Assay Detail
Binding
CHEMBL986142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.77 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 8.52 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.52 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.41 |
| CHEMBL1175 | DULOXETINE | 4.0 | 1 | 8.40 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.22 |
| CHEMBL446809 | — | — | 1 | 8.22 |
| CHEMBL513912 | — | — | 1 | 8.15 |
| CHEMBL475937 | — | — | 1 | 8.15 |
| CHEMBL475936 | — | — | 1 | 7.85 |
| CHEMBL514354 | — | — | 1 | 7.72 |
| CHEMBL515614 | — | — | 1 | 7.58 |
| CHEMBL453838 | — | — | 1 | 7.33 |
| CHEMBL476154 | — | — | 1 | 7.28 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 7.00 |
| CHEMBL514200 | — | — | 1 | 6.76 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 6.25 |
| CHEMBL509007 | — | — | 1 | - |
| CHEMBL475945 | — | — | 1 | - |
| CHEMBL514515 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14370 | REBOXETINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1175 | DULOXETINE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL446809 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL513912 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL475937 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL475936 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL514354 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL515614 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL453838 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL476154 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL490 | PAROXETINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL514200 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL509007 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL475945 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL514515 | — | IC50 | > | 3000.0 | nM | - |