BTP2 [Ligand Id: 2438] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL262766
  • Orai1/Calcium release-activated calcium channel protein 1 in Human [ChEMBL: CHEMBL2384891] [GtoPdb: 2964] [UniProtKB: Q96D31]
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  • TRPC3 in Human [GtoPdb: 488] [UniProtKB: Q13507]
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  • TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Orai1/Calcium release-activated calcium channel protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2384891] [GtoPdb: 2964] [UniProtKB: Q96D31]
ChEMBL Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-based FLIPR assay B 5.55 pIC50 2800 nM IC50 Bioorg Med Chem (2017) 25: 440-449 [PMID:27856238]
TRPC3 in Human [GtoPdb: 488] [UniProtKB: Q13507]
GtoPdb - - 6.5 pIC50 300 nM IC50 J. Biol. Chem. (2005) 280: 10997-1006 [PMID:15647288]
TRPM4 in Human [GtoPdb: 496] [UniProtKB: Q8TD43]
GtoPdb - - 8.1 pEC50 8 nM EC50 Mol. Pharmacol. (2006) 69: 1413-20 [PMID:16407466]

ChEMBL data shown on this page come from version 27:

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]