Assay Detail
Binding
CHEMBL962312
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Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK-Net6 |
| 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 novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.31 | 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 | 8.47 |
| CHEMBL511827 | — | — | 1 | 8.22 |
| CHEMBL471519 | — | — | 1 | 8.05 |
| CHEMBL517424 | — | — | 1 | 7.72 |
| CHEMBL461148 | — | — | 1 | 7.66 |
| CHEMBL516965 | — | — | 1 | 7.52 |
| CHEMBL461323 | — | — | 1 | 7.50 |
| CHEMBL461153 | — | — | 1 | 7.36 |
| CHEMBL453838 | — | — | 1 | 7.33 |
| CHEMBL475527 | — | — | 1 | 6.92 |
| CHEMBL461322 | — | — | 1 | 6.78 |
| CHEMBL513577 | — | — | 1 | 6.70 |
| CHEMBL512677 | — | — | 1 | 6.67 |
| CHEMBL471518 | — | — | 1 | 6.51 |
| CHEMBL461330 | — | — | 1 | 6.33 |
| CHEMBL514193 | — | — | 1 | 6.20 |
| CHEMBL470313 | — | — | 1 | 5.98 |
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 | = | 3.4 | nM | 8.47 |
| CHEMBL511827 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL471519 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL517424 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL461148 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL516965 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL461323 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL461153 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL453838 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL475527 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL461322 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL513577 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL512677 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL471518 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL461330 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL514193 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL470313 | — | IC50 | = | 1053.0 | nM | 5.98 |