Assay Detail
Functional
CHEMBL942790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.77 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229430 | AMG-517 | 1.0 | 1 | 9.05 |
| CHEMBL400571 | — | — | 1 | 8.82 |
| CHEMBL251565 | — | — | 1 | 8.74 |
| CHEMBL251348 | — | — | 1 | 8.49 |
| CHEMBL250185 | — | — | 1 | 8.29 |
| CHEMBL251352 | — | — | 1 | 8.23 |
| CHEMBL446455 | — | — | 1 | 8.21 |
| CHEMBL398968 | — | — | 1 | 8.21 |
| CHEMBL249731 | — | — | 1 | 8.21 |
| CHEMBL251559 | — | — | 1 | 8.11 |
| CHEMBL251560 | — | — | 1 | 8.06 |
| CHEMBL249983 | — | — | 1 | 8.03 |
| CHEMBL249984 | — | — | 1 | 7.96 |
| CHEMBL398410 | — | — | 1 | 7.92 |
| CHEMBL251556 | — | — | 1 | 7.92 |
| CHEMBL401192 | — | — | 1 | 7.70 |
| CHEMBL398411 | — | — | 1 | 7.55 |
| CHEMBL249528 | — | — | 1 | 7.46 |
| CHEMBL251604 | — | — | 1 | 7.41 |
| CHEMBL248741 | — | — | 1 | 7.37 |
| CHEMBL398829 | — | — | 1 | 7.29 |
| CHEMBL251349 | — | — | 1 | 7.00 |
| CHEMBL398293 | — | — | 1 | 6.89 |
| CHEMBL251189 | — | — | 1 | 6.62 |
| CHEMBL249529 | — | — | 1 | 6.39 |
| CHEMBL249732 | — | — | 1 | 6.04 |
| CHEMBL249778 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229430 | AMG-517 | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL400571 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL251565 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL251348 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL250185 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL251352 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL446455 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL398968 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL249731 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL251559 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL251560 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL249983 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL249984 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL398410 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL251556 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL401192 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL398411 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL249528 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL251604 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL248741 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL398829 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL251349 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL398293 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL251189 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL249529 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL249732 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL249778 | — | IC50 | > | 4000.0 | nM | - |