Assay Detail
Binding
CHEMBL1055025
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Inhibition of [3H]nisoxetine binding to human NET expressed in MDCK-Net6 cells by plate scintillation counting
8
Total Activities
8
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 | Intermediate |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.96 | 8.39 |
| Ki | 1 | 8.68 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.68 |
| CHEMBL560877 | — | — | 1 | 8.39 |
| CHEMBL551474 | — | — | 1 | 8.39 |
| CHEMBL564229 | — | — | 1 | 8.19 |
| CHEMBL563518 | — | — | 1 | 7.97 |
| CHEMBL559610 | — | — | 1 | 7.94 |
| CHEMBL563897 | — | — | 1 | 7.78 |
| CHEMBL539716 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72 | DESIPRAMINE | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL560877 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL551474 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL564229 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL563518 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL559610 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL563897 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL539716 | — | IC50 | = | 90.0 | nM | 7.05 |