assay | B | 5.83 | pIC50 | 1480 | nM | IC50 | Bioorg Med Chem (2016) 24: 5611-5617 [PMID:27665180] |
| ChEMBL | Inhibition of HDAC8 in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay | B | 5.85 | pIC50 | 1410 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC8 | B | 5.86 | pIC50 | 1374.7 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 5.87 | pIC50 | 1350 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3346-3348 [PMID:23591111] |
| ChEMBL | Inhibition of human recombinant HDAC8 using MAZ1675 as fluorogenic substrate measured every 5 mins by optimized homogenous fluorescence based assay | B | 5.87 | pIC50 | 1337 | nM | IC50 | J Med Chem (2015) 58: 4812-4821 [PMID:25974739] |
| ChEMBL | Inhibition of full length recombinant human C-terminal His tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-GlyLys (Tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence microtiter plate reader assay | B | 5.88 | pIC50 | 1320 | nM | IC50 | J Med Chem (2022) 65: 2434-2457 [PMID:35043615] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 10 mins followed by substrate addition and further incubated for incubated for 1 hrs by fluorescence microtiter plate reader assay | B | 5.89 | pIC50 | 1279.3 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of human recombinant HDAC8 expressed in Escherichia coli using Z-L-Lys(epsilon-trifluoroacetyl)-AMC as substrate measured after 90 mins by fluorescence assay | B | 5.9 | pIC50 | 1260 | nM | IC50 | J Med Chem (2017) 60: 5493-5506 [PMID:28574690] |
| ChEMBL | Inhibition of HDAC8 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibition of Flag tagged human recombinant HDAC8 expressed in Sf21 cells | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2010) 53: 8546-8555 [PMID:21080629] |
| ChEMBL | Inhibition of HDAC8 after 17 hrs | B | 5.94 | pIC50 | 1140 | nM | IC50 | J Med Chem (2008) 51: 4370-4373 [PMID:18642892] |
| ChEMBL | Inhibition of full length HDAC8 assessed as 7-amino-4-methylcoumarin release from fluorophore conjugated substrate after 5 mins by fluorescence assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2601-2605 [PMID:21334896] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Boc-Lys(TFA)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence-based assay | B | 5.99 | pIC50 | 1030 | nM | IC50 | J Med Chem (2021) 64: 4810-4840 [PMID:33830764] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 5.99 | pIC50 | 1020 | nM | IC50 | Medchemcomm (2014) 5: 1829-1833 |
| ChEMBL | Inhibition of HDAC8 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 5.99 | pIC50 | 1020 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of recombinant human full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant human full length HDAC8 using Fluor-de-Lys as substrate after 60 mins by spectrofluorimetric analysis | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2017) 134: 13-23 [PMID:28395150] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) after 60 mins by fluorescence assay | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of human full-length recombinant C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells preincubated for 5 mins followed by HDAC substrate addition and further incubated for 45 mins by fluorescence microplate reader assay | B | 6.01 | pIC50 | 980 | nM | IC50 | Eur J Med Chem (2021) 222: 113569-113569 [PMID:34111829] |
| ChEMBL | Inhibition of human HDAC8 by fluorescence assay | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (2013) 56: 427-436 [PMID:23252603] |
| ChEMBL | Inhibition of human HDAC8 | B | 6.09 | pIC50 | 820 | nM | IC50 | J Med Chem (2008) 51: 1505-1529 [PMID:18247554] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.11 | pIC50 | 780 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4885-4888 [PMID:28947154] |
| ChEMBL | Inhibition of recombinant full-length human C-terminal HDAC8 expressed in baculovirus infected Sf9 insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC8 expressed in Escherichia coli BL21(DE3) cells using Boc-Lys(TFA)-AMC as substrate preincubated for 5 followed by substrate addition and measured after 30 mins by fluorescence based assay | B | 6.11 | pIC50 | 776 | nM | IC50 | ACS Med Chem Lett (2020) 11: 713-719 [PMID:32435375] |
| ChEMBL | Inhibition of human HDAC8 expressed in Escherichia coli using Boc-Lys (acetyl)-AMC as substrate treated for 5 mins before substrate addition measured after 30 mins by fluorescence assay | B | 6.15 | pIC50 | 700 | nM | IC50 | Eur J Med Chem (2011) 46: 5387-5397 [PMID:21924799] |
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected in Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 6.17 | pIC50 | 682 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of full length human N-terminal FLAG-tagged HDAC8 (1 to 377 residues) expressed in HEK293 cells preincubated for 15 mins followed by Boc-[trifluoroacetyl-Lys]-AMC substrate addition measured after 30 mins by fluorimetric method | B | 6.17 | pIC50 | 669 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1301-1305 [PMID:30613344] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac)AMC as substrate | B | 6.18 | pIC50 | 660 | nM | IC50 | J Med Chem (2015) 58: 2809-2820 [PMID:25734520] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Ac-peptide as a substrate pretreated for 15 mins followed by substrate addition | B | 6.19 | pIC50 | 646 | nM | IC50 | Eur J Med Chem (2021) 225: 113824-113824 [PMID:34509167] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.19 | pIC50 | 645 | nM | IC50 | Eur J Med Chem (2021) 218: 113392-113392 [PMID:33831778] |
| ChEMBL | Inhibition of human recombinant full length HDAC8 using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of human recombinant full-length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cell preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 mins by fluorimetric method | B | 6.27 | pIC50 | 540 | nM | IC50 | Eur J Med Chem (2018) 143: 1790-1806 [PMID:29150330] |
| ChEMBL | Inhibition of full length human C-terminal His-tag HDAC8 expressed in baculovirus expression system preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA | B | 6.27 | pIC50 | 540 | nM | IC50 | ACS Med Chem Lett (2017) 8: 281-286 [PMID:28337317] |
| ChEMBL | Inhibition of HADC8 (unknown origin) | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) by ELISA-based assay | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3254-3258 [PMID:28648461] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) incubated for 30 mins by microplate reader assay | B | 6.3 | pIC50 | >500 | nM | IC50 | Eur J Med Chem (2022) 229: 114058-114058 [PMID:34954595] |
| ChEMBL | Inhibition of human KDAC8 | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2016) 59: 1613-1633 [PMID:26681404] |
| ChEMBL | Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay | B | 6.3 | pIC50 | 497 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Inhibition of human recombinant HDAC8 using fluor de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 25 mins by microplate reader analysis | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6621-6627 [PMID:23010266] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) expressed in Escherichia coli using BML-KI-178 as substrate preincubated up to 3 hrs and measured after 35 mins by fluorescence assay | B | 6.36 | pIC50 | 440 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of human recombinant HDAC8 using Fluor de Lys as substrate | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2011) 54: 4350-4364 [PMID:21548582] |
| ChEMBL | Inhibition of human recombinant HDAC8 using fluorescent acetylated substrate | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2009) 52: 7003-7013 [PMID:19886628] |
| ChEMBL | Inhibition of human recombinant HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins and measured after 30 mins by fluorescence assay | B | 6.37 | pIC50 | 425 | nM | IC50 | Eur J Med Chem (2019) 168: 515-526 [PMID:30851694] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.37 | pIC50 | 425 | nM | IC50 | Eur J Med Chem (2018) 144: 398-409 [PMID:29288941] |
| ChEMBL | Inhibition of human HDAC8 using Boc-Lys (Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay | B | 6.37 | pIC50 | 425 | nM | IC50 | J Nat Prod (2019) 82: 1442-1450 [PMID:31120744] |
| ChEMBL | Inhibition of HDAC8 | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 726-731 [PMID:18060775] |
| ChEMBL | Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 90 mins by fluorescence based micro plate assay | B | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2021) 225: 113745-113745 [PMID:34392190] |
| ChEMBL | Inhibition of recombinant human HDAC8 expressed in baculovirus expression system using fluorogenic Arg-His-Lys(Ac)-Lys(Ac) as substrate incubated for 90 mins by fluorescence assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2019) 62: 1138-1166 [PMID:30645113] |
| ChEMBL | Inhibition of recombinant human HDAC8 using Fluor de Lys as substrate preincubated for 90 mins followed by BML-KI176 addition measured after 45 mins by fluorescence assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2016) 59: 2423-2435 [PMID:26937828] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.43 | pIC50 | 370 | nM | IC50 | Eur J Med Chem (2019) 164: 214-240 [PMID:30594678] |
| ChEMBL | Inhibition of HDAC8 in human HeLa cell nuclear extract using Boc-Lys (Ac)-AMC as substrate after 60 mins by fluorometric analysis | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2015) 58: 9214-9227 [PMID:26555243] |
| ChEMBL | Inhibition of full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 240 mins by fluorescence based assay | B | 6.48 | pIC50 | 328 | nM | IC50 | Eur J Med Chem (2019) 182: 111672-111672 [PMID:31505452] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorogenic peptide as substrate by fluorescence assay | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2014) 57: 8026-8034 [PMID:25238284] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using RHK(Ac)K(Ac) fluorogenic acetylated peptide substrate by fluorometric assay | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4320-4324 [PMID:26264503] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorogenic peptide from p53 residues (379 to 382) (RHK(Ac)K(Ac)) as substrate by fluorescence assay | B | 6.51 | pIC50 | 306 | nM | IC50 | ACS Med Chem Lett (2013) 4: 779-783 [PMID:24015327] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus-infected Sf9 insect cells using Ac-peptide as substrate incubated for 4 hrs followed by trypsin addition and further incubated for 2 hrs | B | 6.52 | pIC50 | 302.6 | nM | IC50 | J Med Chem (2022) 65: 4156-4181 [PMID:35175762] |
| ChEMBL | Inhibition of HDAC8 by in vitro deacetylation assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of HDAC 8 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of recombinant HDAC8 (unknown origin) using Fluor-de-Lys-HDAC8 as substrate by fluorescence assay | B | 6.52 | pIC50 | 300 | nM | IC50 | J Nat Prod (2014) 77: 49-56 [PMID:24328302] |
| ChEMBL | Inhibition of His-tagged full length recombinant human HDAC8 expressed in baculovirus expression system assessed as release of 7-amino-4-methylcoumarin by fluorogenic assay | B | 6.52 | pIC50 | >300 | nM | IC50 | Eur J Med Chem (2016) 122: 92-101 [PMID:27344487] |
| ChEMBL | Inhibition of Histone deacetylase 8 (HDAC8) of HeLa nuclear extracts | B | 6.54 | pIC50 | 290 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 449-453 [PMID:14698179] |
| ChEMBL | Inhibition of HDAC8 | B | 6.57 | pIC50 | 272 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence based microplate reader analysis | B | 6.58 | pIC50 | 261 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.6 | pIC50 | 250 | nM | IC50 | Bioorg Med Chem Lett (2021) 49: 128286-128286 [PMID:34314844] |
| ChEMBL | Inhibition of human HDAC-8 using RHK(Ac)K(Ac) as substrate | B | 6.61 | pIC50 | 243 | nM | IC50 | Eur J Med Chem (2014) 76: 53-60 [PMID:24565573] |
| ChEMBL | Inhibition of human HDAC8 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.61 | pIC50 | 243 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis | B | 6.61 | pIC50 | 243 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 61-64 [PMID:24345446] |
| ChEMBL | Inhibition of human HDAC8 by fluorimetric assay | B | 6.61 | pIC50 | 243 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using fluorogenic tetrapeptide RHK(Ac)K(Ac) substrate by fluorescence assay | B | 6.61 | pIC50 | 243 | nM | IC50 | J Med Chem (2014) 57: 8358-8377 [PMID:25233084] |
| ChEMBL | Inhibition of human HDAC8 using RHK(Ac)K(Ac) as substrate by fluorimetric analysis | B | 6.61 | pIC50 | 243 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| ChEMBL | Inhibition of human HDAC-8 using RHKK(Ac) as substrate by fluorescence assay | B | 6.61 | pIC50 | 243 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human recombinant C-terminal His-tagged HDAC8 (1 to 377 residues) expressed in insect cells using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human recombinant HDAC8 using AMC-K(Ac)GL as substrate by fluorescence based assay | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2020) 11: 977-983 [PMID:32435414] |
| ChEMBL | Inhibition of HDAC8 catalytic domain (unknown origin) expressed in Escherichia coli BL21 (DE3) using GRKacFGC as substrate after 60 mins by SAMDI mass spectrometric analysis | B | 6.63 | pIC50 | 232 | nM | IC50 | J Med Chem (2013) 56: 9969-9981 [PMID:24304348] |
| ChEMBL | Fluor de Lys Assay: Fluor de Lys is a fluorescence based HDAC activity assay comprising a combination of fluorogenic Histone deAcetylase Lysyl substrate and a developer. The kit is a highly sensitive and convenient alternative to radiolabeled, acetylated histones or peptide/HPLC methods for the assay of histone deacetylases. This assay is based on the ability of HeLa nuclear extract, which is enriched in HDAC activity, to mediate the deacetylation of the acetylated lysine side chain of the Fluor de Lys substrate. The assay procedure requires two steps. First, incubation of the HeLa nuclear extract with the Fluor de Lys substrate results in substrate deacetylation and thus sensitizes it to the second step. In the second step, treatment of the deacetylated substrate with the Fluor de Lys developer produces a fluorophore. The substrate-developer reaction, under normal circumstances goes to completion in less than 1 min at 25 C. | B | 6.63 | pIC50 | 232 | nM | IC50 | US-8871728-B2. Non-peptide macrocyclic histone deacetylese (HDAC) inhibitors and methods of making and using thereof (2014) |
| ChEMBL | Inhibition of HDAC8 (unknown origin) after 60 mins by SAMDI spectrophotometric analysis | B | 6.63 | pIC50 | 232 | nM | IC50 | J Med Chem (2013) 56: 3492-3506 [PMID:23547652] |
| ChEMBL | Inhibition of His-tagged HDAC8 (unknown origin) expressed in Escherichia coli BL21(DE3) after 60 mins by MALDI mass spectrometry | B | 6.63 | pIC50 | 232 | nM | IC50 | Eur J Med Chem (2015) 96: 340-359 [PMID:25899338] |
| ChEMBL | Inhibition of recombinant full length human HDAC8 expressed in Baculovirus infected insect Sf9 cells preincubated for 30 mins followed by substrate addition measured after 15 to 45 mins by luminescence assay | B | 6.64 | pIC50 | 230 | nM | IC50 | Medchemcomm (2014) 5: 1887-1891 |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3289-3293 [PMID:28648462] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) by fluorescence based assay | B | 6.69 | pIC50 | 205.2 | nM | IC50 | Eur J Med Chem (2021) 209: 112868-112868 [PMID:33077265] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 6.71 | pIC50 | 195 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant HDAC8 (unknown origin) using Ac-peptide-AMC as substrate incubated for 240 mins by microplate reader analysis | B | 6.72 | pIC50 | 191.5 | nM | IC50 | J Med Chem (2022) 65: 1243-1264 [PMID:33586434] |
| ChEMBL | Inhibition of human recombinant HDAC8 using Ac-Leu-Gly-Lys(Ac)-AMC as substrate by measuring fluorescence intensity incubated for 30 mins by microplate reader assay | B | 6.73 | pIC50 | 188 | nM | IC50 | Eur J Med Chem (2021) 217: 113363-113363 [PMID:33744687] |
| ChEMBL | Inhibition of human HDAC8 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6.76 | pIC50 | 172 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 6.76 | pIC50 | 172 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 6.92 | pIC50 | 119 | nM | IC50 | Eur J Med Chem (2016) 108: 274-286 [PMID:26689485] |
| ChEMBL | Inhibition of human HDAC8 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of full length human C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 7.08 | pIC50 | 83 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) measured after 30 mins by fluorescence microplate reader assay | B | 7.08 | pIC50 | 82.96 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of human HDAC8 | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3906-3910 [PMID:20605448] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in sf9 insect cells using Boc-Lys(TFA)-AM as substrate incubated for 60 mins by fluorescence assay | B | 7.36 | pIC50 | 44 | nM | IC50 | Eur J Med Chem (2020) 192: 112189-112189 [PMID:32151834] |
| ChEMBL | Inhibition of human recombinant HDAC8 incubated for 15 mins by fluorogenic assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2021) 40: 116185-116185 [PMID:33965842] |
| ChEMBL | Inhibition of recombinant C-terminal His-tagged full length human HDAC8 expressed in baculovirus infected insect Sf9 cells using fluorogenic HDAC class 2a substrate after 30 mins by fluorescence assay | B | 8.06 | pIC50 | 8.8 | nM | IC50 | ACS Med Chem Lett (2015) 6: 239-243 [PMID:25815139] |
| ChEMBL | Inhibition of full length human recombinant HDAC8 expressed in baculovirus infected insect S9 cells using Ac-Leu-GlyLys(Tfa)-AMC as substrate after 30 mins by fluorescence assay | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (2015) 58: 4325-4338 [PMID:25906087] |
| ChEMBL | Inhibition of HDAC8 | B | 9 | pIC50 | >1 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5528-5532 [PMID:18809328] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of HDAC9 | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2008) 51: 2898-2906 [PMID:18412327] |
| ChEMBL | Inhibition of HDAC9 | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-3321 [PMID:20451378] |
| GtoPdb | - | - | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 3314-21 [PMID:20451378] |
| ChEMBL | Competitive inhibition of HDAC9 using KI-104 as substrate by fluorescence assay | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2011) 54: 4694-4720 [PMID:21634430] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) | B | 4.1 | pIC50 | 80030 | nM | IC50 | Medchemcomm (2014) 5: 342-351 |
| ChEMBL | Inhibition of HDAC9 (unknown origin) using Ac-LeuGlyLys(tfa)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | B | 4.19 | pIC50 | 64000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1122-1127 [PMID:31413795] |
| ChEMBL | Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2A by fluorescence assay | B | 4.29 | pIC50 | 51290 | nM | IC50 | Eur J Med Chem (2019) 164: 263-272 [PMID:30597327] |
| ChEMBL | Inhibition of human recombinant HDAC9 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 4.31 | pIC50 | 49000 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) assessed as fluorescence intensity measured after 60 mins incubation at room temperature by trypsin-free microfluidic lab-on-a-chip assay | B | 4.48 | pIC50 | >33330 | nM | IC50 | J Med Chem (2013) 56: 1772-1776 [PMID:23368884] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) after 60 mins by fluorescence assay | B | 4.48 | pIC50 | >33000 | nM | IC50 | J Med Chem (2013) 56: 4816-4820 [PMID:23672185] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using fluorogenic HDAC 2A substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay | B | 4.49 | pIC50 | 32260 | nM | IC50 | Eur J Med Chem (2020) 192: 112193-112193 [PMID:32151835] |
| ChEMBL | Inhibition of human recombinant HDAC9 after 60 mins by fluorimetric assay | B | 4.64 | pIC50 | 22800 | nM | IC50 | Eur J Med Chem (2014) 86: 639-652 [PMID:25218912] |
| ChEMBL | Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus-infected Sf9 cells using Boc Lys(TFA)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubated for 30 mins by fluorogenic assay | B | 4.8 | pIC50 | 15830 | nM | IC50 | Eur J Med Chem (2021) 219: 113419-113419 [PMID:33845233] |
| ChEMBL | Inhibition of C-terminal His-tagged human recombinant HDAC9 (amino acids 604- 1066) expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by fluorescence analysis | B | 4.81 | pIC50 | 15600 | nM | IC50 | ACS Med Chem Lett (2013) 4: 132-136 [PMID:24900575] |
| ChEMBL | Inhibition of C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in 7-amino-4-methylcoumarin release measured every 5 mins by fluorescence based analysis | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2021) 42: 116251-116251 [PMID:34116381] |
| ChEMBL | Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of HDAC 9 in human HeLa nuclear extract using fluorogenic HDAC class 2A substrate measured after 60 mins by fluorometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 3484-3497 [PMID:28368585] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) using biotinylated histone H3 KAc peptide (1 to 21 residues) as substrate by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 3678-3700 [PMID:32153186] |
| ChEMBL | Inhibition of recombinant C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate after 1 hr by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 178: 116-130 [PMID:31177073] |
| ChEMBL | Inhibition of recombinant human HDAC9 measured after 30 mins by fluorescence microplate reader assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2021) 64: 15280-15296 [PMID:34624191] |
| ChEMBL | Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay | B | 5.45 | pIC50 | 3570 | nM | IC50 | J Med Chem (2015) 58: 7672-7680 [PMID:26331334] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect cells using 7-AMC-labelled HDAC substrate measured after 30 mins by fluorescence assay | B | 5.51 | pIC50 | 3100 | nM | IC50 | Eur J Med Chem (2018) 158: 620-706 [PMID:30245394] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal GST-tagged HDAC9 (1 to 1069 residues) expressed in wheat germ expression system using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate measured after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 205: 112648-112648 [PMID:32791401] |
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC9 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2019) 62: 1577-1592 [PMID:30629434] |
| ChEMBL | Inhibition of human HDAC9 using RHK-K(Ac)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2016) 112: 99-105 [PMID:26890116] |
| ChEMBL | Inhibition of human HDAC-9 using RHKK(Ac) as substrate by fluorescence assay | B | 6.5 | pIC50 | 316 | nM | IC50 | J Med Chem (2014) 57: 2258-2274 [PMID:24588105] |
| ChEMBL | Inhibition of human HDAC9 using fluorogenic tetrapeptide RHKKAc as substrate | B | 6.5 | pIC50 | 316 | nM | IC50 | Eur J Med Chem (2014) 79: 251-259 [PMID:24742384] |
| ChEMBL | Inhibition of human HDAC9 by fluorimetric assay | B | 6.5 | pIC50 | 316 | nM | IC50 | J Med Chem (2010) 53: 8387-8399 [PMID:21073160] |
| ChEMBL | Inhibition of human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys(acetyl)-AMC as fluorogenic substrate measured after 1 hr by flourescence plate reader method | B | 6.7 | pIC50 | >200 | nM | IC50 | Eur J Med Chem (2021) 225: 113799-113799 [PMID:34500130] |
| ChEMBL | Inhibition of HDAC9 by in vitro deacetylation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Nat Chem Biol (2010) 6: 25-33 [PMID:19966789] |
| ChEMBL | Inhibition of human recombinant HDAC9 | B | 6.97 | pIC50 | 107.2 | nM | IC50 | Eur J Med Chem (2009) 44: 1067-1085 [PMID:18672316] |
| ChEMBL | Inhibition of human HDAC9 pre-incubated for 30 mins before substrate addition and measured after 30 mins by HDAC-Glo I/II assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem (2014) 22: 3720-3731 [PMID:24864038] |
| ChEMBL | Inhibition of human HDAC9 using ArgHisLysLys(Ac) fluorogenic peptide as a substrate by fluorimetric assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2011) 54: 2165-2182 [PMID:21417297] |
| Histone deacetylase HD1B in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3541] [UniProtKB: Q9ZTP8] | ||||||||
| ChEMBL | Inhibition of maize histone deacetylase 1B | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2008) 43: 621-632 [PMID:17698257] |
| ChEMBL | Inhibition of maize HD1B | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
| Histone deacetylase HD2 in Zea mays (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4919] [UniProtKB: Q94F81] | ||||||||
| ChEMBL | Binding affinity against Histone deacetylase 2 (HD2) in maize, expressed as binding constant (pKi) | B | 6.88 | pKi | 131.83 | nM | Ki | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
| ChEMBL | Experimental anti-HDAC (anti-histone deacetylase) activity of the compound | B | 6.88 | pKi | 131.83 | nM | Ki | J Med Chem (2001) 44: 2069-2072 [PMID:11405644] |
| ChEMBL | Inhibition of in vitro enzyme activity measured in a highly purified maize Histone deacetylase 2 preparation | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2002) 45: 3296-3309 [PMID:12109913] |
| ChEMBL | Inhibitory concentration against maize Histone deacetylase 2 | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2003) 46: 5097-5116 [PMID:14613312] |
| ChEMBL | Inhibition of maize Histone deacetylase 2 | B | 7.3 | pIC50 | 50.12 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
| ChEMBL | Tested for maize Histone deacetylase 2 inhibitory activity | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2003) 46: 4826-4829 [PMID:14584932] |
| ChEMBL | Inhibition of maize histone deacetylase 2 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2004) 47: 1351-1359 [PMID:14998325] |
| ChEMBL | In vitro for anti-HD2 (Histone deacetylase 2) activity in maize | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2002) 45: 1778-1784 [PMID:11960489] |
| ChEMBL | Concentration required for inhibition of histone deacetylase HD2 in vitro. | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2004) 47: 1098-1109 [PMID:14971890] |
| ChEMBL | Inhibitory concentration against histone deacetylase activity | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2001) 44: 2069-2072 [PMID:11405644] |
| ChEMBL | Inhibitory concentration against maize histone deacetylase 2 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2005) 48: 3344-3353 [PMID:15857140] |
| ChEMBL | Inhibitory concentration against Histone deacetylase 2 in maize | F | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4656-4661 [PMID:16165353] |
| ChEMBL | Inhibition of maize HD2 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2006) 49: 6046-6056 [PMID:17004718] |
| Histone deacetylase-like amidohydrolase in Alcaligenes sp. (strain DSM 11172) (Bordetella sp. (strain FB188)) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6017] [UniProtKB: Q70I53] | ||||||||
| ChEMBL | Inhibition of Bordetella FB188 HDAH using Boc-L-Lys(acetyl)-MCA as substrate by fluorogenic enzymatic assay | B | 6.52 | pKd | 300 | nM | Kd | Bioorg Med Chem (2012) 20: 985-995 [PMID:22182579] |
| ChEMBL | Displacement of Atto700-HA from Bordetella / Alcaligenes strain FB188 HDAH by fluorescence anisotropy | B | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
| ChEMBL | Binding affinity to Bordetella / Alcaligenes strain FB188 HDAC by FRET assay | B | 6 | pKi | 1000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
| ChEMBL | Inhibition of Bordetella / Alcaligenes strain FB188 HDAH by fluorimetric assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3651-3656 [PMID:19457659] |
| euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7] | ||||||||
| ChEMBL | Inhibition of human G9a enzyme using histone monomethyl-H3K9 peptide as substrate incubated for 1 hr in presence of SAM by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035] | ||||||||
| ChEMBL | Inhibition of recombinant HMG-CoA reductase (unknown origin) after 10 mins by spectrophotometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 3645-3655 [PMID:23570542] |
| ChEMBL | Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negative control. HMGR activity under defined assay conditions, containing NADPH and HMG-CoA substrate in a final volume of 0.2 mL of 100 mM potassium phosphatate buffer (120 mM KCl, 1 mM EDTA, 5 mM DTT, pH 7.4), were initiated in the presence or absence (control) of test compounds dissolved in dimethylsulfoxide (DMSO). The rates of NADPH consumption were monitored every 20 seconds, for up to 10 minutes, by spectrophotometer at 37° C. and 340 nm. | B | 5 | pIC50 | >10000 | nM | IC50 | US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016) |
| Human immunodeficiency virus type 1 Tat protein in Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4011] [UniProtKB: P04608] | ||||||||
| ChEMBL | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | B | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2019) 62: 5148-5175 [PMID:30973727] |
| Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4618] [GtoPdb: 1395] [UniProtKB: P09960] | ||||||||
| ChEMBL | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | B | 5.12 | pIC50 | 7650 | nM | IC50 | J Med Chem (2017) 60: 1817-1828 [PMID:28218840] |
| Leukotriene A4 hydrolase/Leukotriene A4 hydrolase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3738] [GtoPdb: 1395] [UniProtKB: P24527] | ||||||||
| ChEMBL | Inhibition of LTA4H in C57BL/6 mouse assessed as reduction in LTB4 production pre-incubated for 30 mins before 5-(methylamino)-2-({(2R,3R,6S,8S,9R,11R)-3,9,11-trimethyl-8-[(1S)-1-methyl-2-oxo-2-(1H-pyrrol-2-yl)ethyl]-1,7-dioxaspiro[5.5]undec-2-yl}methyl)-1,3-benzoxazole-4-carboxylic acid stimulation for 30 mins by ELISA | B | 5.21 | pIC50 | 6150 | nM | IC50 | J Med Chem (2017) 60: 1817-1828 [PMID:28218840] |
| lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
| ChEMBL | Inhibition of JMJD2E pre-incubated for 30 mins | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2011) 19: 3625-3636 [PMID:21596573] |
| lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341] | ||||||||
| ChEMBL | Inhibition of recombinant LSD1 (157 to 852 amino acids) (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 substrate by amplex red and horseradish peroxidase based fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| ChEMBL | Inhibition of recombinant LSD1 (157 to 852 residues) (unknown origin) expressed in Escherichia coli BL21 (DE) using H3K4me2 as substrate by amplex red assay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2021) 220: 113453-113453 [PMID:33957387] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Inhibition of MAOA (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of MAOB (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| sirtuin 5/NAD-dependent protein deacylase sirtuin-5, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2163183] [GtoPdb: 2711] [UniProtKB: Q9NXA8] | ||||||||
| ChEMBL | Inhibition of SIRT5 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 5582-5590 [PMID:22583019] |
| MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987] | ||||||||
| ChEMBL | Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (2018) 61: 7245-7260 [PMID:30045621] |
| phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336] | ||||||||
| ChEMBL | Inhibition of full length recombinant human His-tagged p110 alpha/p85 alpha expressed in baculovirus expression system incubated for 1 hr by kinase-glo assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 5488-5504 [PMID:27186676] |
| Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653] | ||||||||
| ChEMBL | Antiplasmodial activity against liver stage exo-erythrocytic forms of Plasmodium berghei sporozoites infected in human HepG2-A16-CD81EGFP cells assessed as inhibition of parasite growth compound incubated with cells for 24 hrs prior to infection and measured after 48 hrs by BrightGlo reagent based multilabel reader analysis | F | 6.54 | pIC50 | 290 | nM | IC50 | Eur J Med Chem (2021) 211: 113065-113065 [PMID:33360801] |
| ChEMBL | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells | F | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| ChEMBL | Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method | F | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| ChEMBL | Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs | F | 6.85 | pIC50 | 140 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| ChEMBL | Antiplasmodial activity against exo-erythrocytic stage of GFP-Luc-fused Plasmodium berghei ANKA infected in human HepG2 cells after 48 hrs by bioluminescence assay | F | 8.11 | pIC50 | 7.7 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Gametocytocidal activity against synchronized Plasmodium falciparum NF54 mature stage 5 gametocytes after 48 hrs by ATP bioluminescence assay | F | 5.55 | pIC50 | 2800 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method | F | 5.77 | pIC50 | 1680 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| ChEMBL | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based microscopic method | F | 5.77 | pIC50 | 1680 | nM | IC50 | J Med Chem (2017) 60: 4780-4804 [PMID:28241112] |
| ChEMBL | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method | F | 5.85 | pIC50 | 1410 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | F | 5.89 | pIC50 | 1300 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1454-1461 [PMID:18212103] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum HB3 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | F | 6.02 | pIC50 | 950 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1727-1734 [PMID:19223622] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | F | 6.05 | pIC50 | 900 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1727-1734 [PMID:19223622] |
| ChEMBL | Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method | F | 6.09 | pIC50 | 810 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in O+ human erythrocytes by [3H]hypoxanthine incorporation assay | F | 6.1 | pIC50 | 800 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1454-1461 [PMID:18212103] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum | F | 6.1 | pIC50 | 800 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1454-1461 [PMID:18212103] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | F | 6.12 | pIC50 | 750 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1727-1734 [PMID:19223622] |
| ChEMBL | Antimalarial activity against trophozoites stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 6.28 | pIC50 | 520 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 6.48 | pIC50 | 329 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum TM91C235 by hypoxanthine uptake | F | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum TM91C235 | F | 6.51 | pIC50 | 309.5 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum | F | 6.52 | pIC50 | 301 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against ring stage Plasmodium falciparum 3D7 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | F | 6.56 | pIC50 | 274 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
| ChEMBL | Antimalarial activity against ring stage Plasmodium falciparum K1 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay | F | 6.58 | pIC50 | 262 | nM | IC50 | Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059] |
| ChEMBL | Antiparasitic activity against drug-resistant Plasmodium falciparum Dd2 infected in erythrocytes assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay | F | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2017) 127: 22-40 [PMID:28038325] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum D6 by hypoxanthine uptake | F | 6.61 | pIC50 | 247 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine incorporation | F | 6.61 | pIC50 | 247 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum D6 infected in Aotus lemurinus lemurinus monkey | F | 6.61 | pIC50 | 246.6 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | F | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2009) 52: 2185-2187 [PMID:19317450] |
| ChEMBL | Antiplasmodial activity against asynchronous asexual culture of Plasmodium falciparum NF54 assessed as parasite growth inhibition | F | 6.76 | pIC50 | 175 | nM | IC50 | J Med Chem (2021) 64: 10403-10417 [PMID:34185525] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 by hypoxanthine uptake | F | 6.79 | pIC50 | 161 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation | F | 6.79 | pIC50 | 161 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum W2 | F | 6.79 | pIC50 | 160.9 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant asexual ring stage Plasmodium falciparum Dd2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | F | 6.84 | pIC50 | 146 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antiplasmodial activity against drug-sensitive asexual ring stage Plasmodium falciparum 3D7 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | F | 6.86 | pIC50 | 139 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Inhibition of HDAC in Plasmodium falciparum 3D7 by fluorescent activity assay | B | 6.9 | pIC50 | 127 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1727-1734 [PMID:19223622] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method | F | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method | F | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2018) 158: 801-813 [PMID:30245402] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in mouse RAW264.7 cells | F | 6.96 | pIC50 | 110 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum TM90C2A by hypoxanthine uptake | F | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2008) 51: 3437-3448 [PMID:18494463] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum TM90C2A | F | 6.96 | pIC50 | 109.7 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 3467-3477 [PMID:18644969] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum infected in erythrocytes after 2 hrs | F | 6.96 | pIC50 | 109 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| ChEMBL | Antiplasmodial activity against drug-sensitive asexual intraerythrocytic stage of Plasmodium falciparum 3D7 infected in human O+ erythrocytes assessed as inhibition of parasite growth incubated for 48 hrs followed by addition of [3H]hypoxanthine for 24 hrs by [3H]hypoxanthine incorporation assay | F | 7.16 | pIC50 | 69 | nM | IC50 | Eur J Med Chem (2021) 211: 113065-113065 [PMID:33360801] |
| Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922] | ||||||||
| ChEMBL | Antimalarial activity against asexual blood stage of Plasmodium falciparum 3D7 infected in human serum assessed as [3H]hypoxanthine incorporation incubated for 48 hrs prior to 3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting analysis | F | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2014) 82: 204-213 [PMID:24904967] |
| Plasmodium falciparum (isolate FcB1 / Columbia) in Plasmodium falciparum FcB1/Columbia (target type: ORGANISM) [ChEMBL: CHEMBL612608] | ||||||||
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCB1 assessed as parasite growth inhibition after 48 hrs by standard growth inhibition assay | F | 6.09 | pIC50 | 820 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1727-1734 [PMID:19223622] |
| Plasmodium falciparum NF54 (target type: ORGANISM) [ChEMBL: CHEMBL2367131] | ||||||||
| ChEMBL | Antiprotozoan activity against Plasmodium falciparum NF54 IEF forms | F | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 459-461 [PMID:25563890] |
| Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013] | ||||||||
| ChEMBL | Antimalarial activity against Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 6.77 | pIC50 | 170 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 6.8 | pIC50 | 159 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| ChEMBL | Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum | F | 6.83 | pIC50 | 147 | nM | IC50 | Antimicrob Agents Chemother (2011) 55: 961-966 [PMID:21135175] |
| proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074] | ||||||||
| ChEMBL | Inhibition of chymotrypsin-like activity of 20S proteasome in imatinib-resistant human SUP-B15 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2018) 61: 10299-10309 [PMID:30365892] |
| ChEMBL | Inhibition of chymotrypsin-like activity of 20S proteasome in human SEM cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2018) 61: 10299-10309 [PMID:30365892] |
| ChEMBL | Inhibition of chymotrypsin-like activity of 20S proteasome in human HL60 cells using Suc-LLVY aminoluciferin as substrate after 2 hrs by proteasome-Glo assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2018) 61: 10299-10309 [PMID:30365892] |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Inhibition of wild-type c-Abl by liquid scintillation counting | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2009) 52: 2265-2279 [PMID:19301902] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2015) 95: 104-115 [PMID:25800646] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Inhibition of human recombinant FLT3 after 1 hr by LanthaScreen assay platform | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2015) 95: 104-115 [PMID:25800646] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition VEGFR2 (unknown origin) for 30 mins by ELISA | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5137-5141 [PMID:26475519] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) preincubated for 5 mins followed by addition of ATP/gastrin precursor(Tyr87) biotinylated peptide cocktail incubated for 30 mins by ELISA | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2016) 109: 1-12 [PMID:26741358] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
