Assay Detail
Binding
CHEMBL3579074
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human recombinant TRPM8 expressed in CHO T-rex cells assessed as inhibition of WS12-induced calcium response pre-incubated for 20 mins before WS12 addition
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO T-rex |
| 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
Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.43 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577904 | — | — | 1 | 7.22 |
| CHEMBL3577902 | — | — | 1 | 7.21 |
| CHEMBL3577889 | — | — | 1 | 7.05 |
| CHEMBL3577881 | — | — | 1 | 7.03 |
| CHEMBL3577905 | — | — | 1 | 6.91 |
| CHEMBL3577883 | — | — | 1 | 6.84 |
| CHEMBL3577885 | PF-05105679 | 1.0 | 1 | 6.74 |
| CHEMBL3577907 | — | — | 1 | 6.72 |
| CHEMBL3577900 | — | — | 1 | 6.70 |
| CHEMBL3577906 | — | — | 1 | 6.63 |
| CHEMBL3577898 | — | — | 1 | 6.54 |
| CHEMBL3576881 | — | — | 1 | 6.51 |
| CHEMBL3577903 | — | — | 1 | 6.48 |
| CHEMBL3577886 | — | — | 1 | 6.47 |
| CHEMBL3577893 | — | — | 1 | 6.35 |
| CHEMBL3577880 | — | — | 1 | 6.08 |
| CHEMBL3577882 | — | — | 1 | 6.02 |
| CHEMBL3577890 | — | — | 1 | 5.94 |
| CHEMBL3577895 | — | — | 1 | 5.79 |
| CHEMBL3577891 | — | — | 1 | 5.48 |
| CHEMBL3577884 | — | — | 1 | 5.44 |
| CHEMBL3577901 | — | — | 1 | 5.21 |
| CHEMBL3577879 | — | — | 1 | - |
| CHEMBL3577887 | — | — | 1 | - |
| CHEMBL3577888 | — | — | 1 | - |
| CHEMBL3577892 | — | — | 1 | - |
| CHEMBL3577894 | — | — | 1 | - |
| CHEMBL3577896 | — | — | 1 | - |
| CHEMBL3577897 | — | — | 1 | - |
| CHEMBL3577899 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577904 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3577902 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3577889 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3577881 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3577905 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3577883 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL3577885 | PF-05105679 | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL3577907 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3577900 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3577906 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL3577898 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL3576881 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL3577903 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL3577886 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3577893 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL3577880 | — | IC50 | = | 837.0 | nM | 6.08 |
| CHEMBL3577882 | — | IC50 | = | 951.0 | nM | 6.02 |
| CHEMBL3577890 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL3577895 | — | IC50 | = | 1613.0 | nM | 5.79 |
| CHEMBL3577891 | — | IC50 | = | 3282.0 | nM | 5.48 |
| CHEMBL3577884 | — | IC50 | = | 3619.0 | nM | 5.44 |
| CHEMBL3577901 | — | IC50 | = | 6104.0 | nM | 5.21 |
| CHEMBL3577879 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3577887 | — | IC50 | > | 6166.0 | nM | - |
| CHEMBL3577888 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3577892 | — | IC50 | > | 7820.0 | nM | - |
| CHEMBL3577894 | — | IC50 | > | 3249.0 | nM | - |
| CHEMBL3577896 | — | IC50 | > | 9356.0 | nM | - |
| CHEMBL3577897 | — | IC50 | > | 6863.0 | nM | - |
| CHEMBL3577899 | — | IC50 | > | 10000.0 | nM | - |