Assay Detail
Functional
CHEMBL828080
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity towards rat TRPV1 expressed in CHO cells
22
Total Activities
22
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 | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.27 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229213 | — | — | 1 | 8.47 |
| CHEMBL388824 | — | — | 1 | 8.04 |
| CHEMBL228451 | — | — | 1 | 7.27 |
| CHEMBL187886 | — | — | 1 | 6.96 |
| CHEMBL364193 | — | — | 1 | 6.93 |
| CHEMBL188022 | — | — | 1 | 6.92 |
| CHEMBL188602 | — | — | 1 | 6.65 |
| CHEMBL190536 | — | — | 1 | 6.65 |
| CHEMBL185683 | — | — | 1 | 6.40 |
| CHEMBL363105 | — | — | 1 | 6.33 |
| CHEMBL186109 | — | — | 1 | 6.33 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 6.28 |
| CHEMBL427163 | — | — | 1 | 6.24 |
| CHEMBL188472 | — | — | 1 | 6.20 |
| CHEMBL186221 | — | — | 1 | 5.84 |
| CHEMBL362112 | — | — | 1 | 5.70 |
| CHEMBL188045 | — | — | 1 | 5.33 |
| CHEMBL190431 | — | — | 1 | 5.20 |
| CHEMBL361694 | — | — | 1 | 5.18 |
| CHEMBL186726 | — | — | 1 | 5.17 |
| CHEMBL188621 | — | — | 1 | 5.08 |
| CHEMBL189569 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229213 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL388824 | — | Ki | = | 9.16 | nM | 8.04 |
| CHEMBL228451 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL187886 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL364193 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL188022 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL188602 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL190536 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL185683 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL363105 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL186109 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL427163 | — | Ki | = | 579.0 | nM | 6.24 |
| CHEMBL188472 | — | Ki | = | 635.0 | nM | 6.20 |
| CHEMBL186221 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL362112 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL188045 | — | Ki | = | 4656.0 | nM | 5.33 |
| CHEMBL190431 | — | Ki | = | 6250.0 | nM | 5.20 |
| CHEMBL361694 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL186726 | — | Ki | = | 6760.0 | nM | 5.17 |
| CHEMBL188621 | — | Ki | = | 8400.0 | nM | 5.08 |
| CHEMBL189569 | — | Ki | = | 13555.0 | nM | 4.87 |