Assay Detail
Functional
CHEMBL926241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium 45 uptake
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 29 | 7.44 | 9.24 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254615 | — | — | 1 | 9.24 |
| CHEMBL445412 | — | — | 1 | 8.49 |
| CHEMBL399229 | — | — | 1 | 8.28 |
| CHEMBL254245 | — | — | 1 | 8.11 |
| CHEMBL254407 | — | — | 1 | 8.07 |
| CHEMBL254200 | — | — | 1 | 8.00 |
| CHEMBL254247 | — | — | 1 | 7.97 |
| CHEMBL254409 | — | — | 1 | 7.96 |
| CHEMBL254614 | — | — | 1 | 7.92 |
| CHEMBL595069 | IODORESINIFERATOXIN | — | 1 | 7.91 |
| CHEMBL254041 | — | — | 1 | 7.91 |
| CHEMBL254454 | — | — | 1 | 7.87 |
| CHEMBL428063 | — | — | 1 | 7.52 |
| CHEMBL400674 | — | — | 1 | 7.44 |
| CHEMBL254246 | — | — | 1 | 7.42 |
| CHEMBL253392 | — | — | 1 | 7.28 |
| CHEMBL253393 | — | — | 1 | 7.28 |
| CHEMBL254456 | — | — | 1 | 7.19 |
| CHEMBL403134 | — | — | 1 | 7.01 |
| CHEMBL254455 | — | — | 1 | 6.98 |
| CHEMBL254665 | — | — | 1 | 6.93 |
| CHEMBL398652 | — | — | 1 | 6.88 |
| CHEMBL254408 | — | — | 1 | 6.85 |
| CHEMBL73418 | — | — | 1 | 6.82 |
| CHEMBL254663 | — | — | 1 | 6.71 |
| CHEMBL402928 | — | — | 1 | 6.69 |
| CHEMBL72104 | — | — | 1 | 6.36 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 6.28 |
| CHEMBL254664 | — | — | 1 | 6.25 |
| CHEMBL400477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254615 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL445412 | — | Ki | = | 3.24 | nM | 8.49 |
| CHEMBL399229 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL254245 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL254407 | — | Ki | = | 8.56 | nM | 8.07 |
| CHEMBL254200 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL254247 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL254409 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL254614 | — | Ki | = | 12.1 | nM | 7.92 |
| CHEMBL595069 | IODORESINIFERATOXIN | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL254041 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL254454 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL428063 | — | Ki | = | 30.3 | nM | 7.52 |
| CHEMBL400674 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL254246 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL253392 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL253393 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL254456 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL403134 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL254455 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL254665 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL398652 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL254408 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL73418 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL254663 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL402928 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL72104 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL254664 | — | Ki | = | 567.0 | nM | 6.25 |
| CHEMBL400477 | — | Activity | - | — | - |