Assay Detail
Binding
CHEMBL759291
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Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| 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 |
|---|---|---|---|
| Ki | 26 | 6.82 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.66 |
| CHEMBL440765 | U-69593 | — | 1 | 8.32 |
| CHEMBL610262 | — | — | 1 | 8.22 |
| CHEMBL346173 | — | — | 1 | 8.06 |
| CHEMBL610522 | — | — | 1 | 7.75 |
| CHEMBL610261 | — | — | 1 | 7.70 |
| CHEMBL611687 | — | — | 1 | 7.18 |
| CHEMBL611436 | — | — | 1 | 7.12 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.12 |
| CHEMBL611688 | — | — | 1 | 7.11 |
| CHEMBL611432 | — | — | 1 | 7.09 |
| CHEMBL611431 | — | — | 1 | 7.04 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.73 |
| CHEMBL611435 | — | — | 1 | 6.58 |
| CHEMBL611437 | — | — | 1 | 6.56 |
| CHEMBL611434 | — | — | 1 | 6.44 |
| CHEMBL611685 | — | — | 1 | 6.39 |
| CHEMBL611433 | — | — | 1 | 6.37 |
| CHEMBL611438 | — | — | 1 | 6.33 |
| CHEMBL610260 | — | — | 1 | 6.27 |
| CHEMBL38874 | DAMGO | — | 1 | 5.24 |
| CHEMBL611428 | — | — | 1 | 5.19 |
| CHEMBL611686 | — | — | 1 | 5.13 |
| CHEMBL13470 | SNC-80 | — | 1 | 5.06 |
| CHEMBL611429 | — | — | 1 | - |
| CHEMBL611430 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL440765 | U-69593 | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL610262 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL346173 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL610522 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL610261 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL611687 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL611436 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL611688 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL611432 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL611431 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL70 | MORPHINE | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL611435 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL611437 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL611434 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL611685 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL611433 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL611438 | — | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL610260 | — | Ki | = | 539.0 | nM | 6.27 |
| CHEMBL38874 | DAMGO | Ki | = | 5820.0 | nM | 5.24 |
| CHEMBL611428 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL611686 | — | Ki | = | 7370.0 | nM | 5.13 |
| CHEMBL13470 | SNC-80 | Ki | = | 8760.0 | nM | 5.06 |
| CHEMBL611429 | — | Ki | > | 7100.0 | nM | - |
| CHEMBL611430 | — | Ki | > | 10000.0 | nM | - |