Assay Detail
Binding
CHEMBL750280
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was evaluated for the inhibition of [3H]bremazocine binding to Opioid receptor kappa 1 in guinea pig cerebellum membrane homogenates.
9
Total Activities
9
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
Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.59 | 10.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384584 | — | — | 1 | 10.49 |
| CHEMBL2373009 | — | — | 1 | 10.31 |
| CHEMBL438223 | DYNORPHIN A (1-11) | — | 1 | 9.89 |
| CHEMBL2028997 | — | — | 1 | 9.64 |
| CHEMBL3037891 | — | — | 1 | 7.71 |
| CHEMBL2373014 | — | — | 1 | 7.69 |
| CHEMBL2373013 | — | — | 1 | 7.62 |
| CHEMBL2373008 | — | — | 1 | 7.14 |
| CHEMBL2373012 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384584 | — | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL2373009 | — | Ki | = | 0.049 | nM | 10.31 |
| CHEMBL438223 | DYNORPHIN A (1-11) | Ki | = | 0.128 | nM | 9.89 |
| CHEMBL2028997 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3037891 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL2373014 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL2373013 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL2373008 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2373012 | — | Ki | = | 153.0 | nM | 6.82 |