Assay Detail
Binding
CHEMBL839583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX
24
Total Activities
24
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 | 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 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.02 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229213 | — | — | 1 | 7.30 |
| CHEMBL388824 | — | — | 1 | 7.27 |
| CHEMBL228451 | — | — | 1 | 7.20 |
| CHEMBL186574 | — | — | 1 | 6.84 |
| CHEMBL190637 | — | — | 1 | 6.84 |
| CHEMBL363267 | — | — | 1 | 6.67 |
| CHEMBL426266 | — | — | 1 | 6.64 |
| CHEMBL365213 | — | — | 1 | 6.36 |
| CHEMBL188155 | — | — | 1 | 6.24 |
| CHEMBL165272 | — | — | 1 | 6.19 |
| CHEMBL188024 | — | — | 1 | 6.12 |
| CHEMBL363890 | — | — | 1 | 6.00 |
| CHEMBL361931 | — | — | 1 | 5.94 |
| CHEMBL189418 | — | — | 1 | 5.89 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 5.89 |
| CHEMBL424803 | — | — | 1 | 5.44 |
| CHEMBL187735 | — | — | 1 | 5.41 |
| CHEMBL425180 | — | — | 1 | 5.39 |
| CHEMBL370055 | — | — | 1 | 5.33 |
| CHEMBL189507 | — | — | 1 | 5.22 |
| CHEMBL188264 | — | — | 1 | 5.21 |
| CHEMBL191024 | — | — | 1 | 5.09 |
| CHEMBL189640 | — | — | 1 | 5.02 |
| CHEMBL187838 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229213 | — | Ki | = | 50.4 | nM | 7.30 |
| CHEMBL388824 | — | Ki | = | 53.5 | nM | 7.27 |
| CHEMBL228451 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL186574 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL190637 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL363267 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL426266 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL365213 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL188155 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL165272 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL188024 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL363890 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL361931 | — | Ki | = | 1160.0 | nM | 5.94 |
| CHEMBL189418 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL424803 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL187735 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL425180 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL370055 | — | Ki | = | 4640.0 | nM | 5.33 |
| CHEMBL189507 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL188264 | — | Ki | = | 6120.0 | nM | 5.21 |
| CHEMBL191024 | — | Ki | = | 8072.0 | nM | 5.09 |
| CHEMBL189640 | — | Ki | = | 9560.0 | nM | 5.02 |
| CHEMBL187838 | — | Ki | = | 11900.0 | nM | 4.92 |