Assay Detail
Functional
CHEMBL906775
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Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay
20
Total Activities
20
Compounds Tested
2
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
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 | 18 | 6.90 | 8.35 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412885 | — | — | 1 | 8.35 |
| CHEMBL388824 | — | — | 1 | 8.04 |
| CHEMBL228728 | — | — | 1 | 8.04 |
| CHEMBL288760 | — | — | 1 | 7.83 |
| CHEMBL229214 | — | — | 1 | 7.54 |
| CHEMBL228416 | — | — | 1 | 7.43 |
| CHEMBL228451 | — | — | 1 | 7.27 |
| CHEMBL228465 | — | — | 1 | 7.27 |
| CHEMBL228676 | — | — | 1 | 7.22 |
| CHEMBL265865 | — | — | 1 | 6.65 |
| CHEMBL229218 | — | — | 1 | 6.61 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 1 | 6.28 |
| CHEMBL229217 | — | — | 1 | 6.18 |
| CHEMBL229162 | — | — | 1 | 6.16 |
| CHEMBL388282 | — | — | 1 | 6.07 |
| CHEMBL229163 | — | — | 1 | 6.01 |
| CHEMBL228725 | — | — | 1 | 5.75 |
| CHEMBL390608 | — | — | 1 | 5.57 |
| CHEMBL433276 | — | — | 1 | - |
| CHEMBL229213 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412885 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL388824 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL228728 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL288760 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL229214 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL228416 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL228451 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL228465 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL228676 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL265865 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL229218 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL229217 | — | Ki | = | 663.0 | nM | 6.18 |
| CHEMBL229162 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL388282 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL229163 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL228725 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL390608 | — | Ki | = | 2670.0 | nM | 5.57 |
| CHEMBL433276 | — | Activity | - | — | - | |
| CHEMBL229213 | — | Activity | = | 84.0 | % | - |