Assay Detail
Binding
CHEMBL1831836
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Displacement of [3H]nisoxetine from human NET expressed in MDCK-Net6 cells
22
Total Activities
22
Compounds Tested
2
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
Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.54 | 8.70 |
| Ki | 1 | 8.68 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082458 | — | — | 1 | 8.70 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.68 |
| CHEMBL1828653 | — | — | 1 | 8.30 |
| CHEMBL1830885 | — | — | 1 | 8.30 |
| CHEMBL1830879 | — | — | 1 | 8.30 |
| CHEMBL1830877 | — | — | 1 | 8.15 |
| CHEMBL1830890 | — | — | 1 | 8.10 |
| CHEMBL1830878 | — | — | 1 | 8.05 |
| CHEMBL1083410 | — | — | 1 | 8.05 |
| CHEMBL1830892 | — | — | 1 | 7.89 |
| CHEMBL1830876 | — | — | 1 | 7.89 |
| CHEMBL1830884 | — | — | 1 | 7.52 |
| CHEMBL1830880 | — | — | 1 | 7.13 |
| CHEMBL1830889 | — | — | 1 | 7.10 |
| CHEMBL1830886 | — | — | 1 | 7.00 |
| CHEMBL1830875 | — | — | 1 | 6.99 |
| CHEMBL1830888 | — | — | 1 | 6.84 |
| CHEMBL1830891 | — | — | 1 | 6.68 |
| CHEMBL1830887 | — | — | 1 | 6.55 |
| CHEMBL1830883 | — | — | 1 | 5.64 |
| CHEMBL1830881 | — | — | 1 | - |
| CHEMBL1830882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082458 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL72 | DESIPRAMINE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL1828653 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1830885 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1830879 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1830877 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1830890 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1830878 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1083410 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1830892 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1830876 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1830884 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1830880 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1830889 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1830886 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL1830875 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1830888 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL1830891 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL1830887 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL1830883 | — | IC50 | = | 2304.0 | nM | 5.64 |
| CHEMBL1830881 | — | IC50 | - | — | - | |
| CHEMBL1830882 | — | IC50 | - | — | - |