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 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]