Assay Detail
Toxicity
CHEMBL5144875
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Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.22 | 8.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5186730 | — | — | 1 | 8.56 |
| CHEMBL38874 | DAMGO | — | 1 | 8.45 |
| CHEMBL5200050 | — | — | 1 | 8.33 |
| CHEMBL5175717 | — | — | 1 | 8.27 |
| CHEMBL5200992 | — | — | 1 | 8.25 |
| CHEMBL5185996 | — | — | 1 | 8.15 |
| CHEMBL5178511 | — | — | 1 | 8.03 |
| CHEMBL5170301 | — | — | 1 | 8.03 |
| CHEMBL5200218 | — | — | 1 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5186730 | — | EC50 | = | 2.72 | nM | 8.56 |
| CHEMBL38874 | DAMGO | EC50 | = | 3.59 | nM | 8.45 |
| CHEMBL5200050 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5175717 | — | EC50 | = | 5.37 | nM | 8.27 |
| CHEMBL5200992 | — | EC50 | = | 5.61 | nM | 8.25 |
| CHEMBL5185996 | — | EC50 | = | 7.11 | nM | 8.15 |
| CHEMBL5178511 | — | EC50 | = | 9.43 | nM | 8.03 |
| CHEMBL5170301 | — | EC50 | = | 9.35 | nM | 8.03 |
| CHEMBL5200218 | — | EC50 | = | 12.7 | nM | 7.90 |