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, Ezobresib) |
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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] |
| ChEMBL | Inhibition of N-terminal His6-tagged recombinant human BRD4 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) incubated for 60 mins by TR-FRET assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1165-1171 [PMID:35859878] |
| 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 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]
