Assay Detail
Binding
CHEMBL3412242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced activity by FLIPR assay
28
Total Activities
28
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
Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.56 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407753 | — | — | 1 | 9.52 |
| CHEMBL3407762 | — | — | 1 | 9.52 |
| CHEMBL2177428 | — | — | 1 | 9.52 |
| CHEMBL3407760 | — | — | 1 | 9.30 |
| CHEMBL3407765 | — | — | 1 | 9.30 |
| CHEMBL3407758 | — | — | 1 | 9.22 |
| CHEMBL3407764 | — | — | 1 | 9.22 |
| CHEMBL3407763 | — | — | 1 | 9.10 |
| CHEMBL3407761 | — | — | 1 | 9.10 |
| CHEMBL3407950 | — | — | 1 | 9.05 |
| CHEMBL3407949 | — | — | 1 | 9.05 |
| CHEMBL3407754 | — | — | 1 | 9.05 |
| CHEMBL3407759 | — | — | 1 | 9.00 |
| CHEMBL3407752 | — | — | 1 | 9.00 |
| CHEMBL3407757 | — | — | 1 | 8.96 |
| CHEMBL3407756 | — | — | 1 | 8.89 |
| CHEMBL3407953 | — | — | 1 | 8.52 |
| CHEMBL3407952 | — | — | 1 | 8.38 |
| CHEMBL3407955 | — | — | 1 | 8.04 |
| CHEMBL3407951 | — | — | 1 | 7.84 |
| CHEMBL3407954 | — | — | 1 | 7.76 |
| CHEMBL3407959 | — | — | 1 | 7.54 |
| CHEMBL3407960 | — | — | 1 | 7.49 |
| CHEMBL3407957 | — | — | 1 | 7.36 |
| CHEMBL3407755 | — | — | 1 | 7.23 |
| CHEMBL3407751 | — | — | 1 | 7.14 |
| CHEMBL3407956 | — | — | 1 | 7.00 |
| CHEMBL3407958 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407753 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3407762 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2177428 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3407760 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3407765 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3407758 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3407764 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3407763 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3407761 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3407950 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3407949 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3407754 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3407759 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3407752 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3407757 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3407756 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3407953 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3407952 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3407955 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL3407951 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL3407954 | — | Ki | = | 17.5 | nM | 7.76 |
| CHEMBL3407959 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL3407960 | — | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL3407957 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3407755 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL3407751 | — | Ki | = | 72.1 | nM | 7.14 |
| CHEMBL3407956 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3407958 | — | Ki | - | — | - |