Assay Detail
Binding
CHEMBL3239388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from mu 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 | 9.35 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233014 | — | — | 1 | 9.89 |
| CHEMBL3233200 | — | — | 1 | 9.82 |
| CHEMBL3233197 | — | — | 1 | 9.68 |
| CHEMBL3233191 | — | — | 1 | 9.55 |
| CHEMBL3233195 | — | — | 1 | 9.55 |
| CHEMBL3233194 | — | — | 1 | 9.51 |
| CHEMBL365983 | — | — | 1 | 9.47 |
| CHEMBL3233193 | — | — | 1 | 9.43 |
| CHEMBL3233196 | — | — | 1 | 9.33 |
| CHEMBL3233198 | — | — | 1 | 9.15 |
| CHEMBL3233192 | — | — | 1 | 9.09 |
| CHEMBL3233199 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233014 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL3233200 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3233197 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3233191 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3233195 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL3233194 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL365983 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3233193 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL3233196 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL3233198 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3233192 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL3233199 | — | Ki | = | 16.9 | nM | 7.77 |