Assay Detail
Binding
CHEMBL753965
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Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 |
|---|---|---|---|
| Ki | 25 | 7.00 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346173 | — | — | 1 | 8.82 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.62 |
| CHEMBL38874 | DAMGO | — | 1 | 8.21 |
| CHEMBL611435 | — | — | 1 | 8.10 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.96 |
| CHEMBL611687 | — | — | 1 | 7.89 |
| CHEMBL610522 | — | — | 1 | 7.87 |
| CHEMBL611432 | — | — | 1 | 7.62 |
| CHEMBL611434 | — | — | 1 | 7.58 |
| CHEMBL610261 | — | — | 1 | 7.29 |
| CHEMBL610262 | — | — | 1 | 7.21 |
| CHEMBL611437 | — | — | 1 | 7.03 |
| CHEMBL611685 | — | — | 1 | 7.01 |
| CHEMBL611688 | — | — | 1 | 6.83 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 6.82 |
| CHEMBL611433 | — | — | 1 | 6.71 |
| CHEMBL611431 | — | — | 1 | 6.70 |
| CHEMBL611438 | — | — | 1 | 6.64 |
| CHEMBL611428 | — | — | 1 | 6.49 |
| CHEMBL611436 | — | — | 1 | 6.33 |
| CHEMBL611686 | — | — | 1 | 5.72 |
| CHEMBL610260 | — | — | 1 | 5.71 |
| CHEMBL611429 | — | — | 1 | 5.69 |
| CHEMBL440765 | U-69593 | — | 1 | 5.14 |
| CHEMBL13470 | SNC-80 | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346173 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL19019 | NALTREXONE | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL38874 | DAMGO | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL611435 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL70 | MORPHINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL611687 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL610522 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL611432 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL611434 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL610261 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL610262 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL611437 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL611685 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL611688 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL611433 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL611431 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL611438 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL611428 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL611436 | — | Ki | = | 467.0 | nM | 6.33 |
| CHEMBL611686 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL610260 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL611429 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL440765 | U-69593 | Ki | = | 7250.0 | nM | 5.14 |
| CHEMBL13470 | SNC-80 | Ki | = | 8070.0 | nM | 5.09 |