Assay Detail
Binding
CHEMBL2428534
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]RTX from human TRPV1 expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.08 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | 3.0 | 1 | 8.91 |
| CHEMBL595069 | IODORESINIFERATOXIN | — | 1 | 7.93 |
| CHEMBL2425549 | — | — | 1 | 7.48 |
| CHEMBL595262 | — | — | 1 | 7.31 |
| CHEMBL2425548 | — | — | 1 | 7.30 |
| CHEMBL2425551 | — | — | 1 | 7.09 |
| CHEMBL2425547 | — | — | 1 | 6.86 |
| CHEMBL2425550 | — | — | 1 | 6.85 |
| CHEMBL2425546 | — | — | 1 | 6.67 |
| CHEMBL2425545 | — | — | 1 | 6.48 |
| CHEMBL2425544 | — | — | 1 | 6.08 |
| CHEMBL2425543 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | Ki | = | 1.23 | nM | 8.91 |
| CHEMBL595069 | IODORESINIFERATOXIN | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL2425549 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL595262 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL2425548 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2425551 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL2425547 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL2425550 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2425546 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL2425545 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL2425544 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL2425543 | — | Ki | = | 990.0 | nM | 6.00 |