Assay Detail
Functional
CHEMBL911096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at rat mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
24
Total Activities
8
Compounds Tested
3
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
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 8 | - | - |
| IC50 | 8 | 7.57 | 8.90 |
| EC50 | 8 | 7.56 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL386186 | — | — | 3 | 8.90 |
| CHEMBL375359 | — | — | 3 | 8.73 |
| CHEMBL218651 | — | — | 3 | 8.11 |
| CHEMBL407198 | — | — | 3 | 8.02 |
| CHEMBL218600 | — | — | 3 | 7.77 |
| CHEMBL386212 | — | — | 3 | 7.13 |
| CHEMBL414087 | — | — | 3 | 6.69 |
| CHEMBL217957 | — | — | 3 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL386186 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL386186 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL375359 | — | IC50 | = | 1.862 | nM | 8.73 |
| CHEMBL375359 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL218651 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL218651 | — | IC50 | = | 7.762 | nM | 8.11 |
| CHEMBL407198 | — | IC50 | = | 9.55 | nM | 8.02 |
| CHEMBL218600 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL386212 | — | IC50 | = | 74.13 | nM | 7.13 |
| CHEMBL386212 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL407198 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL218600 | — | IC50 | = | 173.78 | nM | 6.76 |
| CHEMBL414087 | — | IC50 | = | 204.17 | nM | 6.69 |
| CHEMBL414087 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL217957 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL217957 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL218651 | — | Emax | = | 82.0 | % | - |
| CHEMBL217957 | — | Emax | = | 63.0 | % | - |
| CHEMBL386212 | — | Emax | = | 85.0 | % | - |
| CHEMBL218600 | — | Emax | = | 71.0 | % | - |
| CHEMBL386186 | — | Emax | = | 106.0 | % | - |
| CHEMBL375359 | — | Emax | = | 20.0 | % | - |
| CHEMBL407198 | — | Emax | = | 82.0 | % | - |
| CHEMBL414087 | — | Emax | = | 170.0 | % | - |