apabetalone [Ligand Id: 7034] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2393130
  • bromodomain containing 2 in Human [GtoPdb: 1944] [UniProtKB: P25440]
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  • bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain containing 3 in Human [GtoPdb: 2725] [UniProtKB: Q15059]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 2 in Human [GtoPdb: 1944] [UniProtKB: P25440]
GtoPdb Measured using a TR-FRET assay to evaluate binding to BD2 of BRD2. - 7.05 pIC50 90 nM IC50 PLoS ONE (2013) 8: e83190 [PMID:24391744]
bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
GtoPdb Measured using a TR-FRET assay to evaluate binding to BD2 of BRD4. - 7.4 pIC50 40 nM IC50 PLoS ONE (2013) 8: e83190 [PMID:24391744]
bromodomain containing 3 in Human [GtoPdb: 2725] [UniProtKB: Q15059]
GtoPdb AlphaScreen data for bromodomain 1 of BRD3. - 4.06 pIC50 87000 nM IC50 Proc Natl Acad Sci USA (2013) 110: 19754-9 [PMID:24248379]
GtoPdb AlphaScreen data assessing the bromodomain 2 domain of BRD3. - 5.31 pIC50 4900 nM IC50 Proc Natl Acad Sci USA (2013) 110: 19754-9 [PMID:24248379]
GtoPdb Measured using a TR-FRET assay to evaluate binding to BD2 of BRD3. - 6.55 pIC50 280 nM IC50 PLoS ONE (2013) 8: e83190 [PMID:24391744]

ChEMBL data shown on this page come from version 36:

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]