Assay Detail
Functional
CHEMBL889156
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Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx
23
Total Activities
23
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
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.69 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL226723 | — | — | 1 | 8.18 |
| CHEMBL226724 | — | — | 1 | 8.10 |
| CHEMBL226672 | — | — | 1 | 7.66 |
| CHEMBL195789 | — | — | 1 | 6.46 |
| CHEMBL226619 | — | — | 1 | 6.17 |
| CHEMBL227364 | — | — | 1 | 6.17 |
| CHEMBL226671 | — | — | 1 | 5.92 |
| CHEMBL227310 | — | — | 1 | 5.89 |
| CHEMBL226618 | — | — | 1 | 5.66 |
| CHEMBL226569 | — | — | 1 | - |
| CHEMBL390830 | — | — | 1 | - |
| CHEMBL226568 | — | — | 1 | - |
| CHEMBL226567 | — | — | 1 | - |
| CHEMBL227365 | — | — | 1 | - |
| CHEMBL389044 | — | — | 1 | - |
| CHEMBL227363 | — | — | 1 | - |
| CHEMBL227311 | — | — | 1 | - |
| CHEMBL376161 | — | — | 1 | - |
| CHEMBL229758 | — | — | 1 | - |
| CHEMBL226670 | — | — | 1 | - |
| CHEMBL390831 | — | — | 1 | - |
| CHEMBL226617 | — | — | 1 | - |
| CHEMBL227309 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL226723 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL226724 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL226672 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL195789 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL226619 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL227364 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL226671 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL227310 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL226618 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL226569 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL390830 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226568 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226567 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227365 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL389044 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227363 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227311 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL376161 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL229758 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226670 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL390831 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226617 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227309 | — | IC50 | > | 4000.0 | nM | - |