Assay Detail
Binding
CHEMBL751119
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Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane
26
Total Activities
26
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 | 26 | 8.11 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346173 | — | — | 1 | 9.11 |
| CHEMBL610522 | — | — | 1 | 9.06 |
| CHEMBL611685 | — | — | 1 | 8.96 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.80 |
| CHEMBL611432 | — | — | 1 | 8.72 |
| CHEMBL610261 | — | — | 1 | 8.66 |
| CHEMBL610262 | — | — | 1 | 8.59 |
| CHEMBL611434 | — | — | 1 | 8.54 |
| CHEMBL611437 | — | — | 1 | 8.43 |
| CHEMBL611438 | — | — | 1 | 8.41 |
| CHEMBL611433 | — | — | 1 | 8.40 |
| CHEMBL611688 | — | — | 1 | 8.36 |
| CHEMBL611431 | — | — | 1 | 8.30 |
| CHEMBL13470 | SNC-80 | — | 1 | 8.25 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.12 |
| CHEMBL611687 | — | — | 1 | 8.10 |
| CHEMBL611436 | — | — | 1 | 8.09 |
| CHEMBL611435 | — | — | 1 | 7.75 |
| CHEMBL611429 | — | — | 1 | 7.68 |
| CHEMBL611686 | — | — | 1 | 7.64 |
| CHEMBL611430 | — | — | 1 | 7.47 |
| CHEMBL610260 | — | — | 1 | 7.39 |
| CHEMBL611428 | — | — | 1 | 6.84 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.80 |
| CHEMBL38874 | DAMGO | — | 1 | 6.33 |
| CHEMBL440765 | U-69593 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346173 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL610522 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL611685 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL611432 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL610261 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL610262 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL611434 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL611437 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL611438 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL611433 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL611688 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL611431 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL13470 | SNC-80 | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL19019 | NALTREXONE | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL611687 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL611436 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL611435 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL611429 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL611686 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL611430 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL610260 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL611428 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL70 | MORPHINE | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL38874 | DAMGO | Ki | = | 469.0 | nM | 6.33 |
| CHEMBL440765 | U-69593 | Ki | > | 5000.0 | nM | - |