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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 34:
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]