Assay Detail
Binding
CHEMBL754627
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Binding affinity towards Opioid receptor kappa 1 in guinea pig brain membranes using [3H]U-69593 as radioligand
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 | Intermediate |
Publication
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.56 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.28 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 10.15 |
| CHEMBL419511 | — | — | 1 | 10.08 |
| CHEMBL420995 | — | — | 1 | 9.80 |
| CHEMBL327309 | — | — | 1 | 9.68 |
| CHEMBL90463 | — | — | 1 | 9.48 |
| CHEMBL290543 | — | — | 1 | 9.44 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.21 |
| CHEMBL329453 | — | — | 1 | 8.82 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 8.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL419511 | — | Ki | = | 0.083 | nM | 10.08 |
| CHEMBL420995 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL327309 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL90463 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL290543 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL329453 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 2.3 | nM | 8.64 |