Assay Detail
Functional
CHEMBL820103
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 low pH-induced activation of the rat VR1 channel in a HEK293 cell line
31
Total Activities
31
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 | 31 | 6.77 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441472 | — | — | 1 | 8.32 |
| CHEMBL121308 | — | — | 1 | 7.76 |
| CHEMBL120891 | — | — | 1 | 7.76 |
| CHEMBL120619 | — | — | 1 | 7.63 |
| CHEMBL333196 | — | — | 1 | 7.57 |
| CHEMBL420171 | — | — | 1 | 7.41 |
| CHEMBL413109 | — | — | 1 | 7.25 |
| CHEMBL123062 | — | — | 1 | 7.24 |
| CHEMBL120053 | — | — | 1 | 7.21 |
| CHEMBL449086 | — | — | 1 | 7.14 |
| CHEMBL120713 | — | — | 1 | 7.11 |
| CHEMBL120505 | — | — | 1 | 7.09 |
| CHEMBL120690 | — | — | 1 | 7.04 |
| CHEMBL118186 | — | — | 1 | 6.92 |
| CHEMBL120327 | — | — | 1 | 6.76 |
| CHEMBL120875 | — | — | 1 | 6.69 |
| CHEMBL120772 | — | — | 1 | 6.61 |
| CHEMBL120803 | — | — | 1 | 6.58 |
| CHEMBL120849 | — | — | 1 | 6.56 |
| CHEMBL121236 | — | — | 1 | 6.51 |
| CHEMBL121736 | — | — | 1 | 6.36 |
| CHEMBL121632 | — | — | 1 | 6.24 |
| CHEMBL120576 | — | — | 1 | 6.08 |
| CHEMBL420877 | — | — | 1 | 6.04 |
| CHEMBL122241 | — | — | 1 | 6.00 |
| CHEMBL120358 | — | — | 1 | 5.85 |
| CHEMBL121336 | — | — | 1 | 5.81 |
| CHEMBL122298 | — | — | 1 | 5.57 |
| CHEMBL332086 | — | — | 1 | 5.29 |
| CHEMBL121092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441472 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL121308 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL120891 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL120619 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL333196 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL420171 | — | IC50 | = | 39.2 | nM | 7.41 |
| CHEMBL413109 | — | IC50 | = | 56.6 | nM | 7.25 |
| CHEMBL123062 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL120053 | — | IC50 | = | 61.5 | nM | 7.21 |
| CHEMBL449086 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL120713 | — | IC50 | = | 77.4 | nM | 7.11 |
| CHEMBL120505 | — | IC50 | = | 81.4 | nM | 7.09 |
| CHEMBL120690 | — | IC50 | = | 91.7 | nM | 7.04 |
| CHEMBL118186 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL120327 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL120875 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL120772 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL120803 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL120849 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL121236 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL121736 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL121632 | — | IC50 | = | 575.0 | nM | 6.24 |
| CHEMBL120576 | — | IC50 | = | 828.0 | nM | 6.08 |
| CHEMBL420877 | — | IC50 | = | 916.0 | nM | 6.04 |
| CHEMBL122241 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL120358 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL121336 | — | IC50 | = | 1551.0 | nM | 5.81 |
| CHEMBL122298 | — | IC50 | = | 2669.0 | nM | 5.57 |
| CHEMBL332086 | — | IC50 | = | 5181.0 | nM | 5.29 |
| CHEMBL121092 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL419051 | — | IC50 | > | 25000.0 | nM | - |