Assay Detail
Binding
CHEMBL4236563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced intracellular calcium levels preincubated for 2.5 mins followed by icilin addition by CCD-camera-based FLASH luminometric analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily M member 8 (CHEMBL5011) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.77 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4237618 | — | — | 1 | 8.15 |
| CHEMBL4243837 | — | — | 1 | 7.92 |
| CHEMBL4251427 | — | — | 1 | 7.92 |
| CHEMBL4251467 | — | — | 1 | 7.89 |
| CHEMBL4241349 | — | — | 1 | 7.70 |
| CHEMBL4248077 | — | — | 1 | 7.68 |
| CHEMBL4247840 | — | — | 1 | 7.68 |
| CHEMBL4250626 | — | — | 1 | 7.52 |
| CHEMBL4245257 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4237618 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4243837 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4251427 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4251467 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4241349 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4248077 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4247840 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4250626 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4245257 | — | IC50 | = | 34.0 | nM | 7.47 |