Assay Detail
Binding
CHEMBL751218
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Binding affinity towards Opioid receptor mu 1 in guinea pig brain membranes using [3H]DAMGO as radioligand
29
Total Activities
29
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 | 29 | 9.08 | 10.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 10.04 |
| CHEMBL90667 | — | — | 1 | 9.96 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 9.92 |
| CHEMBL327576 | — | — | 1 | 9.92 |
| CHEMBL327935 | — | — | 1 | 9.80 |
| CHEMBL419511 | — | — | 1 | 9.74 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 1 | 9.68 |
| CHEMBL90463 | — | — | 1 | 9.59 |
| CHEMBL327885 | — | — | 1 | 9.57 |
| CHEMBL91231 | — | — | 1 | 9.55 |
| CHEMBL93731 | — | — | 1 | 9.48 |
| CHEMBL328269 | — | — | 1 | 9.47 |
| CHEMBL2114257 | — | — | 1 | 9.38 |
| CHEMBL430833 | — | — | 1 | 9.37 |
| CHEMBL420995 | — | — | 1 | 9.27 |
| CHEMBL328236 | — | — | 1 | 9.27 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | — | 1 | 9.11 |
| CHEMBL92774 | — | — | 1 | 9.04 |
| CHEMBL327309 | — | — | 1 | 9.02 |
| CHEMBL329020 | — | — | 1 | 8.82 |
| CHEMBL314294 | — | — | 1 | 8.64 |
| CHEMBL90305 | — | — | 1 | 8.39 |
| CHEMBL327490 | — | — | 1 | 8.38 |
| CHEMBL329453 | — | — | 1 | 7.75 |
| CHEMBL96785 | — | — | 1 | 7.70 |
| CHEMBL92349 | — | — | 1 | 7.68 |
| CHEMBL290543 | — | — | 1 | 6.66 |
| CHEMBL2115245 | — | — | 1 | - |
| CHEMBL1790045 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | Ki | = | 0.092 | nM | 10.04 |
| CHEMBL90667 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL301160 | BUTORPHAN | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL327576 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL327935 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL419511 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL592 | LEVORPHANOL | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL90463 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL327885 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL91231 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL93731 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL328269 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL2114257 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL430833 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL420995 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL328236 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL279968 | ETHYLKETOCYCLAZOCINE | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL92774 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL327309 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL329020 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL314294 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL90305 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL327490 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL329453 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL96785 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL92349 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL290543 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL2115245 | — | Ki | = | 0.0048 | nM | - |
| CHEMBL1790045 | — | Ki | = | 0.0032 | nM | - |