Assay Detail
Binding
CHEMBL5227864
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at MOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by liquid scintillation counting analysis
12
Total Activities
12
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 | 12 | 7.96 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5277326 | — | — | 1 | 9.15 |
| CHEMBL5287792 | — | — | 1 | 8.55 |
| CHEMBL5270915 | — | — | 1 | 8.39 |
| CHEMBL5272258 | — | — | 1 | 8.29 |
| CHEMBL5275873 | — | — | 1 | 8.25 |
| CHEMBL5272486 | — | — | 1 | 8.19 |
| CHEMBL38874 | DAMGO | — | 1 | 8.09 |
| CHEMBL5282901 | — | — | 1 | 8.03 |
| CHEMBL5279890 | — | — | 1 | 7.73 |
| CHEMBL5273356 | — | — | 1 | 7.24 |
| CHEMBL5287134 | — | — | 1 | 6.96 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5277326 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5287792 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5270915 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5272258 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5275873 | — | EC50 | = | 5.64 | nM | 8.25 |
| CHEMBL5272486 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL38874 | DAMGO | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5282901 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5279890 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL5273356 | — | EC50 | = | 57.1 | nM | 7.24 |
| CHEMBL5287134 | — | EC50 | = | 109.8 | nM | 6.96 |
| CHEMBL1400 | O-DESMETHYL TRAMADOL | EC50 | = | 244.7 | nM | 6.61 |