Assay Detail
Binding
CHEMBL2428536
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-stimulated Ca2+ uptake
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.36 | 8.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595262 | — | — | 1 | 8.65 |
| CHEMBL2425546 | — | — | 1 | 8.61 |
| CHEMBL2425543 | — | — | 1 | 8.57 |
| CHEMBL2425545 | — | — | 1 | 8.39 |
| CHEMBL2425549 | — | — | 1 | 8.28 |
| CHEMBL2425548 | — | — | 1 | 7.67 |
| CHEMBL2425544 | — | — | 1 | - |
| CHEMBL2425551 | — | — | 1 | - |
| CHEMBL2425550 | — | — | 1 | - |
| CHEMBL2425547 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595262 | — | Ki | = | 2.23 | nM | 8.65 |
| CHEMBL2425546 | — | Ki | = | 2.46 | nM | 8.61 |
| CHEMBL2425543 | — | Ki | = | 2.68 | nM | 8.57 |
| CHEMBL2425545 | — | Ki | = | 4.06 | nM | 8.39 |
| CHEMBL2425549 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2425548 | — | Ki | = | 21.3 | nM | 7.67 |
| CHEMBL2425544 | — | Ki | - | — | - | |
| CHEMBL2425551 | — | Ki | - | — | - | |
| CHEMBL2425550 | — | Ki | - | — | - | |
| CHEMBL2425547 | — | Ki | - | — | - |