Assay Detail
Binding
CHEMBL1017798
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Displacement of [3H]resiniferatoxin from rat TRPV1 expressed in CHO cells by scintillation counting
8
Total Activities
8
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
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.08 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229213 | — | — | 1 | 7.30 |
| CHEMBL228451 | — | — | 1 | 7.20 |
| CHEMBL475357 | — | — | 1 | 6.18 |
| CHEMBL475358 | — | — | 1 | 5.80 |
| CHEMBL474191 | — | — | 1 | 5.76 |
| CHEMBL474773 | — | — | 1 | 5.74 |
| CHEMBL474192 | — | — | 1 | 5.47 |
| CHEMBL516191 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229213 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL228451 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL475357 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL475358 | — | Ki | = | 1590.0 | nM | 5.80 |
| CHEMBL474191 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL474773 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL474192 | — | Ki | = | 3370.0 | nM | 5.47 |
| CHEMBL516191 | — | Ki | = | 6900.0 | nM | 5.16 |