Potency data for probe PF-05105679 and control PF-05257137
No in vitro potency data available.
In cell potency
| Target name | Target information | Species | Assay description | PF-05105679 | PF-05257137 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| TRPM8 | HEK-293 cells were stably transfected with a human transient receptor potential melastatin (TRPM8) receptor construct. | Homo sapiens | WS-12 ((2S,5R)-2-isopropyl-N-(4-methoxyphenyl)-5-methylcyclohexanecarboximide) agonist activation | IC50 = 181 nM ± 7.210 nM (n=25) | PMID: 25125580 | |
| TRPM8 | Homo sapiens | Cold activation: The application of cold (10°C) causes a flux of Ca2+ across the cell membrane, which was measured by changes inintracellular fluorescence on a real-time PCR machine. | IC50 = 480 nM ± 42.760 nM (n=13) | PMID: 25125580 | ||
| TRPM8 | Homo sapiens | Voltage activation at room temperature: Whole-cell patch-clamp recordings | IC50 = 103 nM ± 29.400 nM (n=3) | PMID: 25125580 | ||
| TRPM8 | Homo sapiens | Voltage activation at 12 °C: Whole-cell patch-clamp recordings | IC50 = 13.8 nM ± 2.200 nM (n=3) | PMID: 25125580 | ||
| TRPM8 | Homo sapiens | Transients WS-12 activation | IC50 = 29.6 nM ± 14.800 nM (n=3) | PMID: 25125580 | ||
| TRPM8 | Homo sapiens | Assay (coming soon) | IC50 > 10 µM |