Assay Detail
Binding
CHEMBL754619
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Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593
19
Total Activities
19
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
Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.86 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2115245 | — | — | 1 | 10.43 |
| CHEMBL90667 | — | — | 1 | 10.03 |
| CHEMBL328236 | — | — | 1 | 9.89 |
| CHEMBL328269 | — | — | 1 | 9.80 |
| CHEMBL93731 | — | — | 1 | 9.64 |
| CHEMBL329020 | — | — | 1 | 9.49 |
| CHEMBL327935 | — | — | 1 | 9.42 |
| CHEMBL2114257 | — | — | 1 | 9.19 |
| CHEMBL314294 | — | — | 1 | 8.89 |
| CHEMBL327576 | — | — | 1 | 8.89 |
| CHEMBL96785 | — | — | 1 | 8.72 |
| CHEMBL327885 | — | — | 1 | 8.35 |
| CHEMBL91231 | — | — | 1 | 8.10 |
| CHEMBL430833 | — | — | 1 | 8.00 |
| CHEMBL327490 | — | — | 1 | 7.92 |
| CHEMBL92774 | — | — | 1 | 7.82 |
| CHEMBL90305 | — | — | 1 | 7.60 |
| CHEMBL92349 | — | — | 1 | 7.24 |
| CHEMBL1790045 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2115245 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL90667 | — | Ki | = | 0.094 | nM | 10.03 |
| CHEMBL328236 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL328269 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL93731 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL329020 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL327935 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL2114257 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL314294 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL327576 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL96785 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL327885 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL91231 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL430833 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL327490 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL92774 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL90305 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL92349 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL1790045 | — | Ki | = | 0.003 | nM | - |