Assay Detail
Binding
CHEMBL926238
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Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells
30
Total Activities
30
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 | Intermediate |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.32 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595069 | IODORESINIFERATOXIN | — | 1 | 9.21 |
| CHEMBL399229 | — | — | 1 | 8.74 |
| CHEMBL254614 | — | — | 1 | 8.48 |
| CHEMBL254041 | — | — | 1 | 8.44 |
| CHEMBL254615 | — | — | 1 | 8.38 |
| CHEMBL254409 | — | — | 1 | 8.20 |
| CHEMBL400674 | — | — | 1 | 7.95 |
| CHEMBL445412 | — | — | 1 | 7.87 |
| CHEMBL254200 | — | — | 1 | 7.78 |
| CHEMBL253392 | — | — | 1 | 7.65 |
| CHEMBL400477 | — | — | 1 | 7.62 |
| CHEMBL254247 | — | — | 1 | 7.48 |
| CHEMBL254407 | — | — | 1 | 7.37 |
| CHEMBL428063 | — | — | 1 | 7.28 |
| CHEMBL254245 | — | — | 1 | 7.27 |
| CHEMBL253393 | — | — | 1 | 7.26 |
| CHEMBL254408 | — | — | 1 | 7.19 |
| CHEMBL254454 | — | — | 1 | 7.15 |
| CHEMBL72104 | — | — | 1 | 7.13 |
| CHEMBL254246 | — | — | 1 | 6.92 |
| CHEMBL398652 | — | — | 1 | 6.82 |
| CHEMBL73418 | — | — | 1 | 6.80 |
| CHEMBL254665 | — | — | 1 | 6.62 |
| CHEMBL254456 | — | — | 1 | 6.55 |
| CHEMBL403134 | — | — | 1 | 6.53 |
| CHEMBL402928 | — | — | 1 | 6.43 |
| CHEMBL254455 | — | — | 1 | 6.43 |
| CHEMBL254663 | — | — | 1 | 6.40 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 5.89 |
| CHEMBL254664 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595069 | IODORESINIFERATOXIN | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL399229 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL254614 | — | Ki | = | 3.29 | nM | 8.48 |
| CHEMBL254041 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL254615 | — | Ki | = | 4.12 | nM | 8.38 |
| CHEMBL254409 | — | Ki | = | 6.26 | nM | 8.20 |
| CHEMBL400674 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL445412 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL254200 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL253392 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL400477 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL254247 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL254407 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL428063 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL254245 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL253393 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL254408 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL254454 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL72104 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL254246 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL398652 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL73418 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL254665 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL254456 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL403134 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL402928 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL254455 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL254663 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL254664 | — | Ki | = | 1580.0 | nM | 5.80 |