Assay Detail
Functional
CHEMBL756216
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Apparent antagonist activity determined by measuring the ability to inhibit stimulation of [35S]GTP-gamma-S, binding to opioid receptor delta 1 in guinea pig caudate membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 9 | 8.65 | 10.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 10.21 |
| CHEMBL610261 | — | — | 1 | 9.74 |
| CHEMBL611685 | — | — | 1 | 8.96 |
| CHEMBL610262 | — | — | 1 | 8.81 |
| CHEMBL611688 | — | — | 1 | 7.96 |
| CHEMBL611687 | — | — | 1 | 6.22 |
| CHEMBL611435 | — | — | 1 | - |
| CHEMBL611432 | — | — | 1 | - |
| CHEMBL611438 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL610261 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL611685 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL610262 | — | Ki | = | 1.56 | nM | 8.81 |
| CHEMBL611688 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL611687 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL611435 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL611432 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL611438 | — | Ki | = | 17.0 | — | - |