Assay Detail
Functional
CHEMBL870418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
10
Total Activities
3
Compounds Tested
5
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
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Emax | 3 | - | - |
| EC50 | 2 | 8.48 | 8.52 |
| Imax | 2 | - | - |
| IC50 | 2 | 7.25 | 7.68 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL210005 | — | — | 2 | 8.52 |
| CHEMBL58646 | — | — | 4 | 8.43 |
| CHEMBL377789 | — | — | 4 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL210005 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL58646 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL58646 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL377789 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL377789 | — | Activity | - | — | - | |
| CHEMBL58646 | — | Emax | = | 27.0 | % | - |
| CHEMBL58646 | — | Imax | = | 79.0 | % | - |
| CHEMBL377789 | — | Emax | = | 5.6 | % | - |
| CHEMBL377789 | — | Imax | = | 99.0 | % | - |
| CHEMBL210005 | — | Emax | = | 55.0 | % | - |