Assay Detail
Binding
CHEMBL1831835
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Inhibition of human NET expressed in MDCK-Net6 cells assessed as inhibition of norepinephrine uptake
22
Total Activities
22
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
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 | 22 | 7.35 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083410 | — | — | 1 | 8.52 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.47 |
| CHEMBL1082458 | — | — | 1 | 8.40 |
| CHEMBL1830892 | — | — | 1 | 8.15 |
| CHEMBL1830879 | — | — | 1 | 7.96 |
| CHEMBL1830878 | — | — | 1 | 7.89 |
| CHEMBL1830890 | — | — | 1 | 7.85 |
| CHEMBL1830885 | — | — | 1 | 7.82 |
| CHEMBL1830877 | — | — | 1 | 7.75 |
| CHEMBL1828653 | — | — | 1 | 7.66 |
| CHEMBL1830876 | — | — | 1 | 7.57 |
| CHEMBL1830884 | — | — | 1 | 7.27 |
| CHEMBL1830886 | — | — | 1 | 7.05 |
| CHEMBL1830889 | — | — | 1 | 7.04 |
| CHEMBL1830891 | — | — | 1 | 6.92 |
| CHEMBL1830880 | — | — | 1 | 6.83 |
| CHEMBL1830875 | — | — | 1 | 6.82 |
| CHEMBL1830888 | — | — | 1 | 6.70 |
| CHEMBL1830882 | — | — | 1 | 6.70 |
| CHEMBL1830881 | — | — | 1 | 6.68 |
| CHEMBL1830887 | — | — | 1 | 6.21 |
| CHEMBL1830883 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083410 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1082458 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1830892 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1830879 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1830878 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1830890 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1830885 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1830877 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1828653 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1830876 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1830884 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1830886 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1830889 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1830891 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1830880 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL1830875 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL1830888 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL1830882 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL1830881 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL1830887 | — | IC50 | = | 611.0 | nM | 6.21 |
| CHEMBL1830883 | — | IC50 | = | 4310.0 | nM | 5.37 |