MS436 [Ligand Id: 7509] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3086883
  • bromodomain adjacent to zinc finger domain 2B/Bromodomain adjacent to zinc finger domain protein 2B in Human [ChEMBL: CHEMBL1741220] [GtoPdb: 2722] [UniProtKB: Q9UIF8]
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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]
  • bromodomain containing 4/Bromodomain-containing protein 4 in Mouse [ChEMBL: CHEMBL3085619] [GtoPdb: 1945] [UniProtKB: Q9ESU6]
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  • bromodomain containing 7/Bromodomain-containing protein 7 in Human [ChEMBL: CHEMBL3085622] [GtoPdb: 2726] [UniProtKB: Q9NPI1]
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  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
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  • lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831]
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  • bromodomain PHD finger transcription factor/Nucleosome-remodeling factor subunit BPTF in Human [ChEMBL: CHEMBL3085621] [GtoPdb: 2723] [UniProtKB: Q12830]
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  • SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4/Transcription activator BRG1 in Human [ChEMBL: CHEMBL3085620] [GtoPdb: 2740] [UniProtKB: P51532]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]