Assay Detail
Functional
CHEMBL3636129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human kappa-opioid receptor expressed in CHO cell membrane assessed as [35S]GTPgammaS binding for 1 hr by liquid scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
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
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.54 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3634249 | — | — | 1 | 7.01 |
| CHEMBL3634257 | — | — | 1 | 6.75 |
| CHEMBL3634250 | — | — | 1 | 6.62 |
| CHEMBL3634258 | — | — | 1 | 6.47 |
| CHEMBL3634251 | — | — | 1 | 6.46 |
| CHEMBL2322568 | — | — | 1 | 6.27 |
| CHEMBL3634256 | — | — | 1 | 6.21 |
| CHEMBL3634247 | — | — | 1 | - |
| CHEMBL3634248 | — | — | 1 | - |
| CHEMBL2322562 | — | — | 1 | - |
| CHEMBL3634252 | — | — | 1 | - |
| CHEMBL3634253 | — | — | 1 | - |
| CHEMBL2322561 | — | — | 1 | - |
| CHEMBL3634254 | — | — | 1 | - |
| CHEMBL3634255 | — | — | 1 | - |
| CHEMBL2322563 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3634249 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3634257 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3634250 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3634258 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3634251 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2322568 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3634256 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3634247 | — | EC50 | > | 1300.0 | nM | - |
| CHEMBL3634248 | — | EC50 | - | — | - | |
| CHEMBL2322562 | — | EC50 | - | — | - | |
| CHEMBL3634252 | — | EC50 | - | — | - | |
| CHEMBL3634253 | — | EC50 | - | — | - | |
| CHEMBL2322561 | — | EC50 | - | — | - | |
| CHEMBL3634254 | — | EC50 | - | — | - | |
| CHEMBL3634255 | — | EC50 | - | — | - | |
| CHEMBL2322563 | — | EC50 | - | — | - |