Assay Detail
ADMET
CHEMBL3239402
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Agonist activity at GFP-fused mu opioid receptor (unknown origin) expressed in HEK293 cells assessed as recruitment of beta-arrestin-2 after 10 mins by BRET assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 14 | 7.06 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233197 | — | — | 1 | 8.20 |
| CHEMBL3233014 | — | — | 1 | 7.73 |
| CHEMBL38874 | DAMGO | — | 1 | 6.42 |
| CHEMBL340032 | DADLE | — | 1 | 5.89 |
| CHEMBL365983 | — | — | 1 | - |
| CHEMBL3233191 | — | — | 1 | - |
| CHEMBL3233192 | — | — | 1 | - |
| CHEMBL3233193 | — | — | 1 | - |
| CHEMBL3233194 | — | — | 1 | - |
| CHEMBL3233195 | — | — | 1 | - |
| CHEMBL3233196 | — | — | 1 | - |
| CHEMBL3233198 | — | — | 1 | - |
| CHEMBL3233199 | — | — | 1 | - |
| CHEMBL3233200 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233197 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3233014 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL38874 | DAMGO | EC50 | = | 378.0 | nM | 6.42 |
| CHEMBL340032 | DADLE | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL365983 | — | EC50 | - | — | - | |
| CHEMBL3233191 | — | EC50 | - | — | - | |
| CHEMBL3233192 | — | EC50 | - | — | - | |
| CHEMBL3233193 | — | EC50 | - | — | - | |
| CHEMBL3233194 | — | EC50 | - | — | - | |
| CHEMBL3233195 | — | EC50 | - | — | - | |
| CHEMBL3233196 | — | EC50 | - | — | - | |
| CHEMBL3233198 | — | EC50 | - | — | - | |
| CHEMBL3233199 | — | EC50 | - | — | - | |
| CHEMBL3233200 | — | EC50 | - | — | - |