AMTB [Ligand Id: 4132] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1289953 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of icilin-induced 45calcium influx treated 5 mins before icilin challenge measured after 5 mins | F | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of menthol-induced 45calcium influx treated 5 mins before menthol challenge measured after 5 mins | F | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) assessed as reduction in calcium influx | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| ChEMBL | Inhibition of TRPM8 (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| 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 at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol-induced calcium flux preincubated for 60 mins followed by menthol addition by Fluo-4 NW dye based fluorimetric method | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (2020) 63: 9672-9694 [PMID:32787109] |
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]
