ABBV-744 [Ligand Id: 10730] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4297454 (Abbv-744, ABBV-744)
  • bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
  • 7.14
1 CHEMBL4297454_lig_chart_1 Bromodomain-containing protein 2 Human
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  • bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
  • 6.91
2 CHEMBL4297454_lig_chart_2 Bromodomain-containing protein 3 Human
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  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
  • 7.54
3 CHEMBL4297454_lig_chart_3 Bromodomain-containing protein 4 Human
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  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
  • 7.52
4 CHEMBL4297454_lig_chart_4 Bromodomain testis-specific protein Human
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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 Inhibition of N-terminal His6-tagged human BRD2 BD1 (73 to 194 residues) after 1 hr by TR-FRET assay B 5.93 pKi 1162 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of N-terminal His6-tagged human BRD2 BD2 (348 to 455 residues) after 1 hr by TR-FRET assay B 8.34 pKi 4.6 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assay B 5.5 pKi 3140 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assay B 8.31 pKi 4.9 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Inhibition of human N-terminal His6 tagged BRD4 BD1 (57 to 168) residues expressed in Escherichia coli BL21(DE3) cells after 1 hr by TR-FRET assay B 6.28 pKi 520 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of human N-terminal His6 tagged BRD4 BD2 (352 to 457) residues expressed in Escherichia coli BL21(DE3) cells after 1 hr by TR-FRET assay B 8.8 pKi 1.6 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of NanoLuc-tagged BRD4 BD1 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay B 4.68 pIC50 20700 nM IC50 J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of NanoLuc-tagged BRD4 BD2 (unknown origin) expressed in human HeLa cells after 2 hrs by NanoBRET assay B 7.56 pIC50 27.5 nM IC50 J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assay B 6.04 pKi 917 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]
ChEMBL Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assay B 9 pKi 1 nM Ki J Med Chem (2020) 63: 5585-5623 [PMID:32324999]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]