Assay Detail
Binding
CHEMBL3363142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TRPV1 expressed in T-REx HEK cells assessed as increase in intracellular Ca2+ accumulation by Fluo-4 AM dye based fluorescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| 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
Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 4.74 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3325770 | — | — | 1 | 5.16 |
| CHEMBL2163793 | CATHARANTHINE BASE | — | 1 | 4.70 |
| CHEMBL3325767 | — | — | 1 | 4.58 |
| CHEMBL3325765 | — | — | 1 | 4.52 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | - |
| CHEMBL441472 | — | — | 1 | - |
| CHEMBL364613 | CORONARIDINE | — | 1 | - |
| CHEMBL3325769 | — | — | 1 | - |
| CHEMBL3325768 | — | — | 1 | - |
| CHEMBL445022 | VOACAMINE | — | 1 | - |
| CHEMBL3325766 | — | — | 1 | - |
| CHEMBL463317 | VOACRISTINE | — | 1 | - |
| CHEMBL182120 | VOACANGINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3325770 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2163793 | CATHARANTHINE BASE | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3325767 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3325765 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL391997 | CAPSAZEPINE | EC50 | - | — | - | |
| CHEMBL441472 | — | EC50 | - | — | - | |
| CHEMBL364613 | CORONARIDINE | EC50 | - | — | - | |
| CHEMBL3325769 | — | EC50 | - | — | - | |
| CHEMBL3325768 | — | EC50 | - | — | - | |
| CHEMBL445022 | VOACAMINE | EC50 | - | — | - | |
| CHEMBL3325766 | — | EC50 | - | — | - | |
| CHEMBL463317 | VOACRISTINE | EC50 | - | — | - | |
| CHEMBL182120 | VOACANGINE | EC50 | - | — | - |