Assay Detail
Functional
CHEMBL861291
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [35S]GTP-gamma-S binding to rat mu opioid receptor expressed in CHO cells
30
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 7.72 | 9.19 |
| Emax | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374325 | — | — | 3 | 9.19 |
| CHEMBL408889 | — | — | 3 | 8.29 |
| CHEMBL405192 | — | — | 3 | 8.02 |
| CHEMBL375412 | — | — | 3 | 8.02 |
| CHEMBL408832 | — | — | 3 | 8.00 |
| CHEMBL412331 | — | — | 3 | 7.84 |
| CHEMBL38874 | DAMGO | — | 3 | 7.44 |
| CHEMBL442483 | — | — | 3 | 7.12 |
| CHEMBL413644 | — | — | 3 | 6.69 |
| CHEMBL438739 | — | — | 3 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374325 | — | EC50 | = | 0.6457 | nM | 9.19 |
| CHEMBL374325 | — | EC50 | = | 0.64 | nM | 9.19 |
| CHEMBL408889 | — | EC50 | = | 5.129 | nM | 8.29 |
| CHEMBL408889 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL405192 | — | EC50 | = | 9.55 | nM | 8.02 |
| CHEMBL405192 | — | EC50 | = | 9.5 | nM | 8.02 |
| CHEMBL375412 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL375412 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL408832 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL408832 | — | EC50 | = | 10.47 | nM | 7.98 |
| CHEMBL412331 | — | EC50 | = | 14.45 | nM | 7.84 |
| CHEMBL412331 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL38874 | DAMGO | EC50 | = | 36.31 | nM | 7.44 |
| CHEMBL38874 | DAMGO | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL442483 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL442483 | — | EC50 | = | 75.86 | nM | 7.12 |
| CHEMBL413644 | — | EC50 | = | 204.17 | nM | 6.69 |
| CHEMBL413644 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL438739 | — | EC50 | = | 239.88 | nM | 6.62 |
| CHEMBL438739 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL442483 | — | Emax | = | 90.0 | % | - |
| CHEMBL374325 | — | Emax | = | 130.0 | % | - |
| CHEMBL405192 | — | Emax | = | 83.0 | % | - |
| CHEMBL408889 | — | Emax | = | 84.0 | % | - |
| CHEMBL412331 | — | Emax | = | 33.0 | % | - |
| CHEMBL375412 | — | Emax | = | 82.0 | % | - |
| CHEMBL438739 | — | Emax | = | 60.0 | % | - |
| CHEMBL38874 | DAMGO | Emax | = | 150.0 | % | - |
| CHEMBL413644 | — | Emax | = | 170.0 | % | - |
| CHEMBL408832 | — | Emax | = | 103.0 | % | - |