Assay Detail
Functional
CHEMBL758125
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonistic activity towards Opioid receptor mu 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate; g = not active as an agonist
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.02 | 6.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL611685 | — | — | 1 | 6.65 |
| CHEMBL611688 | — | — | 1 | 6.05 |
| CHEMBL611437 | — | — | 1 | 5.88 |
| CHEMBL611431 | — | — | 1 | 5.49 |
| CHEMBL610261 | — | — | 1 | - |
| CHEMBL567175 | NALTRINDOLE | — | 1 | - |
| CHEMBL611438 | — | — | 1 | - |
| CHEMBL610262 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL611685 | — | EC50 | = | 225.0 | nM | 6.65 |
| CHEMBL611688 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL611437 | — | EC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL611431 | — | EC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL610261 | — | EC50 | - | nM | - | |
| CHEMBL567175 | NALTRINDOLE | EC50 | - | nM | - | |
| CHEMBL611438 | — | EC50 | - | — | - | |
| CHEMBL610262 | — | EC50 | - | nM | - |