Assay Detail
Functional
CHEMBL973311
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Antagonist activity at human kappa opioid receptor expressed in CHO cells assessed as inhibition of U50,488-stimulated [35S]GTPgammaS binding
4
Total Activities
3
Compounds Tested
3
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 |
|---|---|---|---|
| Activity | 2 | - | - |
| IC50 | 1 | 5.89 | 5.89 |
| Imax | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL469189 | — | — | 2 | 5.89 |
| CHEMBL493621 | — | — | 1 | - |
| CHEMBL522375 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL469189 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL493621 | — | Activity | - | — | - | |
| CHEMBL522375 | — | Activity | - | — | - | |
| CHEMBL469189 | — | Imax | = | 75.0 | % | - |