GSK2332255B [Ligand Id: 12529] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2418809
  • TRPC3/Short transient receptor potential channel 3 in Human [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507]
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  • TRPC6/Short transient receptor potential channel 6 in Human [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPC3/Short transient receptor potential channel 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507]
ChEMBL Inhibition of human recombinant TRPC3 expressed in HEK293-MSRII cells assessed as carbachol-stimulated Ca2+/Na+ influx after 10 mins by FLIPR assay B 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2013) 23: 4979-4984 [PMID:23886683]
TRPC6/Short transient receptor potential channel 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210]
ChEMBL Inhibition of human recombinant TRPC6 expressed in HEK293-MSRII cells assessed as carbachol-stimulated Ca2+/Na+ influx after 10 mins by FLIPR assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2013) 23: 4979-4984 [PMID:23886683]
GtoPdb - - 8.4 pIC50 - - - Proc Natl Acad Sci USA (2014) 111: 1551-6 [PMID:24453217]

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]