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ChEMBL ligand: CHEMBL3086883 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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bromodomain adjacent to zinc finger domain 2B/Bromodomain adjacent to zinc finger domain protein 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741220] [GtoPdb: 2722] [UniProtKB: Q9UIF8] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS239 from recombinant human BAZ2b after 1 hr by fluorescence anisotropy assay | B | 5.48 | pKi | 3290 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS574 from recombinant human BRD3 BrD2 after 1 hr by fluorescence anisotropy assay | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coli | B | 6.85 | pKi | 140 | nM | Ki | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Displacement of fluorescein-labeled MS574 from recombinant human BRD3 BrD1 after 1 hr by fluorescence anisotropy assay | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coli | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS574 from recombinant human BRD4 BrD2 after 1 hr by fluorescence anisotropy assay | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coli | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
ChEMBL | Displacement of fluorescein-labeled MS574 from recombinant human BRD4 BrD1 after 1 hr by fluorescence anisotropy assay | B | 7.07 | pKi | 85.11 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Displacement of fluorescein-labeled MS574 from recombinant human BRD4 BrD1 after 1 hr by fluorescence anisotropy assay | B | 7.07 | pKi | <85 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coli | B | 7.07 | pKi | <85 | nM | Ki | J Med Chem (2018) 61: 9316-9334 [PMID:30253095] |
GtoPdb | Range of inhibition of binding across both Brd1 and Brd2 bromodomains of BRD4. | - | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2013) 56: 9251-64 [PMID:24144283] |
bromodomain containing 4/Bromodomain-containing protein 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085619] [GtoPdb: 1945] [UniProtKB: Q9ESU6] | ||||||||
ChEMBL | Inhibition of BRD4 in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB-mediated IL-6 expression preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by ELISA | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
ChEMBL | Inhibition of BRD4 in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB-mediated nitric oxide production preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by spectrophotometric analysis | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
bromodomain containing 7/Bromodomain-containing protein 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085622] [GtoPdb: 2726] [UniProtKB: Q9NPI1] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay | B | 5.57 | pKi | 2720 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS226 from recombinant human CBP bromodomain after 1 hr by fluorescence anisotropy assay | B | 5.66 | pKi | 2180 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS239 from recombinant human PCAF after 1 hr by fluorescence anisotropy assay | B | 5.26 | pKi | 5520 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
bromodomain PHD finger transcription factor/Nucleosome-remodeling factor subunit BPTF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085621] [GtoPdb: 2723] [UniProtKB: Q12830] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS239 from recombinant human BPTF after 1 hr by fluorescence anisotropy assay | B | 5.22 | pKi | 6060 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4/Transcription activator BRG1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085620] [GtoPdb: 2740] [UniProtKB: P51532] | ||||||||
ChEMBL | Displacement of fluorescein-labeled MS239 from recombinant human SMARCA4 bromodomain after 1 hr by fluorescence anisotropy assay | B | 5.1 | pKi | 7970 | nM | Ki | J Med Chem (2013) 56: 9251-9264 [PMID:24144283] |
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]