Assay Detail
Functional
CHEMBL890307
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
29
Total Activities
29
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: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.19 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375681 | — | — | 1 | 9.19 |
| CHEMBL229430 | AMG-517 | 1.0 | 1 | 9.05 |
| CHEMBL227228 | — | — | 1 | 8.92 |
| CHEMBL226724 | — | — | 1 | 8.13 |
| CHEMBL227150 | — | — | 1 | 7.96 |
| CHEMBL373731 | — | — | 1 | 7.85 |
| CHEMBL376114 | — | — | 1 | 7.82 |
| CHEMBL227099 | — | — | 1 | 7.46 |
| CHEMBL227151 | — | — | 1 | 7.20 |
| CHEMBL373730 | — | — | 1 | 7.11 |
| CHEMBL226988 | — | — | 1 | 6.92 |
| CHEMBL226987 | — | — | 1 | 6.82 |
| CHEMBL415066 | — | — | 1 | 6.34 |
| CHEMBL226829 | — | — | 1 | 6.20 |
| CHEMBL226989 | — | — | 1 | 6.18 |
| CHEMBL226935 | — | — | 1 | 6.14 |
| CHEMBL227229 | — | — | 1 | 5.96 |
| CHEMBL227287 | — | — | 1 | 5.85 |
| CHEMBL375511 | — | — | 1 | 5.54 |
| CHEMBL227043 | — | — | 1 | - |
| CHEMBL227044 | — | — | 1 | - |
| CHEMBL227045 | — | — | 1 | - |
| CHEMBL227098 | — | — | 1 | - |
| CHEMBL227100 | — | — | 1 | - |
| CHEMBL227013 | — | — | 1 | - |
| CHEMBL389935 | — | — | 1 | - |
| CHEMBL227230 | — | — | 1 | - |
| CHEMBL229382 | — | — | 1 | - |
| CHEMBL227034 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375681 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL229430 | AMG-517 | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL227228 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL226724 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL227150 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL373731 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL376114 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL227099 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL227151 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL373730 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL226988 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL226987 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL415066 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL226829 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL226989 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL226935 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL227229 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL227287 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL375511 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL227043 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227044 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227045 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227098 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227100 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227013 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL389935 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227230 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL229382 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL227034 | — | IC50 | > | 4000.0 | nM | - |