Assay Detail
Binding
CHEMBL758174
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Binding affinity towards Opioid receptor delta 1 by displacing the radioligand [3H]naltrindole from guinea pig brain membrane
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.40 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 9.66 |
| CHEMBL2113675 | — | — | 1 | 9.57 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 9.24 |
| CHEMBL1202427 | — | — | 1 | 9.00 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 8.89 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 8.47 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | — | 1 | 8.38 |
| CHEMBL1202425 | — | — | 1 | 6.82 |
| CHEMBL290543 | — | — | 1 | 5.60 |
| CHEMBL280958 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL2113675 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1202427 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1202425 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL290543 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL280958 | — | Ki | > | 100000.0 | nM | - |