Assay Detail
Binding
CHEMBL754204
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Binding affinity determined by displacing [3H]DAMGO from Opioid receptor mu 1 in rat brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of 14-alkoxymorphinans. 21. Novel 4-alkoxy and 14-phenylpropoxy derivatives of the mu opioid receptor antagonist cyprodime.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.18 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL110640 | — | — | 1 | 6.47 |
| CHEMBL325347 | — | — | 1 | 6.40 |
| CHEMBL321170 | — | — | 1 | 6.08 |
| CHEMBL322796 | CYPRODIME | — | 1 | 4.97 |
| CHEMBL109741 | — | — | 1 | 4.94 |
| CHEMBL326860 | — | — | 1 | 4.86 |
| CHEMBL109441 | — | — | 1 | 4.83 |
| CHEMBL109786 | — | — | 1 | 4.55 |
| CHEMBL409832 | — | — | 1 | 4.36 |
| CHEMBL322738 | — | — | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL110640 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL325347 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL321170 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL322796 | CYPRODIME | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL109741 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL326860 | — | Ki | = | 13800.0 | nM | 4.86 |
| CHEMBL109441 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL109786 | — | Ki | = | 27900.0 | nM | 4.55 |
| CHEMBL409832 | — | Ki | = | 43300.0 | nM | 4.36 |
| CHEMBL322738 | — | Ki | = | 44900.0 | nM | 4.35 |