Assay Detail
Binding
CHEMBL2318810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum after 1 hr by liquid scintillation counting analysis
9
Total Activities
9
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
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.10 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | 4.0 | 1 | 9.75 |
| CHEMBL2315360 | — | — | 1 | 9.48 |
| CHEMBL2315358 | — | — | 1 | 9.29 |
| CHEMBL2315359 | — | — | 1 | 9.23 |
| CHEMBL2315361 | — | — | 1 | 9.20 |
| CHEMBL2315362 | — | — | 1 | 9.13 |
| CHEMBL440765 | U-69593 | — | 1 | 8.86 |
| CHEMBL2315357 | — | — | 1 | 8.66 |
| CHEMBL2315356 | — | — | 1 | 8.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490665 | NALFURAFINE HYDROCHLORIDE | Ki | = | 0.178 | nM | 9.75 |
| CHEMBL2315360 | — | Ki | = | 0.3283 | nM | 9.48 |
| CHEMBL2315358 | — | Ki | = | 0.507 | nM | 9.29 |
| CHEMBL2315359 | — | Ki | = | 0.5895 | nM | 9.23 |
| CHEMBL2315361 | — | Ki | = | 0.6252 | nM | 9.20 |
| CHEMBL2315362 | — | Ki | = | 0.7346 | nM | 9.13 |
| CHEMBL440765 | U-69593 | Ki | = | 1.37 | nM | 8.86 |
| CHEMBL2315357 | — | Ki | = | 2.192 | nM | 8.66 |
| CHEMBL2315356 | — | Ki | = | 4.584 | nM | 8.34 |