Assay Detail
Binding
CHEMBL3385711
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig cerebellum
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and structure-activity relationship of novel opioid κ receptor selective agonists: α-iminoamide derivatives with an azabicyclo[2.2.2]octene skeleton.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.54 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3339374 | — | — | 1 | 10.43 |
| CHEMBL3339378 | — | — | 1 | 10.37 |
| CHEMBL3339372 | — | — | 1 | 9.96 |
| CHEMBL3339379 | — | — | 1 | 9.92 |
| CHEMBL267495 | NALFURAFINE | 4.0 | 1 | 9.74 |
| CHEMBL3339381 | — | — | 1 | 9.74 |
| CHEMBL3339380 | — | — | 1 | 9.64 |
| CHEMBL3339377 | — | — | 1 | 9.42 |
| CHEMBL3339376 | — | — | 1 | 8.85 |
| CHEMBL3339375 | — | — | 1 | 8.81 |
| CHEMBL3339373 | — | — | 1 | 8.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3339374 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL3339378 | — | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL3339372 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL3339379 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL267495 | NALFURAFINE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL3339381 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL3339380 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3339377 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL3339376 | — | Ki | = | 1.42 | nM | 8.85 |
| CHEMBL3339375 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL3339373 | — | Ki | = | 7.74 | nM | 8.11 |