isoxazole azepine compound 3 [Ligand Id: 7527] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2431090
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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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 Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs B 6.85 pIC50 140 nM IC50 ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
ChEMBL Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISA B 7.59 pIC50 26 nM IC50 ACS Med Chem Lett (2013) 4: 835-840 [PMID:24900758]
GtoPdb Assayed using recombinant BRD4-BD1. - 7.59 pIC50 26 nM IC50 ACS Med Chem Lett (2013) 4: 835-40 [PMID:24900758]

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]