Assay Detail
Binding
CHEMBL945185
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Inhibition of norepinephrine uptake at human NET in human HEK293 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.28 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.30 |
| CHEMBL486045 | — | — | 1 | 8.10 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 7.82 |
| CHEMBL486044 | — | — | 1 | 7.14 |
| CHEMBL520201 | — | — | 1 | 6.82 |
| CHEMBL521392 | — | — | 1 | 6.82 |
| CHEMBL525249 | — | — | 1 | 6.80 |
| CHEMBL453062 | — | — | 1 | 6.72 |
| CHEMBL520736 | — | — | 1 | 6.70 |
| CHEMBL488049 | — | — | 1 | 6.37 |
| CHEMBL447598 | — | — | 1 | 6.28 |
| CHEMBL453061 | — | — | 1 | 6.20 |
| CHEMBL446570 | — | — | 1 | 6.18 |
| CHEMBL520735 | — | — | 1 | 6.10 |
| CHEMBL486043 | — | — | 1 | 6.08 |
| CHEMBL453321 | — | — | 1 | 6.02 |
| CHEMBL486237 | — | — | 1 | 5.96 |
| CHEMBL487690 | — | — | 1 | 5.80 |
| CHEMBL486236 | — | — | 1 | 5.70 |
| CHEMBL445185 | — | — | 1 | 5.70 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.70 |
| CHEMBL487869 | — | — | 1 | 5.52 |
| CHEMBL486235 | — | — | 1 | 5.52 |
| CHEMBL488222 | — | — | 1 | 5.40 |
| CHEMBL488424 | — | — | 1 | 5.40 |
| CHEMBL530334 | — | — | 1 | 5.30 |
| CHEMBL487691 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL641 | ATOMOXETINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL486045 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL486044 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL520201 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL521392 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL525249 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL453062 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL520736 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL488049 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL447598 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL453061 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL446570 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL520735 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL486043 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL453321 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL486237 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL487690 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL486236 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL445185 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL487869 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL486235 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL488222 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL488424 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL530334 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL487691 | — | IC50 | = | 6000.0 | nM | 5.22 |