Assay Detail
Binding
CHEMBL871963
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Tested for the binding affinity against the Kappa opioid receptor in guinea pig brain using [3H]U-69593
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.51 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.28 |
| CHEMBL2111914 | — | — | 1 | 9.22 |
| CHEMBL2111911 | — | — | 1 | 8.85 |
| CHEMBL2112729 | — | — | 1 | 8.82 |
| CHEMBL2112730 | — | — | 1 | 8.82 |
| CHEMBL140278 | — | — | 2 | 8.74 |
| CHEMBL2112732 | — | — | 1 | 8.70 |
| CHEMBL31421 | — | — | 1 | 8.68 |
| CHEMBL423341 | — | — | 1 | 8.48 |
| CHEMBL2111912 | — | — | 1 | 8.36 |
| CHEMBL2112740 | — | — | 1 | 8.21 |
| CHEMBL2111913 | — | — | 1 | 7.92 |
| CHEMBL2112736 | — | — | 1 | 7.57 |
| CHEMBL2111916 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL2111914 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2111911 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2112729 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2112730 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL140278 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2112732 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL31421 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL140278 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL423341 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2111912 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL2112740 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL2111913 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2112736 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2111916 | — | IC50 | = | 34.0 | nM | 7.47 |