Assay Detail
Binding
CHEMBL5389261
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Antagonist activity at rat TRPM8 transfected in HEK293 cells assessed as inhibition of icilin induced increase in intracellular Ca2+ concentration preincubated for 5 mins followed by icilin stimulation by Fluo4-AM dye based assay
12
Total Activities
12
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
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich <i>Cannabis sativa</i> L. Chemotype IV.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.29 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497318 | CANNABIGEROL | 2.0 | 1 | 6.80 |
| CHEMBL5421918 | — | — | 1 | 6.10 |
| CHEMBL463843 | CANNABIGEROLIC ACID | — | 1 | 5.88 |
| CHEMBL4636830 | — | — | 1 | 5.52 |
| CHEMBL5433171 | — | — | 1 | 5.40 |
| CHEMBL5410813 | — | — | 1 | 5.28 |
| CHEMBL5424611 | — | — | 1 | 5.10 |
| CHEMBL5415604 | — | — | 1 | 4.98 |
| CHEMBL5437877 | — | — | 1 | 4.76 |
| CHEMBL5432734 | — | — | 1 | 4.62 |
| CHEMBL5404545 | — | — | 1 | 4.53 |
| CHEMBL5404503 | — | — | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497318 | CANNABIGEROL | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5421918 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL463843 | CANNABIGEROLIC ACID | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4636830 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5433171 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5410813 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL5424611 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5415604 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL5437877 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL5432734 | — | IC50 | = | 23900.0 | nM | 4.62 |
| CHEMBL5404545 | — | IC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL5404503 | — | IC50 | = | 33000.0 | nM | 4.48 |