Assay Detail
Functional
CHEMBL820091
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels.
28
Total Activities
28
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 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.54 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102073 | — | — | 1 | 8.62 |
| CHEMBL419351 | — | — | 1 | 8.52 |
| CHEMBL323134 | — | — | 1 | 8.52 |
| CHEMBL101751 | — | — | 1 | 8.52 |
| CHEMBL104028 | — | — | 1 | 8.52 |
| CHEMBL104757 | — | — | 1 | 8.40 |
| CHEMBL105046 | — | — | 1 | 8.30 |
| CHEMBL102486 | — | — | 1 | 8.22 |
| CHEMBL102010 | — | — | 1 | 8.22 |
| CHEMBL103590 | — | — | 1 | 8.00 |
| CHEMBL105252 | — | — | 1 | 7.96 |
| CHEMBL322396 | — | — | 1 | 7.96 |
| CHEMBL104623 | — | — | 1 | 7.89 |
| CHEMBL317045 | — | — | 1 | 7.72 |
| CHEMBL103063 | — | — | 1 | 7.72 |
| CHEMBL317011 | — | — | 1 | 7.50 |
| CHEMBL320906 | — | — | 1 | 7.50 |
| CHEMBL104445 | — | — | 1 | 7.42 |
| CHEMBL323352 | — | — | 1 | 7.35 |
| CHEMBL105101 | — | — | 1 | 7.13 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 7.00 |
| CHEMBL104176 | — | — | 1 | 6.77 |
| CHEMBL104892 | — | — | 1 | 6.65 |
| CHEMBL319037 | — | — | 1 | 6.39 |
| CHEMBL105694 | — | — | 1 | 6.31 |
| CHEMBL103898 | — | — | 1 | 6.17 |
| CHEMBL103842 | — | — | 1 | 6.00 |
| CHEMBL106391 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102073 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL419351 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL323134 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL101751 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL104028 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL104757 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL105046 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL102486 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL102010 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL103590 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL105252 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL322396 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL104623 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL317045 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL103063 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL317011 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL320906 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL104445 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL323352 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL105101 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL104176 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL104892 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL319037 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL105694 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL103898 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL103842 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL106391 | — | IC50 | = | 1500.0 | nM | 5.82 |