Assay Detail
Binding
CHEMBL863625
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Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cells
15
Total Activities
15
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 | Expert |
Publication
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.63 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607125 | — | — | 1 | 9.64 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.40 |
| CHEMBL2113666 | — | — | 1 | 9.27 |
| CHEMBL607126 | — | — | 1 | 9.24 |
| CHEMBL386492 | CLOCINNAMOX | — | 1 | 8.85 |
| CHEMBL610883 | — | — | 1 | 8.82 |
| CHEMBL607018 | — | — | 1 | 8.82 |
| CHEMBL607017 | — | — | 1 | 8.64 |
| CHEMBL611402 | — | — | 1 | 8.62 |
| CHEMBL607016 | — | — | 1 | 8.60 |
| CHEMBL607068 | — | — | 1 | 8.26 |
| CHEMBL607069 | — | — | 1 | 8.19 |
| CHEMBL607127 | — | — | 1 | 8.00 |
| CHEMBL386272 | — | — | 1 | 7.79 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607125 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2113666 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL607126 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL386492 | CLOCINNAMOX | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL610883 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL607018 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL607017 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL611402 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL607016 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL607068 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL607069 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL607127 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL386272 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL70 | MORPHINE | Ki | = | 46.9 | nM | 7.33 |