Assay Detail
Binding
CHEMBL1022992
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Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.78 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.70 |
| CHEMBL514774 | — | — | 1 | 9.47 |
| CHEMBL474755 | — | — | 1 | 8.60 |
| CHEMBL386492 | CLOCINNAMOX | — | 1 | 8.52 |
| CHEMBL512526 | — | — | 1 | 8.46 |
| CHEMBL471543 | — | — | 1 | 8.38 |
| CHEMBL386272 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL514774 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL474755 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL386492 | CLOCINNAMOX | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL512526 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL471543 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL386272 | — | Ki | = | 4.8 | nM | 8.32 |