Assay Detail
Binding
CHEMBL747749
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Tested for the binding affinity against the Mu opioid receptor in guinea pig brain using [3H]-DAMGO
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 | 8.55 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.64 |
| CHEMBL2111914 | — | — | 1 | 9.52 |
| CHEMBL140278 | — | — | 2 | 9.30 |
| CHEMBL2112730 | — | — | 1 | 9.15 |
| CHEMBL2111912 | — | — | 1 | 9.00 |
| CHEMBL2111911 | — | — | 1 | 8.92 |
| CHEMBL2112729 | — | — | 1 | 8.77 |
| CHEMBL2112732 | — | — | 1 | 8.62 |
| CHEMBL2112740 | — | — | 1 | 8.51 |
| CHEMBL2111916 | — | — | 1 | 8.18 |
| CHEMBL423341 | — | — | 1 | 8.18 |
| CHEMBL2111913 | — | — | 1 | 8.00 |
| CHEMBL2112736 | — | — | 1 | 7.80 |
| CHEMBL31421 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL2111914 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL140278 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2112730 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2111912 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL140278 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2111911 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2112729 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2112732 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2112740 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2111916 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL423341 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2111913 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2112736 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL31421 | — | IC50 | = | 1760.0 | nM | 5.75 |