Assay Detail
Binding
CHEMBL3376270
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Displacement of [3H]U-69593 from kappa-opioid receptor in guinea pig brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Combination of cyclohexane and piperazine based κ-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.24 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094879 | — | — | 1 | 9.51 |
| CHEMBL290543 | — | — | 1 | 9.47 |
| CHEMBL440765 | U-69593 | — | 1 | 9.06 |
| CHEMBL3299004 | — | — | 1 | 8.68 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.16 |
| CHEMBL3299002 | — | — | 1 | 8.03 |
| CHEMBL3299005 | — | — | 1 | 8.01 |
| CHEMBL3298904 | — | — | 1 | 6.89 |
| CHEMBL3299003 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094879 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL290543 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL440765 | U-69593 | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL3299004 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL80 | NALOXONE | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL3299002 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3299005 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL3298904 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL3299003 | — | Ki | = | 435.0 | nM | 6.36 |