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 | Agonist activity at human recombinant TRPM8 | B | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
