icilin [Ligand Id: 2429] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL258405 (Icilin, Icillin)
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
  • This target only has 0 pki data point
  • 0
1 CHEMBL258405_lig_chart_1 Transient receptor potential cation channel subfamily A member 1 Human
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
  • TRPM8 in Mouse [GtoPdb: 500] [UniProtKB: Q8R4D5]
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455]
  • This target only has 0 pki data point
  • 0
2 CHEMBL258405_lig_chart_2 Transient receptor potential cation channel subfamily M member 8 HumanMouseRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx F 4 pEC50 100000 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
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 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay B 6.52 pEC50 300 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6118-6122 [PMID:24080460]
ChEMBL Activation of TRPM8 channel B 7.22 pEC50 60 nM EC50 J. Med. Chem. (2010) 53: 5085-5107 [PMID:20356305]
TRPM8 in Mouse [GtoPdb: 500] [UniProtKB: Q8R4D5]
GtoPdb - - 6.9 pEC50 125 nM EC50 J Neurosci (2004) 24: 5364-9 [PMID:15190109];
Br J Pharmacol (2004) 141: 737-45 [PMID:14757700]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5011] [GtoPdb: 500] [UniProtKB: Q8R455]
ChEMBL Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins before icilin stimulation by Fluo-4-AM dye based spectrofluorimetry B 7.24 pIC50 58 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2285-2290 [PMID:25935641]
GtoPdb Whole-cell voltage-clamp recordings or Ca2+-microfluorimetry in heterologous cells (HEK, CHO, and Xenopus oocytes) expressing TRPM8. - 6.4 pEC50 - - - Nature (2002) 416: 52-8 [PMID:11882888];
Cell (2002) 108: 705-15 [PMID:11893340];
PLoS ONE (2009) 4: e5741 [PMID:19492038]
ChEMBL Agonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as increase in intracellular calcium concentration by fluorimetric test F 6.72 pEC50 190 nM EC50 Bioorg. Med. Chem. (2009) 17: 1636-1639 [PMID:19162486]
ChEMBL Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry B 6.96 pEC50 110 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2285-2290 [PMID:25935641]

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]