compound 3 [PMID: 25408830] [Ligand Id: 7811] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1522313
  • bromodomain and PHD finger containing 3/Bromodomain and PHD finger-containing protein 3 in Human [ChEMBL: CHEMBL3108644] [GtoPdb: 2731] [UniProtKB: Q9ULD4]
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  • bromodomain containing 1/Bromodomain-containing protein 1 in Human [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696]
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  • 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 and PHD finger containing 3/Bromodomain and PHD finger-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108644] [GtoPdb: 2731] [UniProtKB: Q9ULD4]
ChEMBL Binding affinity to 6H-Flag-tagged Tev-BRPF3 (579-706 aa) (unknown origin) by TR-FRET competitive assay B 4 pIC50 >100000 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
bromodomain containing 1/Bromodomain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176774] [GtoPdb: 2724] [UniProtKB: O95696]
ChEMBL Binding affinity to 6H-Flag-tagged Tev-BRPF2 (551-673 aa) (unknown origin) by TR-FRET competitive assay B 5.1 pIC50 7943.28 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
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 4.3 pIC50 >50118.72 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
ChEMBL Binding affinity to 6-His-tagged-BRD4 (1 to 477 aa) Y97A mutant (unknown origin) by TR-FRET competitive assay B 5.5 pIC50 3162.28 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
GtoPdb - - 7.1 pIC50 79.4 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 - - 4.3 pIC50 >50118 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
ChEMBL Binding affinity to NanoLuc-tagged BRPF1 isoform 1 bromodomain (625-735 aa) (unknown origin) expressed in HEK293 cells co-transfected with histone H3.3-HaloTag after 18 hrs by NanoBRET assay B 6 pIC50 1000 nM IC50 ACS Med Chem Lett (2014) 5: 1190-1195 [PMID:25408830]
ChEMBL Binding affinity to NanoLuc-tagged BRPF1 isoform 1 bromodomain (625-735 aa) (unknown origin) expressed in HEK293 cells co-transfected with histone H3.3-HaloTag after 18 hrs by NanoBRET assay B 6.01 pIC50 980 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 7.1 pIC50 79.43 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]