ACAA [Ligand Id: 2443] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL173443
  • TRPM2/Transient receptor potential cation channel subfamily M member 2 in Human [ChEMBL: CHEMBL1250402] [GtoPdb: 494] [UniProtKB: O94759]
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPM2/Transient receptor potential cation channel subfamily M member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250402] [GtoPdb: 494] [UniProtKB: O94759]
ChEMBL Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced intracellular calcium flux at 0 mV holding potential by whole cell patch clamp electrophysiology method B 5.35 pIC50 4500 nM IC50 J Nat Prod (2017) 80: 2741-2750 [PMID:29019677]
ChEMBL Inhibition of human TRPM2 expressed in HEK293 cells assessed as inhibition of H2O2-induced intracellular calcium level by patch clamp technique B 5.77 pIC50 1700 nM IC50 J. Med. Chem. (2013) 56: 10079-10102 [PMID:24304219]
ChEMBL Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in H2O2-induced intracellular calcium flux after 30 mins by Fluo4-AM dye based fluorescence assay B 5.77 pIC50 1700 nM IC50 Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
ChEMBL Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced channel currents by whole cell patch clamp electrophysiology method B 5.77 pIC50 1700 nM IC50 Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
GtoPdb - - 5.8 pIC50 1700 nM IC50 Br. J. Pharmacol. (2006) 148: 264-73 [PMID:16604090]
ChEMBL Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced channel currents treated extracellularly after 60 secs by whole cell patch clamp electrophysiology method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL Inhibition of human TRPM8 expressed in HEK293 cells assessed as reduction in H2O2-induced intracellular calcium flux after 30 mins by Fluo4-AM dye based fluorescence assay B 5.41 pIC50 3900 nM IC50 Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]

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]