Assay Detail
Binding
CHEMBL751216
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Opioid receptor mu 1 by displacing the radioligand [3H]DAMGO 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 | 8.80 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113675 | — | — | 1 | 11.00 |
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.04 |
| CHEMBL56585 | CYCLAZOCINE | 2.0 | 1 | 10.00 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 9.92 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | — | 1 | 9.68 |
| CHEMBL1202427 | — | — | 1 | 9.42 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.11 |
| CHEMBL290543 | — | — | 1 | 6.66 |
| CHEMBL1202425 | — | — | 1 | 6.62 |
| CHEMBL280958 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113675 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.092 | nM | 10.04 |
| CHEMBL56585 | CYCLAZOCINE | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1628243 | LEVORPHANOL HYDROCHLORIDE | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL1202427 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL290543 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1202425 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL280958 | — | Ki | = | 2900.0 | nM | 5.54 |