Assay Detail
Binding
CHEMBL753845
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Compound was evaluated for binding affinity towards kappa opioid receptor using [3H](-)-U-69,593 in guinea pig ileum
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Alterations in the stereochemistry of the kappa-selective opioid agonist U50,488 result in high-affinity sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 6.98 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58033 | (-)-U-50488 | — | 1 | 9.05 |
| CHEMBL60547 | — | — | 1 | 6.78 |
| CHEMBL290543 | — | — | 1 | 6.52 |
| CHEMBL301867 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58033 | (-)-U-50488 | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL60547 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL290543 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL301867 | — | Ki | = | 2715.0 | nM | 5.57 |