Assay Detail
Binding
CHEMBL820101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]RTX binding to human Vanilloid receptor subtype 1 expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 9.04 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | 3.0 | 1 | 9.32 |
| CHEMBL18441 | — | — | 1 | 9.15 |
| CHEMBL18246 | — | — | 1 | 8.85 |
| CHEMBL18058 | — | — | 1 | 8.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL18441 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL18246 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL18058 | — | Ki | = | 1.46 | nM | 8.84 |