Assay Detail
Binding
CHEMBL5227868
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Agonist activity at KOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis
7
Total Activities
7
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 |
|---|---|---|---|
| EC50 | 7 | 6.85 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 8.55 |
| CHEMBL5273356 | — | — | 1 | 7.12 |
| CHEMBL5287792 | — | — | 1 | 6.98 |
| CHEMBL5277326 | — | — | 1 | 6.57 |
| CHEMBL5270915 | — | — | 1 | 6.46 |
| CHEMBL5287134 | — | — | 1 | 6.30 |
| CHEMBL5279890 | — | — | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5273356 | — | EC50 | = | 75.4 | nM | 7.12 |
| CHEMBL5287792 | — | EC50 | = | 105.4 | nM | 6.98 |
| CHEMBL5277326 | — | EC50 | = | 267.3 | nM | 6.57 |
| CHEMBL5270915 | — | EC50 | = | 342.8 | nM | 6.46 |
| CHEMBL5287134 | — | EC50 | = | 500.2 | nM | 6.30 |
| CHEMBL5279890 | — | EC50 | = | 1032.0 | nM | 5.99 |