Assay Detail
Functional
CHEMBL3370190
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 5.85 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.00 |
| CHEMBL3325716 | — | — | 1 | 7.39 |
| CHEMBL3325715 | — | — | 1 | 7.39 |
| CHEMBL3325714 | — | — | 1 | 7.39 |
| CHEMBL3325841 | — | — | 1 | 7.00 |
| CHEMBL3325713 | — | — | 1 | 6.82 |
| CHEMBL3325719 | — | — | 1 | 6.43 |
| CHEMBL3325707 | — | — | 1 | 6.43 |
| CHEMBL3325710 | — | — | 1 | 6.43 |
| CHEMBL3325700 | — | — | 1 | 5.95 |
| CHEMBL3325718 | — | — | 1 | 5.81 |
| CHEMBL3325696 | — | — | 1 | 5.64 |
| CHEMBL3325712 | — | — | 1 | 5.54 |
| CHEMBL3325702 | — | — | 1 | 5.33 |
| CHEMBL3325708 | — | — | 1 | 5.05 |
| CHEMBL3325709 | — | — | 1 | 5.00 |
| CHEMBL3325706 | — | — | 1 | 5.00 |
| CHEMBL3325701 | — | — | 1 | 5.00 |
| CHEMBL3325711 | — | — | 1 | 4.99 |
| CHEMBL3325717 | — | — | 1 | 4.87 |
| CHEMBL3325699 | — | — | 1 | 4.87 |
| CHEMBL3325704 | — | — | 1 | 4.74 |
| CHEMBL3325703 | — | — | 1 | 4.72 |
| CHEMBL3325705 | — | — | 1 | 4.52 |
| CHEMBL3325698 | — | — | 1 | - |
| CHEMBL3325697 | — | — | 1 | - |
| CHEMBL594957 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70 | MORPHINE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3325716 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3325715 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3325714 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3325841 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3325713 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3325719 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3325707 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3325710 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3325700 | — | EC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL3325718 | — | EC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL3325696 | — | EC50 | = | 2280.0 | nM | 5.64 |
| CHEMBL3325712 | — | EC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL3325702 | — | EC50 | = | 4720.0 | nM | 5.33 |
| CHEMBL3325708 | — | EC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL3325709 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3325706 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3325701 | — | EC50 | = | 9910.0 | nM | 5.00 |
| CHEMBL3325711 | — | EC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL3325717 | — | EC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL3325699 | — | EC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL3325704 | — | EC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL3325703 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3325705 | — | EC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL3325698 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL3325697 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL594957 | — | EC50 | > | 100000.0 | nM | - |