GW841819X [Ligand Id: 7514] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2153434 (GW841819X)
  • ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18]
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  • bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
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  • bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
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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
ATPase family AAA domain containing 2/ATPase family AAA domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150837] [GtoPdb: 2719] [UniProtKB: Q6PL18]
ChEMBL Binding affinity to ATAD2 by isothermal titration calorimetric analysis B 4.3 pKd >50000 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
ChEMBL Binding affinity to human Brd2 containing bromodomain BD1 expressed in Escherichia coli assessed as dissociation constant at 25 degC by surface plasma resonance B 6.66 pKd 220 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to human Brd2 containing bromodomain BD2 expressed in Escherichia coli assessed as dissociation constant at 25 degC by surface plasma resonance B 7.27 pKd 54 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to N-terminal portion of human Brd2 containing bromodomain BD2 expressed in Escherichia coli at 26 degC by isothermal titration calorimetric analysis B 7.28 pKd 52.5 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to N-terminal portion of human Brd2 containing bromodomain BD12 expressed in Escherichia coli at 26 degC by isothermal titration calorimetric analysis B 7.28 pKd 52 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to N-terminal portion of human Brd2 containing bromodomain BD1 expressed in Escherichia coli at 16 degC by isothermal titration calorimetric analysis B 7.34 pKd 46 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to N-terminal portion of human Brd2 containing bromodomain BD12 expressed in Escherichia coli by isothermal titration calorimetric analysis B 7.72 pKd 19 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to His6-tagged BRD2 (unknown origin) after 60 mins by fluorescence anisotropy binding Assay B 5.9 pIC50 1258.93 nM IC50 J Med Chem (2013) 56: 7501-7515 [PMID:24015967]
GtoPdb Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD2. - 7.52 pIC50 29.9 nM IC50 J Med Chem (2011) 54: 3827-38 [PMID:21568322]
ChEMBL Displacement of tetra-acetylated H4 peptide from human Brd2 bromodomain BD12 after 1 hr by FRET analysis B 7.52 pIC50 29.9 nM IC50 J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
ChEMBL Binding affinity to N-terminal portion of human Brd3 containing bromodomain BD12 expressed in Escherichia coli by isothermal titration calorimetric analysis B 7.72 pKd 19 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to His6-tagged BRD3 (unknown origin) after 60 mins by fluorescence anisotropy binding Assay B 6.2 pIC50 630.96 nM IC50 J Med Chem (2013) 56: 7501-7515 [PMID:24015967]
ChEMBL Displacement of tetra-acetylated H4 peptide from human Brd3 bromodomain BD12 after 1 hr by FRET analysis B 7.55 pIC50 28.4 nM IC50 J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
GtoPdb Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD3. - 7.55 pIC50 28.4 nM IC50 J Med Chem (2011) 54: 3827-38 [PMID:21568322]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Binding affinity to N-terminal portion of human Brd4 containing bromodomain BD12 expressed in Escherichia coli by isothermal titration calorimetric analysis B 7.72 pKd 19 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
ChEMBL Binding affinity to His6-tagged BRD4 (unknown origin) after 60 mins by fluorescence anisotropy binding Assay B 6.3 pIC50 501.19 nM IC50 J Med Chem (2013) 56: 7501-7515 [PMID:24015967]
ChEMBL Inhibition of tetra-acetylated Histone H4 peptide binding to recombinant human His-tagged BRD4 (1 to 477 residues) after 1 hr by FRET assay B 6.3 pIC50 501 nM IC50 J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
ChEMBL Displacement of tetra-acetylated H4 peptide from human Brd4 bromodomain BD12 after 1 hr by FRET analysis B 7.81 pIC50 15.5 nM IC50 J Med Chem (2011) 54: 3827-3838 [PMID:21568322]
GtoPdb Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD4. - 7.81 pIC50 15.5 nM IC50 J Med Chem (2011) 54: 3827-38 [PMID:21568322]
ChEMBL Inhibition of BRD4 in human HepG2 cells assessed as upregulation of ApoA1 by luciferase reporter gene assay B 6.36 pEC50 440 nM EC50 J Med Chem (2017) 60: 4533-4558 [PMID:28195723]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL Binding affinity to CREBBP by isothermal titration calorimetric analysis B 4.3 pKd >50000 nM Kd J Med Chem (2011) 54: 3827-3838 [PMID:21568322]

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]