Assay Detail
Binding
CHEMBL2091978
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Inhibition of rat TRPM8 expressed in HEK293 cells assessed as reduction in 0.25 uM icilin-stimulated increase in intracellular Ca2+ levels
35
Total Activities
35
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
Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.18 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087064 | — | — | 1 | 6.52 |
| CHEMBL2087057 | — | — | 1 | 6.22 |
| CHEMBL2087065 | — | — | 1 | 6.16 |
| CHEMBL2087060 | — | — | 1 | 6.05 |
| CHEMBL2087059 | — | — | 1 | 6.00 |
| CHEMBL2087052 | — | — | 1 | 5.72 |
| CHEMBL1385022 | — | — | 1 | 5.60 |
| CHEMBL2087053 | — | — | 1 | 5.50 |
| CHEMBL2087056 | — | — | 1 | 5.47 |
| CHEMBL2087055 | — | — | 1 | 5.32 |
| CHEMBL2087043 | — | — | 1 | 5.28 |
| CHEMBL2087067 | — | — | 1 | 5.24 |
| CHEMBL2087068 | — | — | 1 | 5.22 |
| CHEMBL2087046 | — | — | 1 | 5.19 |
| CHEMBL2087069 | — | — | 1 | 5.01 |
| CHEMBL2087063 | — | — | 1 | 4.94 |
| CHEMBL2087070 | — | — | 1 | 4.93 |
| CHEMBL2087054 | — | — | 1 | 4.91 |
| CHEMBL2087061 | — | — | 1 | 4.83 |
| CHEMBL2087045 | — | — | 1 | 4.67 |
| CHEMBL2087066 | — | — | 1 | 4.64 |
| CHEMBL2087062 | — | — | 1 | 4.51 |
| CHEMBL2087071 | — | — | 1 | 4.50 |
| CHEMBL2087073 | — | — | 1 | 4.43 |
| CHEMBL2087074 | — | — | 1 | 4.42 |
| CHEMBL2087044 | — | — | 1 | 4.37 |
| CHEMBL2087058 | — | — | 1 | 4.16 |
| CHEMBL2087075 | — | — | 1 | - |
| CHEMBL2087047 | — | — | 1 | - |
| CHEMBL2087048 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087064 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2087057 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2087065 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2087060 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2087059 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2087052 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1385022 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2087053 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2087056 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2087055 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2087043 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2087067 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2087068 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2087046 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2087069 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL2087063 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL2087070 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL2087054 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL2087061 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL2087045 | — | IC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL2087066 | — | IC50 | = | 23100.0 | nM | 4.64 |
| CHEMBL2087062 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL2087071 | — | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL2087073 | — | IC50 | = | 37400.0 | nM | 4.43 |
| CHEMBL2087074 | — | IC50 | = | 38500.0 | nM | 4.42 |
| CHEMBL2087044 | — | IC50 | = | 42700.0 | nM | 4.37 |
| CHEMBL2087058 | — | IC50 | = | 69400.0 | nM | 4.16 |
| CHEMBL2087075 | — | IC50 | = | 238000.0 | nM | - |
| CHEMBL2087047 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2087048 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2087049 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2087050 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2087051 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL29411 | THYMOL | IC50 | = | 314600.0 | nM | - |
| CHEMBL2087072 | — | IC50 | > | 100000.0 | nM | - |