Assay Detail
Binding
CHEMBL998745
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Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
30
Total Activities
30
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
Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.29 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL444742 | — | — | 1 | 8.52 |
| CHEMBL526270 | — | — | 1 | 8.52 |
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | 8.52 |
| CHEMBL497512 | — | — | 1 | 8.40 |
| CHEMBL497846 | — | — | 1 | 8.40 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.30 |
| CHEMBL505433 | — | — | 1 | 8.30 |
| CHEMBL525375 | — | — | 1 | 8.15 |
| CHEMBL525238 | — | — | 1 | 8.15 |
| CHEMBL524313 | — | — | 1 | 8.10 |
| CHEMBL448375 | — | — | 1 | 8.10 |
| CHEMBL497479 | — | — | 1 | 7.58 |
| CHEMBL498120 | — | — | 1 | 7.57 |
| CHEMBL526669 | — | — | 1 | 7.52 |
| CHEMBL498509 | — | — | 1 | 7.46 |
| CHEMBL498482 | — | — | 1 | 7.41 |
| CHEMBL445082 | — | — | 1 | 7.40 |
| CHEMBL497463 | — | — | 1 | 7.00 |
| CHEMBL524798 | — | — | 1 | 7.00 |
| CHEMBL498495 | — | — | 1 | 6.70 |
| CHEMBL452429 | — | — | 1 | 6.64 |
| CHEMBL498142 | — | — | 1 | 6.43 |
| CHEMBL525717 | — | — | 1 | 6.43 |
| CHEMBL497461 | — | — | 1 | 6.38 |
| CHEMBL498481 | — | — | 1 | 6.16 |
| CHEMBL498141 | — | — | 1 | 6.05 |
| CHEMBL525532 | — | — | 1 | 6.00 |
| CHEMBL443952 | — | — | 1 | 6.00 |
| CHEMBL504606 | — | — | 1 | 5.89 |
| CHEMBL510352 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL444742 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL526270 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL180101 | ESREBOXETINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL497512 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL497846 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL505433 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL525375 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL525238 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL524313 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL448375 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL497479 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL498120 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL526669 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL498509 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL498482 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL445082 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL497463 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL524798 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL498495 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL452429 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL498142 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL525717 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL497461 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL498481 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL498141 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL525532 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL443952 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL504606 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL510352 | — | IC50 | = | 3100.0 | nM | 5.51 |