ricolinostat [Ligand Id: 7010] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2364628 (ACY-1215, ACY-63, Ricolinostat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of human recombinant HDAC1 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 6.73 | pIC50 | 187.9 | nM | IC50 | Medchemcomm (2019) 10: 1109-1115 [PMID:31391882] |
| 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 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| 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 | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434] |
| ChEMBL | Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate addition measured after 60 sec by microplate reader assay | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 7.24 | pIC50 | 58 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) | B | 7.24 | pIC50 | 58 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | B | 7.24 | pIC50 | 58 | nM | IC50 | Eur J Med Chem (2017) 127: 115-127 [PMID:28038324] |
| ChEMBL | Inhibition of HADC1 (unknown origin) | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC1 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| GtoPdb | - | - | 7.24 | pIC50 | 58 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| ChEMBL | Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of human HDAC1 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| 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 | 5.8 | pIC50 | 1584.89 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| ChEMBL | Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 6.71 | pIC50 | 194 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay | B | 6.9 | pIC50 | 125.89 | nM | IC50 | J Med Chem (2019) 62: 4426-4443 [PMID:30964290] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| 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 human HDAC11 using fluorogenic HDAC substrate incubated for 30 mins by fluorimetry | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of recombinant full length human HDAC11 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| ChEMBL | Inhibition of recombinant human HDAC11 using fluorogenic HDAC substrate class 2a incubated for 30 mins by fluorimetry | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 6.42 | pIC50 | 379 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| ChEMBL | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay | B | 6.42 | pIC50 | 379 | nM | IC50 | ACS Med Chem Lett (2020) 11: 56-64 [PMID:31938464] |
| ChEMBL | Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 7.02 | pIC50 | 95 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| 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 | 7.18 | pIC50 | 66 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of human HDAC2 expressed in Sf9 insect cells using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 7.32 | pIC50 | 48 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of human HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC2 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | B | 7.32 | pIC50 | 48 | nM | IC50 | Eur J Med Chem (2017) 127: 115-127 [PMID:28038324] |
| ChEMBL | Inhibition of HADC2 (unknown origin) | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| GtoPdb | - | - | 7.32 | pIC50 | 48 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 6.87 | pIC50 | 135 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| GtoPdb | - | - | 7.29 | pIC50 | 51 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate and trypsin addition by microplate reader based assay | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2021) 64: 3794-3812 [PMID:33769811] |
| ChEMBL | Inhibition of HADC3 (unknown origin) | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC3 (unknown origin) | B | 7.29 | pIC50 | 51 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of recombinant HDAC3 (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 assay | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2021) 64: 3794-3812 [PMID:33769811] |
| ChEMBL | Inhibition of recombinant full length human HDAC3 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 7.84 | pIC50 | 14.3 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| 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] | ||||||||
| GtoPdb | - | - | 7.29 | pIC50 | 51 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| 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 FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 7.29 | pIC50 | 51 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| 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 | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| 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 HDAC4 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 5.15 | pIC50 | 7000 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 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 recombinant full length human HDAC4 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| 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 HDAC5 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 5.3 | pIC50 | 5000 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| Histone deacetylase 6 in Danio rerio (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739666] [UniProtKB: F8W336] | ||||||||
| ChEMBL | Inhibition of N-terminal 6 His-SUMO tagged Zebrafish HDAC6 CD2 domain expressed in Escherichia coli BL21(DE3) RILP pretreated for 10 mins before FITC-M344 addition and measured after 10 mins by fluorescence polarization competition assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of full length human HDAC6 using FAM-labeled acetylated peptide as substrate by electrophoretic mobility shift assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2021) 64: 2691-2704 [PMID:33576627] |
| ChEMBL | Enzyme Assays: Compounds for testing were diluted in DMSO to 50 fold the final concentration and a ten point three fold dilution series was made. The compounds were diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, 20 uM TCEP) to 6 fold their final concentration. The HDAC enzymes (purchased from BPS Biosciences) were diluted to 1.5 fold their final concentration in assay buffer. The tripeptide substrate and trypsin at 0.05 uM final concentration were diluted in assay buffer at 6 fold their final concentration. The final enzyme concentrations used in these assays were 3.3 ng/ml (HDAC1), 0.2 ng/ml (HDAC2), 0.08 ng/ml (HDAC3) and 2 ng/ml (HDAC6). The final substrate concentrations used were 16 uM (HDAC1), 10 uM (HDAC2), 17 uM (HDAC3) and 14 uM (HDAC6). | B | 7.08 | pIC50 | 84 | nM | IC50 | US-8609678-B2. Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof (2013) |
| ChEMBL | Inhibition of human HDAC6 (unknown origin) using RHKKAc as substrate by fluorescence method | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127763-127763 [PMID:33359604] |
| ChEMBL | Inhibition of human recombinant HDAC6 using ZMAL (Z-Lys(Ac)-AMC) fluorogenic substrate incubated for 90 mins by fluorescence based assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2020) 63: 10339-10351 [PMID:32803970] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 7.75 | pIC50 | 17.9 | nM | IC50 | Medchemcomm (2019) 10: 1109-1115 [PMID:31391882] |
| ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2019) 62: 10711-10739 [PMID:31710483] |
| ChEMBL | Enzyme Assays: Compounds for testing were diluted in DMSO to 50 fold the final concentration and a ten point three fold dilution series was made. The compounds were diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, 20 uM TCEP) to 6 fold their final concentration. The HDAC enzymes (purchased from BPS Biosciences) were diluted to 1.5 fold their final concentration in assay buffer. The tripeptide substrate and trypsin at 0.05 uM final concentration were diluted in assay buffer at 6 fold their final concentration. The final enzyme concentrations used in these assays were 3.3 ng/ml (HDAC1), 0.2 ng/ml (HDAC2), 0.08 ng/ml (HDAC3) and 2 ng/ml (HDAC6). The final substrate concentrations used were 16 uM (HDAC1), 10 uM (HDAC2), 17 uM (HDAC3) and 14 uM (HDAC6). | B | 8 | pIC50 | 10 | nM | IC50 | US-8609678-B2. Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof (2013) |
| 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 | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of human HDAC6 preincubated for 15 mins followed by substrate addition by fluorescence-based assay | B | 8.17 | pIC50 | 6.8 | nM | IC50 | Eur J Med Chem (2021) 218: 113383-113383 [PMID:33799069] |
| 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 | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using RHKK(Ac) (379 to 382) p53 peptide as substrate by fluorescence assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2014) 57: 4009-4022 [PMID:24766560] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected insect cells using RHK-K(Ac)-AMC as substrate after 90 mins by fluorescence assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2018) 61: 905-917 [PMID:29304284] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
| ChEMBL | Inhibition of HADC6 (unknown origin) | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of human HDAC6 using (Z-(Ac)Lys-AMC) as substrate after 90 mins by fluorescence analysis | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2019) 162: 321-333 [PMID:30448419] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using fluorophore tripeptide as substrate after 30 mins | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate addition measured after 60 sec by microplate reader assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2019) 62: 8557-8577 [PMID:31414801] |
| ChEMBL | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2017) 127: 115-127 [PMID:28038324] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| 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 assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2021) 64: 3794-3812 [PMID:33769811] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) using FTS as substrate preincubated for 10 mins followed by substrate and trypsin addition by microplate reader based assay | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2021) 64: 3794-3812 [PMID:33769811] |
| GtoPdb | - | - | 8.33 | pIC50 | 4.7 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| ChEMBL | Inhibition of recombinant full length human HDAC6 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 8.59 | pIC50 | 2.59 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| 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 HDAC7 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| 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 | 5.3 | pIC50 | >5000 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
| ChEMBL | Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | B | 6.6 | pIC50 | 254 | nM | IC50 | J Med Chem (2016) 59: 1455-1470 [PMID:26443078] |
| ChEMBL | Inhibition of recombinant full length human HDAC8 expressed in SF9 baculovirus using FAM- labelled acetylated peptide as substrate measured by Electrophoretic mobility shift assay | B | 6.61 | pIC50 | 245 | nM | IC50 | Eur J Med Chem (2020) 201: 112411-112411 [PMID:32615502] |
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | Blood (2012) 119: 2579-89 [PMID:22262760] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2021) 221: 113526-113526 [PMID:33992929] |
| ChEMBL | Inhibition of HADC8 (unknown origin) | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2020) 63: 23-39 [PMID:31415174] |
| ChEMBL | Inhibition of HDAC8 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of HDAC9 (unknown origin) using tripeptide MAZ-1675 as substrate after 30 mins | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 6297-6313 [PMID:23627282] |
| 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 HDAC9 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) using MAZ-1675 as substrate preincubated for 10 mins followed by substrate addition and shaken for 60 secs and measured over 30 mins | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| 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 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 1817-1828 [PMID:28218840] |
| sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged SIRT1 (1 to 747 end residues) expressed in Escherichia coli using Ac-RHK-K(Ac)-AMC as substrate after 30 mins in presence of NAD+ by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 905-917 [PMID:29304284] |
| ChEMBL | Inhibition of human sirtuin 1 using fluorogenic HDAC substrate incubated for 20 mins by fluorimetry | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
| ChEMBL | Inhibition of human sirtuin 2 using fluoro-lysine sirtuin 2 deacetylase as substrate incubated for 60 mins by fluorimetry | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 1406-1418 [PMID:29133060] |
| 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] |
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]
