Assay Detail
Binding
CHEMBL3239390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]deltorphin-2 from delta opioid receptor in Sprague-Dawley rat brain P2 synaptosomal membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Endomorphin analogues with mixed μ-opioid (MOP) receptor agonism/δ-opioid (DOP) receptor antagonism and lacking β-arrestin2 recruitment activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.50 | 8.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233196 | — | — | 1 | 8.79 |
| CHEMBL3233014 | — | — | 1 | 7.88 |
| CHEMBL3233192 | — | — | 1 | 7.63 |
| CHEMBL3233193 | — | — | 1 | 7.61 |
| CHEMBL365983 | — | — | 1 | 7.59 |
| CHEMBL3233200 | — | — | 1 | 7.48 |
| CHEMBL3233194 | — | — | 1 | 7.40 |
| CHEMBL3233191 | — | — | 1 | 7.29 |
| CHEMBL3233197 | — | — | 1 | 7.18 |
| CHEMBL3233199 | — | — | 1 | 7.17 |
| CHEMBL3233195 | — | — | 1 | 7.06 |
| CHEMBL3233198 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233196 | — | Ki | = | 1.63 | nM | 8.79 |
| CHEMBL3233014 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL3233192 | — | Ki | = | 23.2 | nM | 7.63 |
| CHEMBL3233193 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL365983 | — | Ki | = | 25.4 | nM | 7.59 |
| CHEMBL3233200 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3233194 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3233191 | — | Ki | = | 51.7 | nM | 7.29 |
| CHEMBL3233197 | — | Ki | = | 66.4 | nM | 7.18 |
| CHEMBL3233199 | — | Ki | = | 68.3 | nM | 7.17 |
| CHEMBL3233195 | — | Ki | = | 87.2 | nM | 7.06 |
| CHEMBL3233198 | — | Ki | = | 120.8 | nM | 6.92 |