Assay Detail
Binding
CHEMBL754626
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Binding affinity towards Opioid receptor kappa 1 by displacing the radioligand [3H]U-69593 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 | 9 — Direct 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 | 9.13 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 10.28 |
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.28 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 10.14 |
| CHEMBL2113675 | — | — | 1 | 9.82 |
| CHEMBL1202427 | — | — | 1 | 9.74 |
| CHEMBL290543 | — | — | 1 | 9.44 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.21 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | — | 1 | 8.64 |
| CHEMBL1202425 | — | — | 1 | 7.62 |
| CHEMBL280958 | — | — | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.052 | nM | 10.28 |
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL2113675 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL1202427 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL290543 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1202425 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL280958 | — | Ki | = | 720.0 | nM | 6.14 |