Assay Detail
Functional
CHEMBL2045508
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 receptor expressed in CHO cells assessed as decrease in pH-induced intracellular 45Ca2+ uptake after 1 hr by fluorometric analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.45 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2042399 | — | — | 1 | 8.08 |
| CHEMBL2042264 | — | — | 1 | 7.90 |
| CHEMBL2042398 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2042399 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL2042264 | — | Ki | = | 12.7 | nM | 7.90 |
| CHEMBL2042398 | — | Ki | = | 440.0 | nM | 6.36 |