Assay Detail
Functional
CHEMBL2188272
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of heat-induced activity after 5 mins by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.93 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177429 | — | — | 1 | 9.10 |
| CHEMBL2042399 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177429 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2042399 | — | IC50 | = | 174.0 | nM | 6.76 |