Assay Detail
Binding
CHEMBL1647125
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
32
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.80 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 8.08 |
| CHEMBL592374 | AMITIFADINE | 2.0 | 2 | 7.70 |
| CHEMBL1642912 | — | — | 1 | 7.58 |
| CHEMBL1642894 | — | — | 1 | 7.57 |
| CHEMBL1642902 | — | — | 1 | 7.55 |
| CHEMBL1642896 | — | — | 1 | 7.35 |
| CHEMBL1642906 | — | — | 1 | 7.14 |
| CHEMBL1642897 | — | — | 1 | 7.14 |
| CHEMBL1642904 | — | — | 1 | 7.04 |
| CHEMBL1642901 | — | — | 1 | 7.01 |
| CHEMBL1642915 | — | — | 1 | 6.95 |
| CHEMBL1642895 | — | — | 1 | 6.93 |
| CHEMBL1642890 | — | — | 1 | 6.91 |
| CHEMBL1642907 | — | — | 1 | 6.90 |
| CHEMBL1642913 | — | — | 1 | 6.80 |
| CHEMBL1642900 | — | — | 1 | 6.79 |
| CHEMBL1642898 | — | — | 1 | 6.78 |
| CHEMBL1642899 | — | — | 1 | 6.76 |
| CHEMBL1642893 | — | — | 1 | 6.76 |
| CHEMBL1642908 | — | — | 1 | 6.68 |
| CHEMBL1642903 | — | — | 1 | 6.59 |
| CHEMBL1642911 | — | — | 1 | 6.51 |
| CHEMBL1642909 | — | — | 1 | 6.43 |
| CHEMBL1642905 | — | — | 1 | 6.43 |
| CHEMBL1642910 | — | — | 1 | 6.25 |
| CHEMBL1642891 | — | — | 1 | 6.14 |
| CHEMBL1642914 | — | — | 1 | 6.12 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 6.08 |
| CHEMBL1642892 | — | — | 1 | 6.07 |
| CHEMBL1642916 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL295467 | NISOXETINE | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1642912 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1642894 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1642902 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1642896 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1642897 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1642906 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1642904 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL1642901 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1642915 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL1642895 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1642890 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL1642907 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1642913 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL1642900 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL1642898 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL1642899 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL1642893 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL1642908 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1642903 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL1642911 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL1642909 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL1642905 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL1642910 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL1642891 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL1642914 | — | IC50 | = | 766.0 | nM | 6.12 |
| CHEMBL809 | SERTRALINE | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL1642892 | — | IC50 | = | 855.0 | nM | 6.07 |
| CHEMBL1642916 | — | IC50 | = | 1642.0 | nM | 5.79 |
| CHEMBL1642917 | — | IC50 | = | 7262.0 | nM | 5.14 |