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 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]