Assay Detail
Binding
CHEMBL753170
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Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig membranes
14
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 | 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 | 6.92 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.33 |
| CHEMBL300662 | — | — | 1 | 7.55 |
| CHEMBL50594 | — | — | 1 | 7.45 |
| CHEMBL52451 | — | — | 1 | 7.41 |
| CHEMBL2113735 | — | — | 1 | 7.09 |
| CHEMBL51838 | — | — | 1 | 6.91 |
| CHEMBL293633 | — | — | 1 | 6.70 |
| CHEMBL64019 | — | — | 1 | 6.53 |
| CHEMBL61718 | — | — | 1 | 6.50 |
| CHEMBL2113734 | — | — | 1 | 6.41 |
| CHEMBL444048 | — | — | 1 | 6.17 |
| CHEMBL60657 | — | — | 1 | 5.94 |
| CHEMBL441049 | — | — | 1 | - |
| CHEMBL61653 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 4.71 | nM | 8.33 |
| CHEMBL300662 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL50594 | — | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL52451 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL2113735 | — | Ki | = | 81.8 | nM | 7.09 |
| CHEMBL51838 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL293633 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL64019 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL61718 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL2113734 | — | Ki | = | 388.0 | nM | 6.41 |
| CHEMBL444048 | — | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL60657 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL441049 | — | Ki | > | 690.0 | nM | - |
| CHEMBL61653 | — | Ki | > | 690.0 | nM | - |