Assay Detail
Functional
CHEMBL820102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.00 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121308 | — | — | 1 | 8.41 |
| CHEMBL333196 | — | — | 1 | 8.34 |
| CHEMBL123062 | — | — | 1 | 7.95 |
| CHEMBL120891 | — | — | 1 | 7.94 |
| CHEMBL120619 | — | — | 1 | 7.76 |
| CHEMBL120327 | — | — | 1 | 7.60 |
| CHEMBL120053 | — | — | 1 | 7.56 |
| CHEMBL120690 | — | — | 1 | 7.53 |
| CHEMBL441472 | — | — | 1 | 7.46 |
| CHEMBL449086 | — | — | 1 | 7.38 |
| CHEMBL120713 | — | — | 1 | 7.25 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 7.24 |
| CHEMBL420171 | — | — | 1 | 7.24 |
| CHEMBL120505 | — | — | 1 | 7.20 |
| CHEMBL120803 | — | — | 1 | 7.03 |
| CHEMBL413109 | — | — | 1 | 6.97 |
| CHEMBL118186 | — | — | 1 | 6.96 |
| CHEMBL120875 | — | — | 1 | 6.93 |
| CHEMBL120772 | — | — | 1 | 6.72 |
| CHEMBL120358 | — | — | 1 | 6.70 |
| CHEMBL120576 | — | — | 1 | 6.64 |
| CHEMBL121736 | — | — | 1 | 6.61 |
| CHEMBL420877 | — | — | 1 | 6.59 |
| CHEMBL121092 | — | — | 1 | 6.54 |
| CHEMBL121236 | — | — | 1 | 6.54 |
| CHEMBL120849 | — | — | 1 | 6.32 |
| CHEMBL122241 | — | — | 1 | 6.31 |
| CHEMBL121336 | — | — | 1 | 6.25 |
| CHEMBL122298 | — | — | 1 | 6.18 |
| CHEMBL121632 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121308 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL333196 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL123062 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL120891 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL120619 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL120327 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL120053 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL120690 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL441472 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL449086 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL120713 | — | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL420171 | — | IC50 | = | 57.5 | nM | 7.24 |
| CHEMBL120505 | — | IC50 | = | 63.5 | nM | 7.20 |
| CHEMBL120803 | — | IC50 | = | 93.2 | nM | 7.03 |
| CHEMBL413109 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL118186 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL120875 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL120772 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL120358 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL120576 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL121736 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL420877 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL121092 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL121236 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL120849 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL122241 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL121336 | — | IC50 | = | 556.0 | nM | 6.25 |
| CHEMBL122298 | — | IC50 | = | 655.0 | nM | 6.18 |
| CHEMBL121632 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL419051 | — | IC50 | = | 1106.0 | nM | 5.96 |
| CHEMBL332086 | — | IC50 | = | 1365.0 | nM | 5.87 |