icilin [Ligand Id: 2429] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL258405 (Icilin, Icillin) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
