Assay Detail
Functional
CHEMBL890293
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 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 | 6.85 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL226672 | — | — | 1 | 8.70 |
| CHEMBL226723 | — | — | 1 | 8.35 |
| CHEMBL226724 | — | — | 1 | 8.13 |
| CHEMBL195789 | — | — | 1 | 7.10 |
| CHEMBL227364 | — | — | 1 | 6.92 |
| CHEMBL227310 | — | — | 1 | 6.64 |
| CHEMBL226619 | — | — | 1 | 6.54 |
| CHEMBL226671 | — | — | 1 | 6.37 |
| CHEMBL226617 | — | — | 1 | 6.12 |
| CHEMBL226568 | — | — | 1 | 6.11 |
| CHEMBL390830 | — | — | 1 | 6.08 |
| CHEMBL226670 | — | — | 1 | 6.04 |
| CHEMBL227311 | — | — | 1 | 5.92 |
| CHEMBL376161 | — | — | 1 | - |
| CHEMBL227309 | — | — | 1 | - |
| CHEMBL227363 | — | — | 1 | - |
| CHEMBL389044 | — | — | 1 | - |
| CHEMBL229758 | — | — | 1 | - |
| CHEMBL227365 | — | — | 1 | - |
| CHEMBL226567 | — | — | 1 | - |
| CHEMBL226569 | — | — | 1 | - |
| CHEMBL226618 | — | — | 1 | - |
| CHEMBL390831 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL226672 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL226723 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL226724 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL195789 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL227364 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL227310 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL226619 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL226671 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL226617 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL226568 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL390830 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL226670 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL227311 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL376161 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227309 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227363 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL389044 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL229758 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227365 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226567 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226569 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL226618 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL390831 | — | IC50 | > | 4000.0 | nM | - |