Assay Detail
Binding
CHEMBL753838
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Binding affinity was measured by the displacement of [3H]- EK in guinea pig brain membrane of Opioid receptor kappa 1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design of peptidomimetic delta opioid receptor antagonists using the message-address concept.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.65 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610015 | — | — | 1 | 7.82 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.70 |
| CHEMBL610526 | — | — | 1 | 7.37 |
| CHEMBL477154 | — | — | 1 | 7.19 |
| CHEMBL606872 | — | — | 1 | 6.49 |
| CHEMBL610529 | — | — | 1 | 6.49 |
| CHEMBL610009 | — | — | 1 | 6.48 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 6.48 |
| CHEMBL609744 | — | — | 1 | 6.13 |
| CHEMBL2372782 | — | — | 1 | 5.65 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 5.35 |
| CHEMBL514693 | — | — | 1 | - |
| CHEMBL47029 | — | — | 1 | - |
| CHEMBL47545 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610015 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL19019 | NALTREXONE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL610526 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL477154 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL606872 | — | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL610529 | — | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL610009 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL609744 | — | Ki | = | 746.0 | nM | 6.13 |
| CHEMBL2372782 | — | Ki | = | 2218.0 | nM | 5.65 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 4467.0 | nM | 5.35 |
| CHEMBL514693 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL47029 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL47545 | — | Ki | > | 1000.0 | nM | - |