Assay Detail
Binding
CHEMBL757482
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Binding affinity was measured by the displacement of [3H]- DAMGO in guinea pig brain membrane of opioid receptor mu
11
Total Activities
11
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 | 11 | 7.55 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.10 |
| CHEMBL610015 | — | — | 1 | 8.77 |
| CHEMBL477154 | — | — | 1 | 7.85 |
| CHEMBL610526 | — | — | 1 | 7.80 |
| CHEMBL609744 | — | — | 1 | 7.55 |
| CHEMBL610009 | — | — | 1 | 7.54 |
| CHEMBL610529 | — | — | 1 | 7.31 |
| CHEMBL606872 | — | — | 1 | 6.98 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 6.33 |
| CHEMBL514693 | — | — | 1 | 6.26 |
| CHEMBL47545 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL610015 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL477154 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL610526 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL609744 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL610009 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL610529 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL606872 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL514693 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL47545 | — | Ki | > | 1000.0 | nM | - |