Assay Detail
Binding
CHEMBL833041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding to human vanilloid receptor subtype VR1
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.94 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL104028 | — | — | 1 | 8.40 |
| CHEMBL103063 | — | — | 1 | 7.72 |
| CHEMBL317045 | — | — | 1 | 7.70 |
| CHEMBL191990 | — | — | 1 | 7.66 |
| CHEMBL175748 | — | — | 1 | 7.43 |
| CHEMBL176044 | — | — | 1 | 7.38 |
| CHEMBL364087 | — | — | 1 | 7.36 |
| CHEMBL322396 | — | — | 1 | 7.29 |
| CHEMBL177554 | — | — | 1 | 7.06 |
| CHEMBL192113 | — | — | 1 | 6.96 |
| CHEMBL175831 | — | — | 1 | 6.77 |
| CHEMBL179296 | — | — | 1 | 6.76 |
| CHEMBL178939 | — | — | 1 | 6.72 |
| CHEMBL192023 | — | — | 1 | 6.65 |
| CHEMBL193279 | — | — | 1 | 6.50 |
| CHEMBL192114 | — | — | 1 | 6.50 |
| CHEMBL193090 | — | — | 1 | 6.38 |
| CHEMBL367774 | — | — | 1 | 5.96 |
| CHEMBL361017 | — | — | 1 | 5.82 |
| CHEMBL369517 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL104028 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL103063 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL317045 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL191990 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL175748 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL176044 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL364087 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL322396 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL177554 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL192113 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL175831 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL179296 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL178939 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL192023 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL193279 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL192114 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL193090 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL367774 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL361017 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL369517 | — | IC50 | = | 1700.0 | nM | 5.77 |