Assay Detail
Binding
CHEMBL4252137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs
4
Total Activities
4
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
Selective kappa opioid antagonists for treatment of addiction, are we there yet?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.90 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415247 | JDTIC | 1.0 | 1 | 10.70 |
| CHEMBL575508 | — | — | 1 | 10.28 |
| CHEMBL2112474 | — | — | 1 | 7.81 |
| CHEMBL2112472 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415247 | JDTIC | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL575508 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL2112474 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL2112472 | — | Ki | = | 164.0 | nM | 6.79 |