TMP269 [Ligand Id: 7491] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3110004 |
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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 HDAC1 using p53 (379 to 382 residues) (RHKKAc) as substrate measured after 2 hrs by cheng-Prusoff analysis | B | 4.64 | pKi | >23000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| 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 | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC10 (unknown origin) | B | 6.68 | pIC50 | 210 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of human HDAC11 using (Boc-Lys(trifluoroacetyl)-AMC) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 4.72 | pKi | >19000 | nM | Ki | 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 human HDAC2 using p53 (379 to 382 residues) (RHKKAc) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 4.72 | pKi | >19000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay | B | 4.37 | pIC50 | >43000 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| 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 HDAC3/NcoR2 using p53 residues 379-382 (RHKKAc) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 4.37 | pKi | >43000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| 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 | 5.75 | pKi | 1770 | nM | Ki | Bioorg Med Chem (2019) 27: 115036-115036 [PMID:31431326] |
| ChEMBL | Inhibition of human HDAC4 using (Boc-Lys(trifluoroacetyl)-AMC) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of N-terminal GST-tagged/C-terminal His-tagged human HDAC4 (627 to 1084 residues) expressed in Sf9 insect cells using Boc-Lys(Tfa)-AMC as fluorogenic substrate preincubated for 60 mins followed by substrate addition and measured after 90 mins by microplate reader analysis | B | 6.12 | pIC50 | 753 | nM | IC50 | J Med Chem (2023) 66: 13821-13837 [PMID:37782298] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using fluorogenic substrate after 1 to 2 hrs by fluorescence assay | B | 6.45 | pIC50 | 353 | nM | IC50 | Eur J Med Chem (2018) 143: 2005-2014 [PMID:29150335] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) using trypsin and Ac-peptide as substrates | B | 6.5 | pIC50 | 317.67 | nM | IC50 | Eur J Med Chem (2022) 230: 114115-114115 [PMID:35033824] |
| ChEMBL | Inhibition of recombinant human HDAC4 using Boc-Lys(trifluoroacetyl)-AMC as substrate by homogeneous fluorescence release assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 161: 277-291 [PMID:30366254] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged and C-terminal His-tagged HDAC4 expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | B | 6.61 | pIC50 | 244 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
| ChEMBL | Inhibition of HDAC4 (unknown origin) | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
| GtoPdb | - | - | 6.8 | pIC50 | 157 | nM | IC50 | Nat Chem Biol (2013) 9: 319-25 [PMID:23524983] |
| ChEMBL | Inhibition of human recombinant N-terminal GST-tagged C-terminal His-tagged HDAC4 (627 to 1084 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.87 | pIC50 | 134.4 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
| ChEMBL | Inhibition of human recombinant HDAC4 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of recombinant human HDAC4 using fluorogenic substrate by fluorescence assay | B | 6.9 | pIC50 | 127 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of human HDAC5 using (Boc-Lys(trifluoroacetyl)-AMC) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of C-terminal His-tagged human HDAC5 (656-1122 residues) expressed in baculovirus expression system using Ac-peptide substrate incubated for 15 mins by fluorescence based assay | B | 6 | pIC50 | 990 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| ChEMBL | Inhibition of recombinant human C-terminal His-fusion tagged HDAC5 (657 to 1123 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | B | 6.48 | pIC50 | 333 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
| ChEMBL | Inhibition of recombinant human HDAC5 using fluorogenic substrate by fluorescence assay | B | 6.58 | pIC50 | 263 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of HDAC5 (unknown origin) | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
| ChEMBL | Inhibition of human recombinant C-terminal His-tagged HDAC5 (657 to 1123 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 6.96 | pIC50 | 108.4 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
| GtoPdb | - | - | 7.01 | pIC50 | 97 | nM | IC50 | Nat Chem Biol (2013) 9: 319-25 [PMID:23524983] |
| ChEMBL | Inhibition of human recombinant HDAC5 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of human HDAC6 using p53 residues 379-382 (RHKKAc) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of human recombinant full length HDAC6 after 60 mins by fluorescence assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of HDAC6 (unknown origin) | B | 6.05 | pIC50 | 890 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of human HDAC7 using (Boc-Lys(trifluoroacetyl)-AMC) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 7.44 | pKi | 36 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of recombinant human HDAC7 using fluorogenic substrate by fluorescence assay | B | 6.95 | pIC50 | 112 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in baculovirus infected insect cells using fluorogenic HDAC class2a as substrate measured after 1 to 2 hrs by fluorescence assay | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
| ChEMBL | Inhibition of HDAC7 (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
| GtoPdb | - | - | 7.37 | pIC50 | 43 | nM | IC50 | Nat Chem Biol (2013) 9: 319-25 [PMID:23524983] |
| ChEMBL | Inhibition of human recombinant N-terminal GST-tagged HDAC7 (518 to 991 residues) expressed in insect cells using Boc-K(TFA)-AMC as substrate incubated for 60 mins by fluorescence assay | B | 7.39 | pIC50 | 40.85 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
| ChEMBL | Inhibition of human recombinant HDAC7 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of human HDAC8 using p53 residues 379-382 (RHKAcKAc) as substrate as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of human recombinant full length HDAC8 using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of human HDAC9 using (Boc-Lys(trifluoroacetyl)-AMC) as substrate measured after 2 hrs by Cheng-Prusoff analysis | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2020) 63: 12460-12484 [PMID:32608981] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) using fluorogenic HDAC class 2a as substrate measured after 1 to 2 hrs by fluorescence assay | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (2020) 63: 4256-4292 [PMID:32212730] |
| ChEMBL | Inhibition of human recombinant HDAC9 using trifluoroacetyl lysine as substrate | B | 7.63 | pIC50 | 23.24 | nM | IC50 | Eur J Med Chem (2016) 116: 126-135 [PMID:27060764] |
| GtoPdb | - | - | 7.64 | pIC50 | 23 | nM | IC50 | Nat Chem Biol (2013) 9: 319-25 [PMID:23524983] |
| ChEMBL | Inhibition of human recombinant HDAC9 catalytic domain using Boc_Lys_TFA as substrate after 60 mins by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2013) 56: 9934-9954 [PMID:24261862] |
| ChEMBL | Inhibition of recombinant human HDAC9 using fluorogenic substrate by fluorescence assay | B | 7.71 | pIC50 | 19.4 | nM | IC50 | Eur J Med Chem (2017) 125: 1268-1278 [PMID:27886544] |
| ChEMBL | Inhibition of HDAC9 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2021) 225: 113790-113790 [PMID:34454126] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
