Assay Detail
Binding
CHEMBL5227857
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69593 from human KOR expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method
36
Total Activities
36
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
Discovery, Structure-Activity Relationship, and Mechanistic Studies of 1-((3<i>R</i>,4<i>S</i>)-3-((Dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)piperidin-1-yl)-2-(2,4,5-trifluorophenyl)ethan-1-one as a Novel Potent Analgesic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 6.61 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 9.05 |
| CHEMBL5277326 | — | — | 1 | 8.10 |
| CHEMBL5270915 | — | — | 1 | 7.71 |
| CHEMBL5272486 | — | — | 1 | 7.38 |
| CHEMBL5287134 | — | — | 1 | 7.37 |
| CHEMBL5272258 | — | — | 1 | 7.37 |
| CHEMBL5275873 | — | — | 1 | 7.21 |
| CHEMBL5273356 | — | — | 1 | 7.19 |
| CHEMBL5274664 | — | — | 1 | 7.13 |
| CHEMBL5272171 | — | — | 1 | 7.03 |
| CHEMBL5269558 | — | — | 1 | 7.03 |
| CHEMBL5287792 | — | — | 1 | 6.98 |
| CHEMBL5279890 | — | — | 1 | 6.90 |
| CHEMBL5281054 | — | — | 1 | 6.79 |
| CHEMBL5274208 | — | — | 1 | 6.77 |
| CHEMBL5281561 | — | — | 1 | 6.77 |
| CHEMBL5288358 | — | — | 1 | 6.69 |
| CHEMBL5281864 | — | — | 1 | 6.64 |
| CHEMBL5272744 | — | — | 1 | 6.62 |
| CHEMBL5282901 | — | — | 1 | 6.56 |
| CHEMBL5275209 | — | — | 1 | 6.54 |
| CHEMBL5274117 | — | — | 1 | 6.19 |
| CHEMBL5277743 | — | — | 1 | 6.17 |
| CHEMBL5277164 | — | — | 1 | 6.17 |
| CHEMBL5281114 | — | — | 1 | 6.00 |
| CHEMBL5270488 | — | — | 1 | 5.89 |
| CHEMBL5285920 | — | — | 1 | 5.77 |
| CHEMBL5283662 | — | — | 1 | 5.70 |
| CHEMBL5278225 | — | — | 1 | 5.63 |
| CHEMBL5287093 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL5277326 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL5270915 | — | Ki | = | 19.7 | nM | 7.71 |
| CHEMBL5272486 | — | Ki | = | 41.9 | nM | 7.38 |
| CHEMBL5287134 | — | Ki | = | 42.3 | nM | 7.37 |
| CHEMBL5272258 | — | Ki | = | 43.1 | nM | 7.37 |
| CHEMBL5275873 | — | Ki | = | 61.2 | nM | 7.21 |
| CHEMBL5273356 | — | Ki | = | 64.1 | nM | 7.19 |
| CHEMBL5274664 | — | Ki | = | 74.4 | nM | 7.13 |
| CHEMBL5269558 | — | Ki | = | 93.6 | nM | 7.03 |
| CHEMBL5272171 | — | Ki | = | 94.2 | nM | 7.03 |
| CHEMBL5287792 | — | Ki | = | 104.9 | nM | 6.98 |
| CHEMBL5279890 | — | Ki | = | 126.9 | nM | 6.90 |
| CHEMBL5281054 | — | Ki | = | 163.9 | nM | 6.79 |
| CHEMBL5281561 | — | Ki | = | 169.3 | nM | 6.77 |
| CHEMBL5274208 | — | Ki | = | 169.1 | nM | 6.77 |
| CHEMBL5288358 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL5281864 | — | Ki | = | 227.4 | nM | 6.64 |
| CHEMBL5272744 | — | Ki | = | 241.8 | nM | 6.62 |
| CHEMBL5282901 | — | Ki | = | 277.1 | nM | 6.56 |
| CHEMBL5275209 | — | Ki | = | 287.6 | nM | 6.54 |
| CHEMBL5274117 | — | Ki | = | 648.9 | nM | 6.19 |
| CHEMBL5277743 | — | Ki | = | 673.1 | nM | 6.17 |
| CHEMBL5277164 | — | Ki | = | 675.4 | nM | 6.17 |
| CHEMBL5281114 | — | Ki | = | 1009.0 | nM | 6.00 |
| CHEMBL5270488 | — | Ki | = | 1277.0 | nM | 5.89 |
| CHEMBL5285920 | — | Ki | = | 1701.0 | nM | 5.77 |
| CHEMBL5283662 | — | Ki | = | 1987.0 | nM | 5.70 |
| CHEMBL5278225 | — | Ki | = | 2357.0 | nM | 5.63 |
| CHEMBL5287093 | — | Ki | = | 2651.0 | nM | 5.58 |
| CHEMBL5268603 | — | Ki | = | 3031.0 | nM | 5.52 |
| CHEMBL5288272 | — | Ki | = | 3098.0 | nM | 5.51 |
| CHEMBL5273683 | — | Ki | = | 4055.0 | nM | 5.39 |
| CHEMBL5290025 | — | Ki | = | 4424.0 | nM | 5.35 |
| CHEMBL5269806 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL5283376 | — | Ki | > | 5000.0 | nM | - |