Assay Detail
Binding
CHEMBL5227855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] DAMGO from mouse MOR expressed in CHO cell membrane incubated for 90 mins by scintillation method
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 | 44 | 7.62 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5270915 | — | — | 1 | 9.70 |
| CHEMBL5274117 | — | — | 1 | 9.15 |
| CHEMBL5272258 | — | — | 1 | 8.82 |
| CHEMBL5275873 | — | — | 1 | 8.82 |
| CHEMBL5279890 | — | — | 1 | 8.74 |
| CHEMBL5273356 | — | — | 1 | 8.70 |
| CHEMBL5281561 | — | — | 1 | 8.66 |
| CHEMBL38874 | DAMGO | — | 1 | 8.64 |
| CHEMBL5272171 | — | — | 1 | 8.55 |
| CHEMBL5281054 | — | — | 1 | 8.41 |
| CHEMBL5272744 | — | — | 1 | 8.39 |
| CHEMBL5274208 | — | — | 1 | 8.22 |
| CHEMBL5282901 | — | — | 1 | 8.04 |
| CHEMBL5274664 | — | — | 1 | 8.01 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | 7.89 |
| CHEMBL5281864 | — | — | 1 | 7.82 |
| CHEMBL5281114 | — | — | 1 | 7.62 |
| CHEMBL5290025 | — | — | 1 | 7.60 |
| CHEMBL5289463 | — | — | 1 | 7.60 |
| CHEMBL5270488 | — | — | 1 | 7.55 |
| CHEMBL5277164 | — | — | 1 | 7.52 |
| CHEMBL5271351 | — | — | 1 | 7.46 |
| CHEMBL5277743 | — | — | 1 | 7.38 |
| CHEMBL5269558 | — | — | 1 | 7.35 |
| CHEMBL5287134 | — | — | 1 | 7.27 |
| CHEMBL5269806 | — | — | 1 | 7.24 |
| CHEMBL5275209 | — | — | 1 | 7.16 |
| CHEMBL5273683 | — | — | 1 | 7.14 |
| CHEMBL5287093 | — | — | 1 | 7.09 |
| CHEMBL5278225 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5270915 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL5274117 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL5275873 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5272258 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL5279890 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL5273356 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL5281561 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL38874 | DAMGO | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5272171 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL5281054 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL5272744 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL5274208 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5282901 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL5274664 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5281864 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL5281114 | — | Ki | = | 24.2 | nM | 7.62 |
| CHEMBL5290025 | — | Ki | = | 25.3 | nM | 7.60 |
| CHEMBL5289463 | — | Ki | = | 25.2 | nM | 7.60 |
| CHEMBL5270488 | — | Ki | = | 28.1 | nM | 7.55 |
| CHEMBL5277164 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL5271351 | — | Ki | = | 34.8 | nM | 7.46 |
| CHEMBL5277743 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL5269558 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL5287134 | — | Ki | = | 53.5 | nM | 7.27 |
| CHEMBL5269806 | — | Ki | = | 57.6 | nM | 7.24 |
| CHEMBL5275209 | — | Ki | = | 69.2 | nM | 7.16 |
| CHEMBL5273683 | — | Ki | = | 72.9 | nM | 7.14 |
| CHEMBL5287093 | — | Ki | = | 81.6 | nM | 7.09 |
| CHEMBL5278225 | — | Ki | = | 82.3 | nM | 7.08 |
| CHEMBL5283662 | — | Ki | = | 85.6 | nM | 7.07 |
| CHEMBL5272486 | — | Ki | = | 87.8 | nM | 7.06 |
| CHEMBL5271628 | — | Ki | = | 89.6 | nM | 7.05 |
| CHEMBL5288272 | — | Ki | = | 115.4 | nM | 6.94 |
| CHEMBL5282507 | — | Ki | = | 155.1 | nM | 6.81 |
| CHEMBL5279510 | — | Ki | = | 164.8 | nM | 6.78 |
| CHEMBL5268998 | — | Ki | = | 200.2 | nM | 6.70 |
| CHEMBL5283376 | — | Ki | = | 218.8 | nM | 6.66 |
| CHEMBL5288358 | — | Ki | = | 225.2 | nM | 6.65 |
| CHEMBL5286526 | — | Ki | = | 233.6 | nM | 6.63 |
| CHEMBL5285920 | — | Ki | = | 353.0 | nM | 6.45 |
| CHEMBL5268021 | — | Ki | = | 2312.0 | nM | 5.64 |
| CHEMBL5287792 | — | Ki | = | 0.0026 | nM | - |
| CHEMBL5277326 | — | Ki | = | 0.0034 | nM | - |