Assay Detail
Binding
CHEMBL950283
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Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of alpha- and beta-6-amido derivatives of 17-cyclopropylmethyl-3, 14beta-dihydroxy-4, 5alpha-epoxymorphinan: potential alcohol-cessation agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 9.17 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL410122 | — | — | 1 | 10.22 |
| CHEMBL412050 | — | — | 1 | 10.05 |
| CHEMBL272215 | — | — | 1 | 10.00 |
| CHEMBL271815 | — | — | 1 | 9.80 |
| CHEMBL410526 | — | — | 1 | 9.62 |
| CHEMBL407466 | — | — | 1 | 9.55 |
| CHEMBL271811 | — | — | 1 | 9.54 |
| CHEMBL409458 | — | — | 1 | 9.43 |
| CHEMBL260528 | — | — | 1 | 9.41 |
| CHEMBL272051 | — | — | 1 | 9.40 |
| CHEMBL270918 | — | — | 1 | 9.38 |
| CHEMBL411927 | — | — | 1 | 9.37 |
| CHEMBL273105 | — | — | 1 | 9.35 |
| CHEMBL406116 | — | — | 1 | 9.29 |
| CHEMBL410884 | — | — | 1 | 9.14 |
| CHEMBL429929 | — | — | 1 | 9.14 |
| CHEMBL271797 | — | — | 1 | 9.11 |
| CHEMBL271755 | — | — | 1 | 9.10 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.09 |
| CHEMBL438413 | — | — | 1 | 9.04 |
| CHEMBL982 | NALMEFENE | 4.0 | 1 | 8.99 |
| CHEMBL443326 | — | — | 1 | 8.92 |
| CHEMBL411916 | — | — | 1 | 8.77 |
| CHEMBL272181 | — | — | 1 | 8.69 |
| CHEMBL411738 | — | — | 1 | 8.62 |
| CHEMBL429588 | — | — | 1 | 8.56 |
| CHEMBL409036 | — | — | 1 | 8.35 |
| CHEMBL272021 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL410122 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL412050 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL272215 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL271815 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL410526 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL407466 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL271811 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL409458 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL260528 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL272051 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL270918 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL411927 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL273105 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL406116 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL410884 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL429929 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL271797 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL271755 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL438413 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL982 | NALMEFENE | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL443326 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL411916 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL272181 | — | Ki | = | 2.03 | nM | 8.69 |
| CHEMBL411738 | — | Ki | = | 2.41 | nM | 8.62 |
| CHEMBL429588 | — | Ki | = | 2.74 | nM | 8.56 |
| CHEMBL409036 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL272021 | — | Ki | = | 150.61 | nM | 6.82 |