Assay Detail
Binding
CHEMBL3361606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced channel activation by FLIPR assay
34
Total Activities
34
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
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.63 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3317476 | — | — | 1 | 9.70 |
| CHEMBL2177428 | — | — | 1 | 9.52 |
| CHEMBL3317484 | — | — | 1 | 9.52 |
| CHEMBL3319108 | — | — | 1 | 9.40 |
| CHEMBL3317477 | — | — | 1 | 9.40 |
| CHEMBL3319112 | — | — | 1 | 9.30 |
| CHEMBL3319115 | — | — | 1 | 9.30 |
| CHEMBL3317497 | — | — | 1 | 9.22 |
| CHEMBL3319111 | — | — | 1 | 9.15 |
| CHEMBL3317496 | — | — | 1 | 9.10 |
| CHEMBL3317478 | — | — | 1 | 9.05 |
| CHEMBL3319113 | — | — | 1 | 9.00 |
| CHEMBL3317492 | — | — | 1 | 9.00 |
| CHEMBL3319109 | — | — | 1 | 8.89 |
| CHEMBL3317494 | — | — | 1 | 8.85 |
| CHEMBL3317487 | — | — | 1 | 8.85 |
| CHEMBL3317498 | — | — | 1 | 8.74 |
| CHEMBL3317485 | — | — | 1 | 8.70 |
| CHEMBL3317495 | — | — | 1 | 8.66 |
| CHEMBL3319114 | — | — | 1 | 8.49 |
| CHEMBL3317483 | — | — | 1 | 8.47 |
| CHEMBL3317479 | — | — | 1 | 8.38 |
| CHEMBL3317482 | — | — | 1 | 8.30 |
| CHEMBL3317486 | — | — | 1 | 8.24 |
| CHEMBL3319107 | — | — | 1 | 8.19 |
| CHEMBL3317491 | — | — | 1 | 7.69 |
| CHEMBL3317480 | — | — | 1 | 7.59 |
| CHEMBL3317488 | — | — | 1 | 7.44 |
| CHEMBL3317481 | — | — | 1 | 7.24 |
| CHEMBL3319110 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3317476 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177428 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3317484 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3319108 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3317477 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3319112 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3319115 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3317497 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3319111 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3317496 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3317478 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3319113 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3317492 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3319109 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3317487 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3317494 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3317498 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3317485 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3317495 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3319114 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3317483 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL3317479 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3317482 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3317486 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL3319107 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL3317491 | — | Ki | = | 20.3 | nM | 7.69 |
| CHEMBL3317480 | — | Ki | = | 25.6 | nM | 7.59 |
| CHEMBL3317488 | — | Ki | = | 36.1 | nM | 7.44 |
| CHEMBL3317481 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3319110 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL3317493 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL3319116 | — | Ki | - | — | - | |
| CHEMBL3317489 | — | Ki | - | — | - | |
| CHEMBL3317490 | — | Ki | - | — | - |