Assay Detail
Functional
CHEMBL953046
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay
21
Total Activities
21
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 | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted aryl pyrimidines as potent and soluble TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.26 | 10.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455580 | — | — | 1 | 10.16 |
| CHEMBL445237 | — | — | 1 | 9.44 |
| CHEMBL525804 | — | — | 1 | 9.32 |
| CHEMBL453146 | — | — | 1 | 9.28 |
| CHEMBL447666 | — | — | 1 | 9.17 |
| CHEMBL229430 | AMG-517 | 1.0 | 1 | 9.05 |
| CHEMBL500900 | — | — | 1 | 9.00 |
| CHEMBL500380 | — | — | 1 | 8.92 |
| CHEMBL525417 | — | — | 1 | 8.62 |
| CHEMBL500379 | — | — | 1 | 8.55 |
| CHEMBL496135 | — | — | 1 | 8.38 |
| CHEMBL496725 | — | — | 1 | 8.09 |
| CHEMBL482411 | — | — | 1 | 8.00 |
| CHEMBL498610 | — | — | 1 | 7.89 |
| CHEMBL499990 | — | — | 1 | 7.77 |
| CHEMBL497567 | — | — | 1 | 7.20 |
| CHEMBL522726 | — | — | 1 | 6.89 |
| CHEMBL496525 | — | — | 1 | 6.68 |
| CHEMBL444499 | — | — | 1 | 6.55 |
| CHEMBL499309 | — | — | 1 | 6.28 |
| CHEMBL522078 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455580 | — | IC50 | = | 0.069 | nM | 10.16 |
| CHEMBL445237 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL525804 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL453146 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL447666 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL229430 | AMG-517 | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL500900 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL500380 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL525417 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL500379 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL496135 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL496725 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL482411 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL498610 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL499990 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL497567 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL522726 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL496525 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL444499 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL499309 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL522078 | — | IC50 | > | 4000.0 | nM | - |