compound 2 [PMID: 25408830] [Ligand Id: 7810] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1444120
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain and PHD finger containing 1/Peregrin in Human [ChEMBL: CHEMBL3132741] [GtoPdb: 2730] [UniProtKB: P55201]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Binding affinity to 6His-tagged-BRD4 BD1 Y390A mutant (1 to 477 aa) (unknown origin) by TR-FRET competitive assay B 5.6 pIC50 2511.89 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
ChEMBL Inhibition of recombinant human N-terminal His6-tagged BRD4 by TR-FRET assay B 5.6 pIC50 2500 nM IC50 Bioorg Med Chem (2018) 26: 3399-3405 [PMID:29764756]
GtoPdb - - 6.7 pIC50 200 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
bromodomain and PHD finger containing 1/Peregrin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3132741] [GtoPdb: 2730] [UniProtKB: P55201]
GtoPdb - - 5.6 pIC50 2511 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
ChEMBL Binding affinity to 6H-Flag-tagged Tev-BRPF1 (622-738 aa) (unknown origin) by TR-FRET competitive assay B 6.7 pIC50 199.53 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]

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]