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ChEMBL ligand: CHEMBL2153434 (GW841819X) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]