GSK417651A [Ligand Id: 10279] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1506485
  • 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 5.9 pIC50 1260 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4979-4984 [PMID:23886683]
GtoPdb Inhibition of recombinant hTRPC3-mediated, carbachol-stimulated Ca2+/Na+ influx in HEK293-MSRII cells assessed by FLIPR assay. - 7.1 pIC50 80 nM IC50 Bioorg Med Chem Lett (2013) 23: 4979-84 [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 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4979-4984 [PMID:23886683]
GtoPdb Inhibition of recombinant hTRPC6-mediated, carbachol-stimulated Ca2+/Na+ influx in HEK293-MSRII cells assessed by FLIPR assay. - 6.36 pIC50 440 nM IC50 Bioorg Med Chem Lett (2013) 23: 4979-84 [PMID:23886683]

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]