Assay Detail
Binding
CHEMBL1769985
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.25 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173597 | — | — | 1 | 8.05 |
| CHEMBL1765600 | — | — | 1 | 7.89 |
| CHEMBL1173772 | — | — | 1 | 7.72 |
| CHEMBL1765599 | — | — | 1 | 7.62 |
| CHEMBL1173275 | — | — | 1 | 7.50 |
| CHEMBL1172928 | RADAFAXINE | 2.0 | 1 | 7.00 |
| CHEMBL1173276 | — | — | 1 | 6.82 |
| CHEMBL1171260 | — | — | 1 | 6.77 |
| CHEMBL1172929 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173597 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1765600 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1173772 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1765599 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1173275 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1172928 | RADAFAXINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1173276 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1171260 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1172929 | — | IC50 | = | 1200.0 | nM | 5.92 |