Assay Detail
Binding
CHEMBL3363422
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of menthol-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to menthol stimulation 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 | Mus musculus |
| Cell Type | HEK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily M member 8 (CHEMBL3108632) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 |
|---|---|---|---|
| IC50 | 13 | 5.35 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441472 | — | — | 1 | 6.40 |
| CHEMBL3325770 | — | — | 1 | 6.22 |
| CHEMBL2163793 | CATHARANTHINE BASE | — | 1 | 6.16 |
| CHEMBL364613 | CORONARIDINE | — | 1 | 5.52 |
| CHEMBL182120 | VOACANGINE | — | 1 | 5.05 |
| CHEMBL3325768 | — | — | 1 | 4.72 |
| CHEMBL3325769 | — | — | 1 | 4.41 |
| CHEMBL391997 | CAPSAZEPINE | — | 1 | 4.30 |
| CHEMBL3325767 | — | — | 1 | - |
| CHEMBL445022 | VOACAMINE | — | 1 | - |
| CHEMBL3325766 | — | — | 1 | - |
| CHEMBL463317 | VOACRISTINE | — | 1 | - |
| CHEMBL3325765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441472 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3325770 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2163793 | CATHARANTHINE BASE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL364613 | CORONARIDINE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL182120 | VOACANGINE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3325768 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3325769 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL391997 | CAPSAZEPINE | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3325767 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL445022 | VOACAMINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL3325766 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL463317 | VOACRISTINE | IC50 | - | — | - | |
| CHEMBL3325765 | — | IC50 | > | 100000.0 | nM | - |