Assay Detail
Binding
CHEMBL820100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 28 | 7.68 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL323134 | — | — | 1 | 9.52 |
| CHEMBL102486 | — | — | 1 | 9.10 |
| CHEMBL105046 | — | — | 1 | 8.92 |
| CHEMBL101751 | — | — | 1 | 8.89 |
| CHEMBL419351 | — | — | 1 | 8.89 |
| CHEMBL320906 | — | — | 1 | 8.85 |
| CHEMBL104623 | — | — | 1 | 8.40 |
| CHEMBL104028 | — | — | 1 | 8.30 |
| CHEMBL105252 | — | — | 1 | 8.22 |
| CHEMBL104757 | — | — | 1 | 8.05 |
| CHEMBL319037 | — | — | 1 | 7.96 |
| CHEMBL103590 | — | — | 1 | 7.77 |
| CHEMBL104176 | — | — | 1 | 7.77 |
| CHEMBL317011 | — | — | 1 | 7.72 |
| CHEMBL103063 | — | — | 1 | 7.66 |
| CHEMBL322396 | — | — | 1 | 7.64 |
| CHEMBL102010 | — | — | 1 | 7.51 |
| CHEMBL317045 | — | — | 1 | 7.39 |
| CHEMBL104445 | — | — | 1 | 7.22 |
| CHEMBL102073 | — | — | 1 | 7.15 |
| CHEMBL105101 | — | — | 1 | 7.01 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 6.92 |
| CHEMBL104892 | — | — | 1 | 6.80 |
| CHEMBL323352 | — | — | 1 | 6.71 |
| CHEMBL105694 | — | — | 1 | 6.48 |
| CHEMBL106391 | — | — | 1 | 6.40 |
| CHEMBL103898 | — | — | 1 | 5.89 |
| CHEMBL103842 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL323134 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL102486 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL105046 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL101751 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL419351 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL320906 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL104623 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL104028 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL105252 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL104757 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL319037 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL103590 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL104176 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL317011 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL103063 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL322396 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL102010 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL317045 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL104445 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL102073 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL105101 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL391997 | CAPSAZEPINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL104892 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL323352 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL105694 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL106391 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL103898 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL103842 | — | Ki | = | 1440.0 | nM | 5.84 |