compound 4d [PMID: 21851057] [Ligand Id: 7516] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1828986
  • bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
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  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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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 Displacement of H4Ac4 peptide from first bromodomain of human BRD2 by peptide displacement assay B 5.8 pIC50 1600 nM IC50 J Med Chem (2011) 54: 6761-6770 [PMID:21851057]
GtoPdb Inhibition of binding to recombinant BRD2-BD1. - 5.8 pIC50 1600 nM IC50 J Med Chem (2011) 54: 6761-70 [PMID:21851057]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Displacement of H4Ac4 peptide from first bromodomain of human BRD4 by peptide displacement assay B 5.32 pIC50 4800 nM IC50 J Med Chem (2011) 54: 6761-6770 [PMID:21851057]
ChEMBL Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay B 5.32 pIC50 4800 nM IC50 J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
ChEMBL Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assay B 5.32 pIC50 4786.3 nM IC50 J Med Chem (2013) 56: 3217-3227 [PMID:23517011]
GtoPdb Inhibition of binding to recombinant BRD4-BD1. - 5.32 pIC50 4800 nM IC50 J Med Chem (2011) 54: 6761-70 [PMID:21851057]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL Displacement of H3K56Ac from human CREBBP by peptide displacement assay B 4.55 pIC50 28100 nM IC50 J Med Chem (2011) 54: 6761-6770 [PMID:21851057]

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]