Assay Detail
Binding
CHEMBL5144872
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Displacement of [3H]-U-69593 from recombinant human KOR expressed in CHO cell membranes measured after 2 hrs by microbeta scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.32 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485583 | — | — | 1 | 9.89 |
| CHEMBL5186730 | — | — | 1 | 9.85 |
| CHEMBL5178511 | — | — | 1 | 9.71 |
| CHEMBL5200218 | — | — | 1 | 9.71 |
| CHEMBL5200050 | — | — | 1 | 9.59 |
| CHEMBL5185996 | — | — | 1 | 9.56 |
| CHEMBL5200992 | — | — | 1 | 9.48 |
| CHEMBL5175717 | — | — | 1 | 8.77 |
| CHEMBL5170301 | — | — | 1 | 8.63 |
| CHEMBL5208385 | — | — | 1 | 7.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485583 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL5186730 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL5178511 | — | Ki | = | 0.193 | nM | 9.71 |
| CHEMBL5200218 | — | Ki | = | 0.197 | nM | 9.71 |
| CHEMBL5200050 | — | Ki | = | 0.256 | nM | 9.59 |
| CHEMBL5185996 | — | Ki | = | 0.278 | nM | 9.56 |
| CHEMBL5200992 | — | Ki | = | 0.332 | nM | 9.48 |
| CHEMBL5175717 | — | Ki | = | 1.71 | nM | 8.77 |
| CHEMBL5170301 | — | Ki | = | 2.36 | nM | 8.63 |
| CHEMBL5208385 | — | Ki | = | 10.6 | nM | 7.97 |