Assay Detail
Binding
CHEMBL995197
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Inhibition of norepinephrine uptake at human NET expressed in HEK cells
41
Total Activities
41
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
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497512 | — | — | 1 | 8.40 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 8.30 |
| CHEMBL526270 | — | — | 1 | 8.22 |
| CHEMBL497846 | — | — | 1 | 8.15 |
| CHEMBL526825 | — | — | 1 | 8.10 |
| CHEMBL444742 | — | — | 1 | 8.10 |
| CHEMBL497679 | — | — | 1 | 8.05 |
| CHEMBL455447 | — | — | 1 | 8.00 |
| CHEMBL497845 | — | — | 1 | 7.96 |
| CHEMBL497680 | — | — | 1 | 7.89 |
| CHEMBL497493 | — | — | 1 | 7.85 |
| CHEMBL498687 | — | — | 1 | 7.82 |
| CHEMBL295467 | NISOXETINE | 2.0 | 1 | 7.82 |
| CHEMBL448375 | — | — | 1 | 7.77 |
| CHEMBL505433 | — | — | 1 | 7.75 |
| CHEMBL445082 | — | — | 1 | 7.58 |
| CHEMBL524271 | — | — | 1 | 7.52 |
| CHEMBL497665 | — | — | 1 | 7.46 |
| CHEMBL522065 | — | — | 1 | 7.44 |
| CHEMBL497479 | — | — | 1 | 7.44 |
| CHEMBL525375 | — | — | 1 | 7.40 |
| CHEMBL497492 | — | — | 1 | 7.35 |
| CHEMBL498509 | — | — | 1 | 7.34 |
| CHEMBL526670 | — | — | 1 | 7.12 |
| CHEMBL524798 | — | — | 1 | 7.02 |
| CHEMBL526669 | — | — | 1 | 7.00 |
| CHEMBL498680 | — | — | 1 | 6.85 |
| CHEMBL496284 | — | — | 1 | 6.85 |
| CHEMBL498510 | — | — | 1 | 6.84 |
| CHEMBL498686 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497512 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL641 | ATOMOXETINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL526270 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL497846 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL526825 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL444742 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL497679 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL455447 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL497845 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL497680 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL497493 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL498687 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL295467 | NISOXETINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL448375 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL505433 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL445082 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL524271 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL497665 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL522065 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL497479 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL525375 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL497492 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL498509 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL526670 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL524798 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL526669 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL498680 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL496284 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL498510 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL498686 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL498495 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL496285 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL526306 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL523574 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL524624 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL451105 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL497666 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL497664 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL505902 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL505439 | — | IC50 | = | 8000.0 | nM | 5.10 |