Assay Detail
Functional
CHEMBL973308
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Antagonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of DAMGO-stimulated [35S]GTPgammaS binding
6
Total Activities
3
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 | Autocuration |
Publication
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.04 | 7.55 |
| Imax | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL469189 | — | — | 2 | 7.55 |
| CHEMBL522375 | — | — | 2 | 7.51 |
| CHEMBL493621 | — | — | 2 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL469189 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL522375 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL493621 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL469189 | — | Imax | = | 88.0 | % | - |
| CHEMBL493621 | — | Imax | = | 69.0 | % | - |
| CHEMBL522375 | — | Imax | = | 93.0 | % | - |