Assay Detail
Binding
CHEMBL3373787
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 increase in intracellular Ca2+ level by FLIPR assay
37
Total Activities
37
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-Alkyl/alkenyl 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 | 37 | 9.15 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3314409 | — | — | 1 | 10.00 |
| CHEMBL3314407 | — | — | 1 | 10.00 |
| CHEMBL3314406 | — | — | 1 | 10.00 |
| CHEMBL3314411 | — | — | 1 | 10.00 |
| CHEMBL3314393 | — | — | 1 | 9.70 |
| CHEMBL3314410 | — | — | 1 | 9.70 |
| CHEMBL3314408 | — | — | 1 | 9.70 |
| CHEMBL3314405 | — | — | 1 | 9.70 |
| CHEMBL3314404 | — | — | 1 | 9.70 |
| CHEMBL2177429 | — | — | 1 | 9.70 |
| CHEMBL3314377 | — | — | 1 | 9.70 |
| CHEMBL3314392 | — | — | 1 | 9.52 |
| CHEMBL3314390 | — | — | 1 | 9.52 |
| CHEMBL3314394 | — | — | 1 | 9.52 |
| CHEMBL3314396 | — | — | 1 | 9.52 |
| CHEMBL3314403 | — | — | 1 | 9.52 |
| CHEMBL3314398 | — | — | 1 | 9.52 |
| CHEMBL3314397 | — | — | 1 | 9.40 |
| CHEMBL3314391 | — | — | 1 | 9.40 |
| CHEMBL3314383 | — | — | 1 | 9.22 |
| CHEMBL3314389 | — | — | 1 | 9.22 |
| CHEMBL3314387 | — | — | 1 | 9.15 |
| CHEMBL3314388 | — | — | 1 | 9.15 |
| CHEMBL3314402 | — | — | 1 | 9.15 |
| CHEMBL3314401 | — | — | 1 | 9.10 |
| CHEMBL3314385 | — | — | 1 | 9.05 |
| CHEMBL3314382 | — | — | 1 | 9.05 |
| CHEMBL3313936 | — | — | 1 | 9.00 |
| CHEMBL3314395 | — | — | 1 | 8.89 |
| CHEMBL3314400 | — | — | 1 | 8.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3314409 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3314411 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3314406 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3314407 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3314393 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314410 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314408 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314405 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314404 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2177429 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314377 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3314398 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314403 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314396 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314394 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314392 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314390 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3314391 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3314397 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3314383 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3314389 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3314387 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3314388 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3314402 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3314401 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3314385 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3314382 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3313936 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3314395 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3314400 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3314399 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3314381 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3314386 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3314384 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL3314380 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL3314378 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL3314379 | — | Ki | = | 387.0 | nM | 6.41 |