Assay Detail
Binding
CHEMBL752595
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Inhibition of binding [3H]U-69539 at Opioid receptor kappa 1 of guinea pig brain membrane (GPB) homogenates.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Effects of modifications of residues in position 3 of dynorphin A(1-11)-NH2 on kappa receptor selectivity and potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.58 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216640 | — | — | 1 | 9.24 |
| CHEMBL415224 | — | — | 1 | 9.12 |
| CHEMBL413228 | — | — | 1 | 9.05 |
| CHEMBL407303 | — | — | 1 | 8.96 |
| CHEMBL412792 | — | — | 1 | 8.23 |
| CHEMBL2369902 | — | — | 1 | 8.22 |
| CHEMBL2369896 | — | — | 1 | 8.05 |
| CHEMBL438034 | — | — | 1 | 7.64 |
| CHEMBL439898 | — | — | 1 | 7.40 |
| CHEMBL2369126 | — | — | 1 | 7.26 |
| CHEMBL2369125 | — | — | 1 | 6.95 |
| CHEMBL2369124 | — | — | 1 | 6.92 |
| CHEMBL2369903 | — | — | 1 | 6.90 |
| CHEMBL2369901 | — | — | 1 | 6.82 |
| CHEMBL269119 | — | — | 1 | 6.64 |
| CHEMBL2369891 | — | — | 1 | 6.62 |
| CHEMBL216940 | — | — | 1 | 6.42 |
| CHEMBL414554 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216640 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL415224 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL413228 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL407303 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL412792 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL2369902 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2369896 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL438034 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL439898 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2369126 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2369125 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL2369124 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL2369903 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL2369901 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL269119 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2369891 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL216940 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL414554 | — | IC50 | = | 1100.0 | nM | 5.96 |