Assay Detail
Binding
CHEMBL828734
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Inhibition of rat transient receptor potential vanilloid 1 receptor (n=3)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.02 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL362673 | — | — | 1 | 7.00 |
| CHEMBL440749 | — | — | 1 | 6.71 |
| CHEMBL3138733 | — | — | 1 | 6.66 |
| CHEMBL369647 | — | — | 1 | 6.39 |
| CHEMBL175893 | — | — | 1 | 6.06 |
| CHEMBL177827 | — | — | 1 | 6.04 |
| CHEMBL367039 | — | — | 1 | 5.64 |
| CHEMBL175763 | — | — | 1 | 4.88 |
| CHEMBL369137 | — | — | 1 | 4.83 |
| CHEMBL177219 | — | — | 1 | - |
| CHEMBL177897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL362673 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL440749 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3138733 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL369647 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL175893 | — | IC50 | = | 863.0 | nM | 6.06 |
| CHEMBL177827 | — | IC50 | = | 908.0 | nM | 6.04 |
| CHEMBL367039 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL175763 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL369137 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL177219 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL177897 | — | IC50 | > | 10000.0 | nM | - |