Assay Detail
Binding
CHEMBL753814
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Inhibition of binding [3H]DAMGO at Opioid receptor mu 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 | 6.20 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216640 | — | — | 1 | 8.00 |
| CHEMBL413228 | — | — | 1 | 7.57 |
| CHEMBL412792 | — | — | 1 | 7.07 |
| CHEMBL2369902 | — | — | 1 | 6.95 |
| CHEMBL407303 | — | — | 1 | 6.68 |
| CHEMBL415224 | — | — | 1 | 6.58 |
| CHEMBL2369896 | — | — | 1 | 6.54 |
| CHEMBL438034 | — | — | 1 | 6.19 |
| CHEMBL439898 | — | — | 1 | 6.07 |
| CHEMBL2369126 | — | — | 1 | 5.99 |
| CHEMBL2369124 | — | — | 1 | 5.87 |
| CHEMBL216940 | — | — | 1 | 5.72 |
| CHEMBL2369903 | — | — | 1 | 5.63 |
| CHEMBL414554 | — | — | 1 | 5.60 |
| CHEMBL2369125 | — | — | 1 | 5.55 |
| CHEMBL269119 | — | — | 1 | 5.29 |
| CHEMBL2369901 | — | — | 1 | 5.18 |
| CHEMBL2369891 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216640 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL413228 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL412792 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2369902 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL407303 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL415224 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2369896 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL438034 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL439898 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL2369126 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL2369124 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL216940 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2369903 | — | IC50 | = | 2350.0 | nM | 5.63 |
| CHEMBL414554 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2369125 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL269119 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2369901 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2369891 | — | IC50 | = | 7400.0 | nM | 5.13 |