Assay Detail
Binding
CHEMBL3239393
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 |
|---|---|---|---|
| IC50 | 14 | 7.85 | 9.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233200 | — | — | 1 | 9.56 |
| CHEMBL120758 | — | — | 1 | 8.63 |
| CHEMBL3233014 | — | — | 1 | 8.57 |
| CHEMBL3233198 | — | — | 1 | 8.33 |
| CHEMBL3233196 | — | — | 1 | 8.03 |
| CHEMBL3233197 | — | — | 1 | 7.98 |
| CHEMBL340032 | DADLE | — | 1 | 7.87 |
| CHEMBL3233191 | — | — | 1 | 7.84 |
| CHEMBL3233192 | — | — | 1 | 7.40 |
| CHEMBL3233195 | — | — | 1 | 7.35 |
| CHEMBL3233193 | — | — | 1 | 7.18 |
| CHEMBL365983 | — | — | 1 | 6.68 |
| CHEMBL3233194 | — | — | 1 | 6.60 |
| CHEMBL3233199 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233200 | — | IC50 | = | 0.274 | nM | 9.56 |
| CHEMBL120758 | — | IC50 | = | 2.33 | nM | 8.63 |
| CHEMBL3233014 | — | IC50 | = | 2.68 | nM | 8.57 |
| CHEMBL3233198 | — | IC50 | = | 4.63 | nM | 8.33 |
| CHEMBL3233196 | — | IC50 | = | 9.28 | nM | 8.03 |
| CHEMBL3233197 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL340032 | DADLE | IC50 | = | 13.39 | nM | 7.87 |
| CHEMBL3233191 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL3233192 | — | IC50 | = | 40.2 | nM | 7.40 |
| CHEMBL3233195 | — | IC50 | = | 44.6 | nM | 7.35 |
| CHEMBL3233193 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL365983 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3233194 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL3233199 | — | IC50 | > | 10000.0 | nM | - |