Assay Detail
Binding
CHEMBL2393682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay
20
Total Activities
10
Compounds Tested
2
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
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.18 | 7.08 |
| IC50 | 10 | 5.46 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273575 | NOMIFENSINE | 4.0 | 2 | 7.08 |
| CHEMBL612 | DEXTROAMPHETAMINE | 4.0 | 2 | 7.00 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 6.48 |
| CHEMBL43048 | MIDOMAFETAMINE | 3.0 | 2 | 6.40 |
| CHEMBL30713 | — | — | 2 | 6.19 |
| CHEMBL6731 | TENAMFETAMINE | 2.0 | 2 | 6.15 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 5.90 |
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 5.86 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 2 | 5.79 |
| CHEMBL2391541 | — | — | 2 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273575 | NOMIFENSINE | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL612 | DEXTROAMPHETAMINE | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL43048 | MIDOMAFETAMINE | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL612 | DEXTROAMPHETAMINE | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL273575 | NOMIFENSINE | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL30713 | — | Ki | = | 642.0 | nM | 6.19 |
| CHEMBL6731 | TENAMFETAMINE | Ki | = | 704.0 | nM | 6.15 |
| CHEMBL370805 | COCAINE | Ki | = | 1257.0 | nM | 5.90 |
| CHEMBL41 | FLUOXETINE | Ki | = | 1394.0 | nM | 5.86 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 1623.0 | nM | 5.79 |
| CHEMBL43048 | MIDOMAFETAMINE | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL6731 | TENAMFETAMINE | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL30713 | — | IC50 | = | 3715.35 | nM | 5.43 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL370805 | COCAINE | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2391541 | — | Ki | = | 12008.0 | nM | 4.92 |
| CHEMBL2391541 | — | IC50 | = | 42657.95 | nM | 4.37 |