Assay Detail
Binding
CHEMBL1055024
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Inhibition of [3H]norepinephrine uptake at human NET expressed in MDCK-Net6 cells by scintillation counting
21
Total Activities
21
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 | 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 | 21 | 7.77 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.51 |
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | 8.51 |
| CHEMBL14370 | REBOXETINE | 4.0 | 1 | 8.49 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 8.47 |
| CHEMBL551474 | — | — | 1 | 8.16 |
| CHEMBL564229 | — | — | 1 | 8.13 |
| CHEMBL551473 | — | — | 1 | 8.11 |
| CHEMBL560877 | — | — | 1 | 7.98 |
| CHEMBL563518 | — | — | 1 | 7.87 |
| CHEMBL559610 | — | — | 1 | 7.86 |
| CHEMBL563897 | — | — | 1 | 7.76 |
| CHEMBL564786 | — | — | 1 | 7.73 |
| CHEMBL562476 | — | — | 1 | 7.55 |
| CHEMBL564445 | — | — | 1 | 7.43 |
| CHEMBL557528 | — | — | 1 | 7.41 |
| CHEMBL539716 | — | — | 1 | 7.37 |
| CHEMBL562767 | — | — | 1 | 7.25 |
| CHEMBL559490 | — | — | 1 | 7.18 |
| CHEMBL557868 | — | — | 1 | 7.04 |
| CHEMBL561140 | — | — | 1 | 6.59 |
| CHEMBL563060 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL180101 | ESREBOXETINE | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL14370 | REBOXETINE | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL551474 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL564229 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL551473 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL560877 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL563518 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL559610 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL563897 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL564786 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL562476 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL564445 | — | IC50 | = | 36.7 | nM | 7.43 |
| CHEMBL557528 | — | IC50 | = | 39.4 | nM | 7.41 |
| CHEMBL539716 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL562767 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL559490 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL557868 | — | IC50 | = | 91.9 | nM | 7.04 |
| CHEMBL561140 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL563060 | — | IC50 | > | 1000.0 | nM | - |