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| ChEMBL ligand: CHEMBL470670 (Levomenthol, Levomentol, L-menthol) |
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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 recombinant human TRPA1 expressed in HEK293 cells assessed as increase in intracellular Ca2+ level pre-incubated for 5 mins by Fluo4-AM dye-based fluorescence assay | B | 4.02 | pEC50 | 96000 | nM | EC50 | ACS Med Chem Lett (2017) 8: 715-719 [PMID:28740604] |
| GtoPdb | Calcium imaging, patch clamp | - | 4.5 | pEC50 | 28400 | nM | EC50 |
J Neurosci (2008) 28: 9640-51 [PMID:18815250]; J Neurosci (2007) 27: 9874-84 [PMID:17855602] |
| TRPA1 in Mouse [GtoPdb: 485] [UniProtKB: Q8BLA8] | ||||||||
| GtoPdb | - | - | 4.2 | pIC50 | - | - | - | Mol Cell Neurosci (2006) 32: 335-43 [PMID:16829128] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Agonist activity at TRPM8 (unknown origin) by fluorometric imaging plate reader analysis | B | 4.22 | pEC50 | 60000 | nM | EC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| GtoPdb | - | - | 4.6 | pEC50 | 25100 | nM | EC50 | Nature (2004) 430: 748-54 [PMID:15306801] |
| ChEMBL | Agonist activity at full length recombinant human TRPM8 expressed in HEK293 cells assessed as increase in intracellular Ca2+ level pre-incubated for 5 mins by Fluo4-AM dye-based fluorescence assay | B | 5 | pEC50 | 10100 | nM | EC50 | ACS Med Chem Lett (2017) 8: 715-719 [PMID:28740604] |
| ChEMBL | TRPM8 receptor assay: In the first set of data, the potency and in vitro effects of test compounds were evaluated on cloned hTRPM8 channel (encoded by the human TRPM8 gene, expressed in CHO cells) using a Fluo-8 calcium kit and a Fluorescence Imaging Plate Reader (FLIPRTETRA) instrument. The assays were conducted by ChanTest Corporation (Cleveland, Ohio 44128, USA). Test solutions were in a HEPES-buffered saline, in 384-well plates, and placed into the FLIPR instrument (Molecular Devices Corporation, Union City, Calif., USA). Four 4 to 8 concentrations were tested, with L-menthol as the positive control. The test cells were Chinese Hamster Ovary (CHO) cells stably transfected with human TRPM8 cDNAs. Concentration-response data were analyzed via FLIPR Control software) and fitted to a Hill equation for the EC50. The 95% Confidence Interval was obtained using GraphPad Prism 6 software. | B | 5.42 | pEC50 | 3800 | nM | EC50 | US-11406649-B2. Treatment of upper aerodigestive tract disorders and cough (2022) |
| TRPM8 in Mouse [GtoPdb: 500] [UniProtKB: Q8R4D5] | ||||||||
| GtoPdb | - | - | 5.4 | pEC50 | - | - | - |
J Neurosci (2004) 24: 5364-9 [PMID:15190109]; Br J Pharmacol (2004) 141: 737-45 [PMID:14757700] |
| TRPM8 in Rat [GtoPdb: 500] [UniProtKB: Q8R455] | ||||||||
| GtoPdb | - | - | 4.2 | pEC50 | - | - | - | Nature (2002) 416: 52-8 [PMID:11882888] |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2830] [UniProtKB: P15381] | ||||||||
| ChEMBL | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in rabbit ventricular myocytes | F | 4.13 | pIC50 | 74600 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
| TRPV3 in Mouse [GtoPdb: 509] [UniProtKB: Q8K424] | ||||||||
| GtoPdb | Patch clamp electrophysiology and calcium imaging | - | 1.7 | pEC50 | 19952624 | nM | EC50 | Mol Cell Neurosci (2006) 32: 335-43 [PMID:16829128] |
ChEMBL data shown on this page come from version 36:
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]