Assay Detail
Binding
CHEMBL876782
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In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells
28
Total Activities
28
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 '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 | 28 | 5.85 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229213 | — | — | 1 | 7.30 |
| CHEMBL388824 | — | — | 1 | 7.27 |
| CHEMBL228451 | — | — | 1 | 7.20 |
| CHEMBL188022 | — | — | 1 | 6.35 |
| CHEMBL187886 | — | — | 1 | 6.34 |
| CHEMBL364193 | — | — | 1 | 6.33 |
| CHEMBL190536 | — | — | 1 | 6.11 |
| CHEMBL187675 | — | — | 1 | 6.10 |
| CHEMBL190293 | — | — | 1 | 6.03 |
| CHEMBL363105 | — | — | 1 | 5.96 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 5.89 |
| CHEMBL188472 | — | — | 1 | 5.88 |
| CHEMBL427163 | — | — | 1 | 5.88 |
| CHEMBL185683 | — | — | 1 | 5.68 |
| CHEMBL188621 | — | — | 1 | 5.66 |
| CHEMBL363244 | — | — | 1 | 5.64 |
| CHEMBL188602 | — | — | 1 | 5.59 |
| CHEMBL188045 | — | — | 1 | 5.57 |
| CHEMBL186886 | — | — | 1 | 5.46 |
| CHEMBL186109 | — | — | 1 | 5.37 |
| CHEMBL190431 | — | — | 1 | 5.34 |
| CHEMBL186726 | — | — | 1 | 5.28 |
| CHEMBL186114 | — | — | 1 | 5.28 |
| CHEMBL361694 | — | — | 1 | 5.19 |
| CHEMBL362112 | — | — | 1 | 5.19 |
| CHEMBL189569 | — | — | 1 | 5.14 |
| CHEMBL186221 | — | — | 1 | 4.92 |
| CHEMBL187401 | — | — | 1 | - |
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 |
| CHEMBL188022 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL187886 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL364193 | — | Ki | = | 472.0 | nM | 6.33 |
| CHEMBL190536 | — | Ki | = | 772.0 | nM | 6.11 |
| CHEMBL187675 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL190293 | — | Ki | = | 926.0 | nM | 6.03 |
| CHEMBL363105 | — | Ki | = | 1090.0 | nM | 5.96 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL188472 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL427163 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL185683 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL188621 | — | Ki | = | 2170.0 | nM | 5.66 |
| CHEMBL363244 | — | Ki | = | 2270.0 | nM | 5.64 |
| CHEMBL188602 | — | Ki | = | 2560.0 | nM | 5.59 |
| CHEMBL188045 | — | Ki | = | 2710.0 | nM | 5.57 |
| CHEMBL186886 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL186109 | — | Ki | = | 4260.0 | nM | 5.37 |
| CHEMBL190431 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL186726 | — | Ki | = | 5220.0 | nM | 5.28 |
| CHEMBL186114 | — | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL361694 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL362112 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL189569 | — | Ki | = | 7180.0 | nM | 5.14 |
| CHEMBL186221 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL187401 | — | Ki | > | 25000.0 | nM | - |