Assay Detail
Binding
CHEMBL754482
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Binding affinity at delta opioid receptor 1 in rat brain membrane by [3H]DADLE displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of 14-alkoxymorphinans. 17. Highly delta opioid receptor selective 14-alkoxy-substituted indolo- and benzofuromorphinans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.21 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 9.09 |
| CHEMBL2113646 | — | — | 1 | 8.93 |
| CHEMBL2113653 | — | — | 1 | 8.92 |
| CHEMBL2113645 | — | — | 1 | 8.89 |
| CHEMBL2113662 | — | — | 1 | 8.71 |
| CHEMBL2113654 | — | — | 1 | 8.59 |
| CHEMBL2113657 | — | — | 1 | 8.42 |
| CHEMBL608246 | — | — | 1 | 8.41 |
| CHEMBL2113656 | — | — | 1 | 8.40 |
| CHEMBL610798 | — | — | 1 | 8.36 |
| CHEMBL2113652 | — | — | 1 | 8.28 |
| CHEMBL2113647 | — | — | 1 | 8.28 |
| CHEMBL2113661 | — | — | 1 | 8.14 |
| CHEMBL2113660 | — | — | 1 | 7.94 |
| CHEMBL2113659 | — | — | 1 | 7.90 |
| CHEMBL2113655 | — | — | 1 | 7.89 |
| CHEMBL2113658 | — | — | 1 | 7.51 |
| CHEMBL2113663 | — | — | 1 | 6.82 |
| CHEMBL2113651 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL2113646 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL2113653 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2113645 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL2113662 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL2113654 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2113657 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL608246 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2113656 | — | Ki | = | 3.95 | nM | 8.40 |
| CHEMBL610798 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2113652 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2113647 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2113661 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2113660 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL2113659 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL2113655 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL2113658 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2113663 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL2113651 | — | Ki | = | 370.0 | nM | 6.43 |