Assay Detail
Binding
CHEMBL3636666
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Displacement of [3H]diprenorphine from rat kappa-opioid receptor expressed in CHO cells after 90 mins by scintillation counter
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.62 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3634917 | — | — | 1 | 7.54 |
| CHEMBL3634920 | — | — | 1 | 7.35 |
| CHEMBL3634921 | — | — | 1 | 7.21 |
| CHEMBL3634927 | — | — | 1 | 7.16 |
| CHEMBL2372399 | ZYKLOPHIN | — | 1 | 7.02 |
| CHEMBL3634918 | — | — | 1 | 6.80 |
| CHEMBL3632647 | — | — | 1 | 6.78 |
| CHEMBL3634929 | — | — | 1 | 6.65 |
| CHEMBL3634926 | — | — | 1 | 6.53 |
| CHEMBL3634919 | — | — | 1 | 6.49 |
| CHEMBL3634922 | — | — | 1 | 6.46 |
| CHEMBL3634928 | — | — | 1 | 6.39 |
| CHEMBL3634930 | — | — | 1 | 6.39 |
| CHEMBL3634916 | — | — | 1 | 6.38 |
| CHEMBL3634923 | — | — | 1 | 6.29 |
| CHEMBL3634925 | — | — | 1 | 5.76 |
| CHEMBL3634924 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3634917 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL3634920 | — | Ki | = | 44.4 | nM | 7.35 |
| CHEMBL3634921 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3634927 | — | Ki | = | 68.7 | nM | 7.16 |
| CHEMBL2372399 | ZYKLOPHIN | Ki | = | 95.2 | nM | 7.02 |
| CHEMBL3634918 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3632647 | — | Ki | = | 168.0 | nM | 6.78 |
| CHEMBL3634929 | — | Ki | = | 222.0 | nM | 6.65 |
| CHEMBL3634926 | — | Ki | = | 293.0 | nM | 6.53 |
| CHEMBL3634919 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL3634922 | — | Ki | = | 346.0 | nM | 6.46 |
| CHEMBL3634928 | — | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL3634930 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL3634916 | — | Ki | = | 412.0 | nM | 6.38 |
| CHEMBL3634923 | — | Ki | = | 516.0 | nM | 6.29 |
| CHEMBL3634925 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL3634924 | — | Ki | = | 4010.0 | nM | 5.40 |