Assay Detail
Functional
CHEMBL913686
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at mu opioid receptor assessed as increase in calcium level in CHO cells by aequorin luminescence based calcium assay
16
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 11 | - | - |
| EC50 | 5 | 8.26 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | — | 2 | 10.40 |
| CHEMBL375068 | — | — | 2 | 8.94 |
| CHEMBL219108 | — | — | 2 | 7.09 |
| CHEMBL267211 | — | — | 2 | 6.61 |
| CHEMBL316446 | ENDOMORPHIN-1 | — | 2 | - |
| CHEMBL218433 | — | — | 1 | - |
| CHEMBL254919 | — | — | 1 | - |
| CHEMBL385583 | — | — | 1 | - |
| CHEMBL375070 | — | — | 1 | - |
| CHEMBL375069 | — | — | 1 | - |
| CHEMBL80 | NALOXONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333357 | ENDOMORPHIN 2 | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL375068 | — | EC50 | = | 1.15 | nM | 8.94 |
| CHEMBL219108 | — | EC50 | = | 82.1 | nM | 7.09 |
| CHEMBL267211 | — | EC50 | = | 248.0 | nM | 6.61 |
| CHEMBL316446 | ENDOMORPHIN-1 | EC50 | = | 0.001 | nM | - |
| CHEMBL316446 | ENDOMORPHIN-1 | Activity | = | 86.05 | % | - |
| CHEMBL375068 | — | Activity | = | 64.05 | % | - |
| CHEMBL267211 | — | Activity | = | 34.07 | % | - |
| CHEMBL219108 | — | Activity | = | 58.67 | % | - |
| CHEMBL218433 | — | Activity | = | 22.36 | % | - |
| CHEMBL333357 | ENDOMORPHIN 2 | Activity | = | 85.89 | % | - |
| CHEMBL254919 | — | Activity | = | 22.87 | % | - |
| CHEMBL385583 | — | Activity | = | 46.45 | % | - |
| CHEMBL375070 | — | Activity | = | 35.75 | % | - |
| CHEMBL375069 | — | Activity | = | 6.74 | % | - |
| CHEMBL80 | NALOXONE | Activity | = | 0.1 | % | - |