Assay Detail
Binding
CHEMBL759234
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Binding affinity at mu opioid receptor 1 in rat brain membrane by [3H]DAMGO displacement.
20
Total Activities
20
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 | 20 | 6.67 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.89 |
| CHEMBL2113658 | — | — | 1 | 7.85 |
| CHEMBL2113645 | — | — | 1 | 7.83 |
| CHEMBL2113653 | — | — | 1 | 7.64 |
| CHEMBL2113652 | — | — | 1 | 7.52 |
| CHEMBL2113656 | — | — | 1 | 7.24 |
| CHEMBL2113660 | — | — | 1 | 6.97 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 6.77 |
| CHEMBL2113646 | — | — | 1 | 6.73 |
| CHEMBL2113655 | — | — | 1 | 6.62 |
| CHEMBL610798 | — | — | 1 | 6.47 |
| CHEMBL2113659 | — | — | 1 | 6.39 |
| CHEMBL608246 | — | — | 1 | 6.29 |
| CHEMBL2113647 | — | — | 1 | 6.26 |
| CHEMBL2113662 | — | — | 1 | 6.14 |
| CHEMBL2113657 | — | — | 1 | 6.06 |
| CHEMBL2113661 | — | — | 1 | 6.00 |
| CHEMBL2113663 | — | — | 1 | 5.91 |
| CHEMBL2113654 | — | — | 1 | 5.86 |
| CHEMBL2113651 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567175 | NALTRINDOLE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2113658 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2113645 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL2113653 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL2113652 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2113656 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2113660 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL2113646 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL2113655 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL610798 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL2113659 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL608246 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL2113647 | — | Ki | = | 555.0 | nM | 6.26 |
| CHEMBL2113662 | — | Ki | = | 731.0 | nM | 6.14 |
| CHEMBL2113657 | — | Ki | = | 869.0 | nM | 6.06 |
| CHEMBL2113661 | — | Ki | = | 1001.0 | nM | 6.00 |
| CHEMBL2113663 | — | Ki | = | 1231.0 | nM | 5.91 |
| CHEMBL2113654 | — | Ki | = | 1368.0 | nM | 5.86 |
| CHEMBL2113651 | — | Ki | = | 13978.0 | nM | 4.86 |