Assay Detail
Binding
CHEMBL757699
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Binding affinity for Opioid receptor mu 1 was determined by inhibition of binding of [3H]DAMGO (1.4-3 nM) to rat brain membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.27 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346173 | — | — | 1 | 8.82 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.60 |
| CHEMBL2112572 | — | — | 1 | 8.38 |
| CHEMBL2112575 | — | — | 1 | 8.22 |
| CHEMBL2112576 | — | — | 1 | 7.96 |
| CHEMBL610522 | — | — | 1 | 7.87 |
| CHEMBL2112571 | — | — | 1 | 7.66 |
| CHEMBL610261 | — | — | 1 | 7.29 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.00 |
| CHEMBL118487 | — | — | 1 | 6.81 |
| CHEMBL118479 | — | — | 1 | 6.72 |
| CHEMBL2112578 | — | — | 1 | 6.63 |
| CHEMBL333393 | — | — | 1 | 6.59 |
| CHEMBL2112573 | — | — | 1 | 6.51 |
| CHEMBL2112570 | — | — | 1 | 6.46 |
| CHEMBL2112568 | — | — | 1 | 6.19 |
| CHEMBL2112577 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346173 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL19019 | NALTREXONE | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2112572 | — | Ki | = | 4.15 | nM | 8.38 |
| CHEMBL2112575 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2112576 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL610522 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2112571 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL610261 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL118487 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL118479 | — | Ki | = | 191.0 | nM | 6.72 |
| CHEMBL2112578 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL333393 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL2112573 | — | Ki | = | 308.0 | nM | 6.51 |
| CHEMBL2112570 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL2112568 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL2112577 | — | Ki | = | 1167.0 | nM | 5.93 |