Assay Detail
Binding
CHEMBL754473
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Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.37 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.02 |
| CHEMBL52451 | — | — | 1 | 6.85 |
| CHEMBL50594 | — | — | 1 | 6.78 |
| CHEMBL300662 | — | — | 1 | 6.70 |
| CHEMBL51838 | — | — | 1 | 6.49 |
| CHEMBL2113735 | — | — | 1 | 6.15 |
| CHEMBL2113734 | — | — | 1 | 6.08 |
| CHEMBL64019 | — | — | 1 | 6.03 |
| CHEMBL61653 | — | — | 1 | 5.84 |
| CHEMBL441049 | — | — | 1 | 5.80 |
| CHEMBL60657 | — | — | 1 | - |
| CHEMBL444048 | — | — | 1 | - |
| CHEMBL61718 | — | — | 1 | - |
| CHEMBL293633 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 94.9 | nM | 7.02 |
| CHEMBL52451 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL50594 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL300662 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL51838 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL2113735 | — | Ki | = | 709.0 | nM | 6.15 |
| CHEMBL2113734 | — | Ki | = | 827.0 | nM | 6.08 |
| CHEMBL64019 | — | Ki | = | 931.0 | nM | 6.03 |
| CHEMBL61653 | — | Ki | = | 1450.0 | nM | 5.84 |
| CHEMBL441049 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL60657 | — | Ki | > | 7300.0 | nM | - |
| CHEMBL444048 | — | Ki | > | 7300.0 | nM | - |
| CHEMBL61718 | — | Ki | > | 7300.0 | nM | - |
| CHEMBL293633 | — | Ki | > | 7300.0 | nM | - |