Assay Detail
Binding
CHEMBL4178992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at elevated temperature activated human TRPV1 expressed in CHO cells assessed as inhibition of intracellular calcium level preincubated for 5 mins followed by receptor activation by increasing temperature to 45 degC by Fluo-4 dye based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.09 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3689046 | — | — | 1 | 8.09 |
| CHEMBL3689037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3689046 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3689037 | — | IC50 | - | — | - |