Assay Detail
Binding
CHEMBL2428533
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake
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 |
|---|---|---|---|
| EC50 | 12 | 7.88 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | 3.0 | 1 | 9.04 |
| CHEMBL2425550 | — | — | 1 | 8.20 |
| CHEMBL2425547 | — | — | 1 | 7.79 |
| CHEMBL2425551 | — | — | 1 | 7.78 |
| CHEMBL2425544 | — | — | 1 | 7.75 |
| CHEMBL2425548 | — | — | 1 | 6.74 |
| CHEMBL2425543 | — | — | 1 | - |
| CHEMBL2425546 | — | — | 1 | - |
| CHEMBL2425545 | — | — | 1 | - |
| CHEMBL595262 | — | — | 1 | - |
| CHEMBL2425549 | — | — | 1 | - |
| CHEMBL595069 | IODORESINIFERATOXIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17976 | RESINIFERATOXIN | EC50 | = | 0.92 | nM | 9.04 |
| CHEMBL2425550 | — | EC50 | = | 6.28 | nM | 8.20 |
| CHEMBL2425547 | — | EC50 | = | 16.3 | nM | 7.79 |
| CHEMBL2425551 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL2425544 | — | EC50 | = | 17.9 | nM | 7.75 |
| CHEMBL2425548 | — | EC50 | = | 183.0 | nM | 6.74 |
| CHEMBL2425543 | — | EC50 | - | — | - | |
| CHEMBL2425546 | — | EC50 | - | — | - | |
| CHEMBL2425545 | — | EC50 | - | — | - | |
| CHEMBL595262 | — | EC50 | - | — | - | |
| CHEMBL2425549 | — | EC50 | - | — | - | |
| CHEMBL595069 | IODORESINIFERATOXIN | EC50 | - | — | - |