Assay Detail
Binding
CHEMBL2045501
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells after 60 mins by scintillation counting
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.72 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2042266 | — | — | 1 | 8.13 |
| CHEMBL2042384 | — | — | 1 | 7.70 |
| CHEMBL2042383 | — | — | 1 | 7.63 |
| CHEMBL2042399 | — | — | 1 | 7.61 |
| CHEMBL2042265 | — | — | 1 | 7.51 |
| CHEMBL2042396 | — | — | 1 | 7.48 |
| CHEMBL2042264 | — | — | 1 | 7.33 |
| CHEMBL229213 | — | — | 1 | 7.29 |
| CHEMBL388824 | — | — | 1 | 7.27 |
| CHEMBL228451 | — | — | 1 | 7.20 |
| CHEMBL2042263 | — | — | 1 | 6.97 |
| CHEMBL2042387 | — | — | 1 | 6.46 |
| CHEMBL2042385 | — | — | 1 | 6.44 |
| CHEMBL364193 | — | — | 1 | 6.33 |
| CHEMBL2042397 | — | — | 1 | 6.27 |
| CHEMBL2042398 | — | — | 1 | 6.12 |
| CHEMBL2042386 | — | — | 1 | 5.85 |
| CHEMBL2042390 | — | — | 1 | 5.79 |
| CHEMBL2042391 | — | — | 1 | 5.43 |
| CHEMBL2042388 | — | — | 1 | 5.17 |
| CHEMBL2042394 | — | — | 1 | 5.16 |
| CHEMBL2042389 | — | — | 1 | - |
| CHEMBL2042392 | — | — | 1 | - |
| CHEMBL2042393 | — | — | 1 | - |
| CHEMBL2042395 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2042266 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL2042384 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL2042383 | — | Ki | = | 23.3 | nM | 7.63 |
| CHEMBL2042399 | — | Ki | = | 24.4 | nM | 7.61 |
| CHEMBL2042265 | — | Ki | = | 30.7 | nM | 7.51 |
| CHEMBL2042396 | — | Ki | = | 32.8 | nM | 7.48 |
| CHEMBL2042264 | — | Ki | = | 46.2 | nM | 7.33 |
| CHEMBL229213 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL388824 | — | Ki | = | 53.5 | nM | 7.27 |
| CHEMBL228451 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2042263 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL2042387 | — | Ki | = | 344.0 | nM | 6.46 |
| CHEMBL2042385 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL364193 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL2042397 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL2042398 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL2042386 | — | Ki | = | 1420.0 | nM | 5.85 |
| CHEMBL2042390 | — | Ki | = | 1606.0 | nM | 5.79 |
| CHEMBL2042391 | — | Ki | = | 3710.0 | nM | 5.43 |
| CHEMBL2042388 | — | Ki | = | 6700.0 | nM | 5.17 |
| CHEMBL2042394 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL2042389 | — | Ki | - | — | - | |
| CHEMBL2042392 | — | Ki | - | — | - | |
| CHEMBL2042393 | — | Ki | - | — | - | |
| CHEMBL2042395 | — | Ki | - | — | - |