Assay Detail
Binding
CHEMBL754825
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Opioid receptor kappa 1 using [3H]diprenorphine as radioligand in guinea pig cerebellar membrane in absence of 120 mM NaCl + 50 uM Gpp(NH)p
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 | Autocuration |
Publication
Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.47 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384584 | — | — | 1 | 9.59 |
| CHEMBL442323 | — | — | 1 | 9.39 |
| CHEMBL406338 | — | — | 1 | 8.64 |
| CHEMBL406893 | — | — | 1 | 8.48 |
| CHEMBL268818 | — | — | 1 | 8.13 |
| CHEMBL266782 | — | — | 1 | 7.67 |
| CHEMBL267215 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384584 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL442323 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL406338 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL406893 | — | IC50 | = | 3.31 | nM | 8.48 |
| CHEMBL268818 | — | IC50 | = | 7.32 | nM | 8.13 |
| CHEMBL266782 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL267215 | — | IC50 | = | 43.2 | nM | 7.37 |