Assay Detail
Binding
CHEMBL906773
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
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.57 | 7.41 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228416 | — | — | 1 | 7.41 |
| CHEMBL412885 | — | — | 1 | 7.39 |
| CHEMBL229213 | — | — | 1 | 7.29 |
| CHEMBL228728 | — | — | 1 | 7.27 |
| CHEMBL388824 | — | — | 1 | 7.27 |
| CHEMBL288760 | — | — | 1 | 7.23 |
| CHEMBL228451 | — | — | 1 | 7.20 |
| CHEMBL229214 | — | — | 1 | 7.17 |
| CHEMBL388282 | — | — | 1 | 7.00 |
| CHEMBL228676 | — | — | 1 | 6.77 |
| CHEMBL228465 | — | — | 1 | 6.64 |
| CHEMBL265865 | — | — | 1 | 6.47 |
| CHEMBL229218 | — | — | 1 | 6.43 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 5.89 |
| CHEMBL229162 | — | — | 1 | 5.76 |
| CHEMBL390608 | — | — | 1 | 5.67 |
| CHEMBL229217 | — | — | 1 | 5.54 |
| CHEMBL433276 | — | — | 1 | 5.40 |
| CHEMBL229163 | — | — | 1 | 5.11 |
| CHEMBL228725 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228416 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL412885 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL229213 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL228728 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL388824 | — | Ki | = | 53.5 | nM | 7.27 |
| CHEMBL288760 | — | Ki | = | 59.3 | nM | 7.23 |
| CHEMBL228451 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL229214 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL388282 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL228676 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL228465 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL265865 | — | Ki | = | 339.0 | nM | 6.47 |
| CHEMBL229218 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL229162 | — | Ki | = | 1740.0 | nM | 5.76 |
| CHEMBL390608 | — | Ki | = | 2140.0 | nM | 5.67 |
| CHEMBL229217 | — | Ki | = | 2890.0 | nM | 5.54 |
| CHEMBL433276 | — | Ki | = | 3950.0 | nM | 5.40 |
| CHEMBL229163 | — | Ki | = | 7700.0 | nM | 5.11 |
| CHEMBL228725 | — | Activity | - | — | - |