Assay Detail
Binding
CHEMBL752591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of plasma membrane homogenates of guinea pig brain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain/Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, and biological activities of cyclic lactam peptide analogues of dynorphine A(1-11)-NH2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.62 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216640 | — | — | 1 | 9.24 |
| CHEMBL217049 | — | — | 1 | 8.82 |
| CHEMBL216182 | — | — | 1 | 8.31 |
| CHEMBL387083 | — | — | 1 | 8.18 |
| CHEMBL412580 | — | — | 1 | 7.76 |
| CHEMBL386170 | — | — | 1 | 7.60 |
| CHEMBL384485 | — | — | 1 | 7.46 |
| CHEMBL277132 | — | — | 1 | 7.33 |
| CHEMBL412600 | — | — | 1 | 7.00 |
| CHEMBL415339 | — | — | 1 | 7.00 |
| CHEMBL413011 | — | — | 1 | 6.96 |
| CHEMBL387437 | — | — | 1 | 6.72 |
| CHEMBL264733 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216640 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL217049 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL216182 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL387083 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL412580 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL386170 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL384485 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL277132 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL412600 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL415339 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL413011 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL387437 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL264733 | — | IC50 | = | 220.0 | nM | 6.66 |