Assay Detail
Binding
CHEMBL754453
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Binding affinity at kappa opioid receptor 1 in guinea pig brain by [3H]U-69593 displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 6.55 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113645 | — | — | 1 | 8.51 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.80 |
| CHEMBL2113653 | — | — | 1 | 7.17 |
| CHEMBL2113646 | — | — | 1 | 7.03 |
| CHEMBL2113660 | — | — | 1 | 6.94 |
| CHEMBL610798 | — | — | 1 | 6.87 |
| CHEMBL2113662 | — | — | 1 | 6.83 |
| CHEMBL2113657 | — | — | 1 | 6.63 |
| CHEMBL2113654 | — | — | 1 | 6.46 |
| CHEMBL2113659 | — | — | 1 | 6.42 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 6.40 |
| CHEMBL2113647 | — | — | 1 | 6.30 |
| CHEMBL2113652 | — | — | 1 | 6.25 |
| CHEMBL608246 | — | — | 1 | 6.14 |
| CHEMBL2113661 | — | — | 1 | 6.12 |
| CHEMBL2113655 | — | — | 1 | 5.90 |
| CHEMBL2113656 | — | — | 1 | 5.82 |
| CHEMBL2113651 | — | — | 1 | 5.49 |
| CHEMBL2113658 | — | — | 1 | 5.44 |
| CHEMBL2113663 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113645 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL2113653 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2113646 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2113660 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL610798 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL2113662 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL2113657 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL2113654 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL2113659 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 395.0 | nM | 6.40 |
| CHEMBL2113647 | — | Ki | = | 504.0 | nM | 6.30 |
| CHEMBL2113652 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL608246 | — | Ki | = | 725.0 | nM | 6.14 |
| CHEMBL2113661 | — | Ki | = | 763.0 | nM | 6.12 |
| CHEMBL2113655 | — | Ki | = | 1263.0 | nM | 5.90 |
| CHEMBL2113656 | — | Ki | = | 1527.0 | nM | 5.82 |
| CHEMBL2113651 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL2113658 | — | Ki | = | 3639.0 | nM | 5.44 |
| CHEMBL2113663 | — | Ki | = | 721429.0 | nM | - |