Assay Detail
Binding
CHEMBL2444600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced 45Ca2+ uptake incubated for 10 mins prior to icilin-challenge measured after 4 mins by liquid scintillation counting analysis
31
Total Activities
31
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 M member 8 (CHEMBL1075319) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.01 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2443061 | — | — | 1 | 8.05 |
| CHEMBL2443079 | — | — | 1 | 8.02 |
| CHEMBL2443076 | — | — | 1 | 7.88 |
| CHEMBL2443063 | — | — | 1 | 7.78 |
| CHEMBL2443085 | — | — | 1 | 7.72 |
| CHEMBL2443077 | — | — | 1 | 7.71 |
| CHEMBL2443075 | — | — | 1 | 7.65 |
| CHEMBL2443086 | — | — | 1 | 7.39 |
| CHEMBL2443074 | — | — | 1 | 7.35 |
| CHEMBL2443060 | — | — | 1 | 7.33 |
| CHEMBL2443084 | — | — | 1 | 7.31 |
| CHEMBL2443062 | — | — | 1 | 7.22 |
| CHEMBL2443073 | — | — | 1 | 7.18 |
| CHEMBL2443072 | — | — | 1 | 7.04 |
| CHEMBL2443078 | — | — | 1 | 7.03 |
| CHEMBL2443083 | — | — | 1 | 7.01 |
| CHEMBL2443071 | — | — | 1 | 6.97 |
| CHEMBL2443070 | — | — | 1 | 6.96 |
| CHEMBL2443066 | — | — | 1 | 6.95 |
| CHEMBL2443089 | — | — | 1 | 6.75 |
| CHEMBL2440148 | — | — | 1 | 6.74 |
| CHEMBL2443068 | — | — | 1 | 6.64 |
| CHEMBL2443065 | — | — | 1 | 6.58 |
| CHEMBL2443081 | — | — | 1 | 6.55 |
| CHEMBL2443088 | — | — | 1 | 6.54 |
| CHEMBL2443067 | — | — | 1 | 6.53 |
| CHEMBL2443064 | — | — | 1 | 6.34 |
| CHEMBL2443087 | — | — | 1 | 6.26 |
| CHEMBL2443069 | — | — | 1 | 6.18 |
| CHEMBL2443082 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2443061 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2443079 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL2443076 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL2443063 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL2443085 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL2443077 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL2443075 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL2443086 | — | IC50 | = | 41.1 | nM | 7.39 |
| CHEMBL2443074 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL2443060 | — | IC50 | = | 46.3 | nM | 7.33 |
| CHEMBL2443084 | — | IC50 | = | 48.5 | nM | 7.31 |
| CHEMBL2443062 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2443073 | — | IC50 | = | 65.9 | nM | 7.18 |
| CHEMBL2443072 | — | IC50 | = | 90.1 | nM | 7.04 |
| CHEMBL2443078 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2443083 | — | IC50 | = | 97.3 | nM | 7.01 |
| CHEMBL2443071 | — | IC50 | = | 107.3 | nM | 6.97 |
| CHEMBL2443070 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL2443066 | — | IC50 | = | 113.1 | nM | 6.95 |
| CHEMBL2443089 | — | IC50 | = | 177.8 | nM | 6.75 |
| CHEMBL2440148 | — | IC50 | = | 182.1 | nM | 6.74 |
| CHEMBL2443068 | — | IC50 | = | 230.4 | nM | 6.64 |
| CHEMBL2443065 | — | IC50 | = | 265.8 | nM | 6.58 |
| CHEMBL2443081 | — | IC50 | = | 280.7 | nM | 6.55 |
| CHEMBL2443088 | — | IC50 | = | 289.6 | nM | 6.54 |
| CHEMBL2443067 | — | IC50 | = | 295.2 | nM | 6.53 |
| CHEMBL2443064 | — | IC50 | = | 457.2 | nM | 6.34 |
| CHEMBL2443087 | — | IC50 | = | 543.7 | nM | 6.26 |
| CHEMBL2443069 | — | IC50 | = | 656.9 | nM | 6.18 |
| CHEMBL2443082 | — | IC50 | = | 666.9 | nM | 6.18 |
| CHEMBL2443080 | — | IC50 | = | 2423.0 | nM | 5.62 |