Assay Detail
Binding
CHEMBL5133576
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Displacement of [3H]U-69-593 from human DOR expressed in HEK293 cell membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Effect of removal of the 14-hydroxy group on the affinity of the 4,5-epoxymorphinan derivatives for orexin and opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.68 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5185211 | — | — | 1 | 8.01 |
| CHEMBL5188658 | — | — | 1 | 7.58 |
| CHEMBL267495 | NALFURAFINE | 4.0 | 1 | 7.44 |
| CHEMBL5204400 | — | — | 1 | - |
| CHEMBL5181937 | — | — | 1 | - |
| CHEMBL5186673 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5185211 | — | Ki | = | 9.76 | nM | 8.01 |
| CHEMBL5188658 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL267495 | NALFURAFINE | Ki | = | 36.5 | nM | 7.44 |
| CHEMBL5204400 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5181937 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5186673 | — | Ki | > | 10000.0 | nM | - |