Assay Detail
Binding
CHEMBL931354
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Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
34
Total Activities
34
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
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.18 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255663 | — | — | 1 | 8.57 |
| CHEMBL255450 | — | — | 1 | 8.55 |
| CHEMBL401677 | — | — | 1 | 8.54 |
| CHEMBL257389 | — | — | 1 | 8.41 |
| CHEMBL257602 | — | — | 1 | 8.25 |
| CHEMBL257388 | — | — | 1 | 8.09 |
| CHEMBL404027 | — | — | 1 | 8.08 |
| CHEMBL255449 | — | — | 1 | 8.06 |
| CHEMBL402089 | — | — | 1 | 7.92 |
| CHEMBL403616 | — | — | 1 | 7.70 |
| CHEMBL255246 | — | — | 1 | 7.70 |
| CHEMBL257809 | — | — | 1 | 7.54 |
| CHEMBL257348 | — | — | 1 | 7.43 |
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 7.40 |
| CHEMBL257810 | — | — | 1 | 7.40 |
| CHEMBL402027 | — | — | 1 | 7.36 |
| CHEMBL401676 | — | — | 1 | 7.31 |
| CHEMBL257390 | — | — | 1 | 7.19 |
| CHEMBL257338 | — | — | 1 | 7.19 |
| CHEMBL257964 | — | — | 1 | 7.12 |
| CHEMBL257603 | — | — | 1 | 7.00 |
| CHEMBL439423 | — | — | 1 | 6.96 |
| CHEMBL257130 | — | — | 1 | 6.82 |
| CHEMBL257808 | — | — | 1 | 6.77 |
| CHEMBL402090 | — | — | 1 | 6.70 |
| CHEMBL258013 | — | — | 1 | 6.57 |
| CHEMBL401804 | — | — | 1 | 6.25 |
| CHEMBL255448 | — | — | 1 | 5.96 |
| CHEMBL401976 | — | — | 1 | 5.82 |
| CHEMBL402088 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255663 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL255450 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL401677 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL257389 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL257602 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL257388 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL404027 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL255449 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL402089 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL403616 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL255246 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL257809 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL257348 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL99946 | LEVOMILNACIPRAN | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL257810 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL402027 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL401676 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL257390 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL257338 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL257964 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL257603 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL439423 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL257130 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL257808 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL402090 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL258013 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL401804 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL255448 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL401976 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL402088 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL403370 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL403760 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL259209 | MILNACIPRAN | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL403759 | — | IC50 | > | 10000.0 | nM | - |