Assay Detail
Functional
CHEMBL1017800
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 capsaicin-stimulated 45Ca2+ uptake
8
Total Activities
8
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 | 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 | 6.16 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229213 | — | — | 1 | 8.47 |
| CHEMBL228451 | — | — | 1 | 7.27 |
| CHEMBL475357 | — | — | 1 | 6.13 |
| CHEMBL474773 | — | — | 1 | 5.77 |
| CHEMBL475358 | — | — | 1 | 5.58 |
| CHEMBL474191 | — | — | 1 | 5.33 |
| CHEMBL474192 | — | — | 1 | 4.60 |
| CHEMBL516191 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229213 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL228451 | — | Ki | = | 53.9 | nM | 7.27 |
| CHEMBL475357 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL474773 | — | Ki | = | 1690.0 | nM | 5.77 |
| CHEMBL475358 | — | Ki | = | 2640.0 | nM | 5.58 |
| CHEMBL474191 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL474192 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL516191 | — | Ki | - | — | - |