Assay Detail
Functional
CHEMBL5209624
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 1745860)
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.08 | 8.30 |
| EC50 | 3 | 5.10 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256695 | NISOXETINE HYDROCHLORIDE | — | 1 | 8.30 |
| CHEMBL2105282 | — | — | 1 | 8.30 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | 4.0 | 1 | 8.20 |
| CHEMBL1702 | ATOMOXETINE HYDROCHLORIDE | 4.0 | 1 | 7.70 |
| CHEMBL1201156 | NORTRIPTYLINE HYDROCHLORIDE | 4.0 | 1 | 7.40 |
| CHEMBL1237135 | MAPROTILINE HYDROCHLORIDE | 4.0 | 1 | 7.30 |
| CHEMBL1237129 | 1R,2S-MILNACIPRAN HYDROCHLORIDE | — | 1 | 7.30 |
| CHEMBL1200964 | AMITRIPTYLINE HYDROCHLORIDE | 4.0 | 1 | 6.70 |
| CHEMBL85236 | — | — | 1 | 6.50 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | 4.0 | 1 | 6.20 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.10 |
| CHEMBL1200818 | — | — | 1 | 5.40 |
| CHEMBL5087452 | — | — | 1 | 5.20 |
| CHEMBL1698 | BUPROPION HYDROCHLORIDE | 4.0 | 1 | 4.90 |
| CHEMBL1557 | DOPAMINE HYDROCHLORIDE | 4.0 | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256695 | NISOXETINE HYDROCHLORIDE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2105282 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1702 | ATOMOXETINE HYDROCHLORIDE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1201156 | NORTRIPTYLINE HYDROCHLORIDE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1237135 | MAPROTILINE HYDROCHLORIDE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1237129 | 1R,2S-MILNACIPRAN HYDROCHLORIDE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1200964 | AMITRIPTYLINE HYDROCHLORIDE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL85236 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL529437 | COCAINE HYDROCHLORIDE | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL1200818 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5087452 | — | EC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1698 | BUPROPION HYDROCHLORIDE | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1557 | DOPAMINE HYDROCHLORIDE | EC50 | = | 20000.0 | nM | 4.70 |