Assay Detail
Binding
CHEMBL759227
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Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous 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 | 7.82 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL300662 | — | — | 1 | 9.49 |
| CHEMBL51838 | — | — | 1 | 9.13 |
| CHEMBL52451 | — | — | 1 | 9.07 |
| CHEMBL50594 | — | — | 1 | 8.95 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.86 |
| CHEMBL2113735 | — | — | 1 | 8.76 |
| CHEMBL64019 | — | — | 1 | 7.94 |
| CHEMBL441049 | — | — | 1 | 7.67 |
| CHEMBL61653 | — | — | 1 | 7.65 |
| CHEMBL2113734 | — | — | 1 | 7.25 |
| CHEMBL444048 | — | — | 1 | 6.69 |
| CHEMBL293633 | — | — | 1 | 6.35 |
| CHEMBL61718 | — | — | 1 | 5.89 |
| CHEMBL60657 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL300662 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL51838 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL52451 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL50594 | — | Ki | = | 1.12 | nM | 8.95 |
| CHEMBL19019 | NALTREXONE | Ki | = | 1.39 | nM | 8.86 |
| CHEMBL2113735 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL64019 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL441049 | — | Ki | = | 21.2 | nM | 7.67 |
| CHEMBL61653 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL2113734 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL444048 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL293633 | — | Ki | = | 444.0 | nM | 6.35 |
| CHEMBL61718 | — | Ki | = | 1280.0 | nM | 5.89 |
| CHEMBL60657 | — | Ki | = | 1570.0 | nM | 5.80 |