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ChEMBL ligand: CHEMBL29411 (NSC-49142, Gppe mthwsh tab, NSC-47821, Thymol, NSC-11215, Listerine, Sotol, Valda, Tellodont, FEMA NO. 3066, Eftab, Tellora) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Heat sensitive channel TRPV3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879847] [UniProtKB: Q4QYD9] | ||||||||
ChEMBL | Activation of rat TRPV3 overexpressed in HEK293 cells assessed as increase in 2-aminoethoxydiphenyl borate-induced intracellular calcium concentration by Fluo-4AM dye-based spectrofluorometry | B | 4.54 | pEC50 | 29000 | nM | EC50 | J Nat Prod (2016) 79: 1762-1768 [PMID:27352042] |
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
ChEMBL | Activation of TRPA1 channel | B | 4.2 | pEC50 | 62500 | nM | EC50 | J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay | B | 4.22 | pEC50 | 60255.96 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay | B | 4.22 | pEC50 | 60000 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by calcium-3 dye based FLIPR analysis | B | 4.7 | pEC50 | 20000 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
GtoPdb | FLIPR calcium influx assay | - | 4.7 | pEC50 | 20000 | nM | EC50 | Br J Pharmacol (2008) 153: 1739-49 [PMID:18334983] |
ChEMBL | Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx | F | 5.22 | pEC50 | 6000 | nM | EC50 | J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Activation of human TRPA1 assessed as stimulation of intracellular Ca2+ levels | B | 5.22 | pEC50 | 6000 | nM | EC50 | Bioorg. Med. Chem. Lett. (2012) 22: 3535-3539 [PMID:22503249] |
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455] | ||||||||
ChEMBL | Activation of rat TRPM8 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels | B | 4.28 | pEC50 | 52200 | nM | EC50 | Bioorg. Med. Chem. Lett. (2012) 22: 3535-3539 [PMID:22503249] |
TRPV3 in Mouse [GtoPdb: 509] [UniProtKB: Q8K424] | ||||||||
GtoPdb | Patch clamp electrophysiology | - | 3.3 | pEC50 | - | - | - | Nat Neurosci (2006) 9: 628-35 [PMID:16617338] |
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]