Assay Detail
Binding
CHEMBL759364
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Binding affinity for Opioid receptor delta 1 was determined by inhibition of binding of [3H]DADLE (1.3-2.0 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 | 7.71 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 9.39 |
| CHEMBL346173 | — | — | 1 | 9.11 |
| CHEMBL610522 | — | — | 1 | 9.06 |
| CHEMBL2112576 | — | — | 1 | 8.75 |
| CHEMBL610261 | — | — | 1 | 8.66 |
| CHEMBL2112572 | — | — | 1 | 8.46 |
| CHEMBL2112571 | — | — | 1 | 7.80 |
| CHEMBL2112575 | — | — | 1 | 7.64 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.40 |
| CHEMBL118479 | — | — | 1 | 7.14 |
| CHEMBL2112573 | — | — | 1 | 7.14 |
| CHEMBL2112568 | — | — | 1 | 7.07 |
| CHEMBL2112578 | — | — | 1 | 7.00 |
| CHEMBL118487 | — | — | 1 | 6.90 |
| CHEMBL2112570 | — | — | 1 | 6.64 |
| CHEMBL333393 | — | — | 1 | 6.49 |
| CHEMBL2112577 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL346173 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL610522 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL2112576 | — | Ki | = | 1.76 | nM | 8.75 |
| CHEMBL610261 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL2112572 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL2112571 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2112575 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL19019 | NALTREXONE | Ki | = | 39.5 | nM | 7.40 |
| CHEMBL118479 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2112573 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2112568 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2112578 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL118487 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL2112570 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL333393 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL2112577 | — | Ki | = | 344.0 | nM | 6.46 |