Assay Detail
Binding
CHEMBL4256797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as reduction in menthol-induced calcium flux incubated for 60 mins by Fluo-4 NW-dye based fluorimetric assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily M member 8 (CHEMBL5011) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.67 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4295040 | — | — | 1 | 7.40 |
| CHEMBL4284808 | — | — | 1 | 6.22 |
| CHEMBL4291622 | — | — | 1 | 5.80 |
| CHEMBL4287812 | — | — | 1 | 5.72 |
| CHEMBL4292679 | — | — | 1 | 5.66 |
| CHEMBL4277563 | — | — | 1 | 5.52 |
| CHEMBL1779158 | — | — | 1 | 5.50 |
| CHEMBL4288211 | — | — | 1 | 5.48 |
| CHEMBL4277150 | — | — | 1 | 5.48 |
| CHEMBL3900018 | — | — | 1 | 5.19 |
| CHEMBL4279001 | — | — | 1 | 5.09 |
| CHEMBL4284391 | — | — | 1 | 4.93 |
| CHEMBL4280979 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4295040 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4284808 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4291622 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4287812 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4292679 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4277563 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1779158 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4288211 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4277150 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3900018 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4279001 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL4284391 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL4280979 | — | IC50 | > | 100000.0 | nM | - |