Assay Detail
Binding
CHEMBL756052
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Binding affinity for Opioid receptor kappa 1 was determined by inhibition of binding of [3H]U-69593 (1.2-2.2 nM) to guinea pig brain membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.06 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112572 | — | — | 1 | 8.21 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.15 |
| CHEMBL346173 | — | — | 1 | 8.06 |
| CHEMBL2112571 | — | — | 1 | 7.96 |
| CHEMBL610522 | — | — | 1 | 7.75 |
| CHEMBL2112576 | — | — | 1 | 7.74 |
| CHEMBL610261 | — | — | 1 | 7.70 |
| CHEMBL2112575 | — | — | 1 | 7.60 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.45 |
| CHEMBL2112570 | — | — | 1 | 6.67 |
| CHEMBL118479 | — | — | 1 | 6.58 |
| CHEMBL2112573 | — | — | 1 | 6.57 |
| CHEMBL333393 | — | — | 1 | 6.25 |
| CHEMBL118487 | — | — | 1 | 6.17 |
| CHEMBL2112578 | — | — | 1 | 5.90 |
| CHEMBL2112568 | — | — | 1 | 5.67 |
| CHEMBL2112577 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112572 | — | Ki | = | 6.24 | nM | 8.21 |
| CHEMBL19019 | NALTREXONE | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL346173 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL2112571 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL610522 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL2112576 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL610261 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2112575 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL2112570 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL118479 | — | Ki | = | 264.0 | nM | 6.58 |
| CHEMBL2112573 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL333393 | — | Ki | = | 565.0 | nM | 6.25 |
| CHEMBL118487 | — | Ki | = | 677.0 | nM | 6.17 |
| CHEMBL2112578 | — | Ki | = | 1269.0 | nM | 5.90 |
| CHEMBL2112568 | — | Ki | = | 2116.0 | nM | 5.67 |
| CHEMBL2112577 | — | Ki | = | 2539.0 | nM | 5.59 |