Assay Detail
Binding
CHEMBL757490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested for inhibitory effect on binding of [3H]DAMGO to opioid receptor mu in guinea pig cerebellum membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.65 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384584 | — | — | 1 | 9.62 |
| CHEMBL425806 | — | — | 1 | 8.02 |
| CHEMBL265387 | — | — | 1 | 7.96 |
| CHEMBL407529 | — | — | 1 | 7.51 |
| CHEMBL413160 | — | — | 1 | 7.50 |
| CHEMBL290543 | — | — | 1 | 6.69 |
| CHEMBL440765 | U-69593 | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384584 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL425806 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL265387 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL407529 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL413160 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL290543 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL440765 | U-69593 | Ki | = | 551.0 | nM | 6.26 |