BMS-986158 [Ligand Id: 11757] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297458 (Bet inhibitor bms-986158, Bms-986158, BMS-986158) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440] | ||||||||
| ChEMBL | Inhibition of human BRD2 measured by TR-FRET assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2021) 64: 14247-14265 [PMID:34543572] |
| bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] | ||||||||
| ChEMBL | Inhibition of human BRD3 measured by TR-FRET assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2021) 64: 14247-14265 [PMID:34543572] |
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of human BRD4 (1 to 477 residues) measured after 60 mins by TR-FRET assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2021) 64: 14247-14265 [PMID:34543572] |
| GtoPdb | Time-resolved FRET binding assay using hBRD4 BD-1 bromodomain. | - | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2009) 52: 6527-30 [PMID:19821562] |
| ChEMBL | Inhibition of BRD4 (unknown origin) | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2021) 51: 128376-128376 [PMID:34560263] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by flux assay | B | 4.1 | pIC50 | >80000 | nM | IC50 | J Med Chem (2021) 64: 14247-14265 [PMID:34543572] |
| ChEMBL | Inhibition of human ERG by patch-clamp assay | B | 4.55 | pIC50 | 28000 | nM | IC50 | J Med Chem (2021) 64: 14247-14265 [PMID:34543572] |
| Myc proto-oncogene protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250348] [UniProtKB: P01106] | ||||||||
| ChEMBL | Inhibition of c-MYC (unknown origin) | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem Lett (2021) 51: 128376-128376 [PMID:34560263] |
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]
