MS363 | Ligand Activity Charts | IUPHAR/BPS Guide to PHARMACOLOGY

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MS363
Ligand Activity Charts

MS363 [Ligand Id: 8876] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3086885
bromodomain adjacent to zinc finger domain 2B/Bromodomain adjacent to zinc finger domain protein 2B in Human [ChEMBL: CHEMBL1741220] [GtoPdb: 2722] [UniProtKB: Q9UIF8] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
bromodomain containing 7/Bromodomain-containing protein 7 in Human [ChEMBL: CHEMBL3085622] [GtoPdb: 2726] [UniProtKB: Q9NPI1] There should be some charts here, you may need to enable JavaScript!
CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] There should be some charts here, you may need to enable JavaScript!
lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] There should be some charts here, you may need to enable JavaScript!
bromodomain PHD finger transcription factor/Nucleosome-remodeling factor subunit BPTF in Human [ChEMBL: CHEMBL3085621] [GtoPdb: 2723] [UniProtKB: Q12830] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!

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	3300	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	6.49	pKi	320	nM	Ki	J Med Chem (2013) 56: 9251-9264 [PMID:24144283]
ChEMBL	Displacement of fluorescein-labeled MS574 from recombinant human BRD3 BrD1 after 1 hr by fluorescence anisotropy assay	B	6.62	pKi	240	nM	Ki	J Med Chem (2013) 56: 9251-9264 [PMID:24144283]
GtoPdb	Affinity at bromodomain 1 of BRD3.	-	6.62	pKi	240	nM	Ki	J Med Chem (2013) 56: 9251-64 [PMID:24144283]
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	6.19	pKi	640	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	6.77	pKi	170	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	6.77	pKi	169.82	nM	Ki	J Med Chem (2013) 56: 9251-9264 [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	5.42	pIC50	3800	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	5.47	pIC50	3400	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	5.84	pKi	<1430	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	5.25	pKi	5590	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	5.48	pKi	<3340	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]
GtoPdb	-	-	5.79	pKi	1620	nM	Ki	J Med Chem (2013) 56: 9251-64 [PMID:24144283]
ChEMBL	Displacement of fluorescein-labeled MS239 from recombinant human BPTF after 1 hr by fluorescence anisotropy assay	B	5.79	pKi	1620	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	5.18	pKi	<6560	nM	Ki	J Med Chem (2013) 56: 9251-9264 [PMID:24144283]

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]