Assay Detail
Binding
CHEMBL2393681
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Inhibition of [3H]5-HT uptake at human SERT 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 serotonin transporter (CHEMBL228) ↗| 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 | 6.12 | 7.01 |
| IC50 | 10 | 5.62 | 6.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | 4.0 | 2 | 7.01 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 2 | 6.95 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 6.85 |
| CHEMBL30713 | — | — | 2 | 6.09 |
| CHEMBL370805 | COCAINE | 4.0 | 2 | 6.09 |
| CHEMBL43048 | MIDOMAFETAMINE | 3.0 | 2 | 6.02 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 2 | 5.71 |
| CHEMBL6731 | TENAMFETAMINE | 2.0 | 2 | 5.64 |
| CHEMBL2391541 | — | — | 2 | 5.61 |
| CHEMBL612 | DEXTROAMPHETAMINE | 4.0 | 2 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL41 | FLUOXETINE | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL41 | FLUOXETINE | IC50 | = | 281.84 | nM | 6.55 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL30713 | — | Ki | = | 812.0 | nM | 6.09 |
| CHEMBL370805 | COCAINE | Ki | = | 818.0 | nM | 6.09 |
| CHEMBL43048 | MIDOMAFETAMINE | Ki | = | 948.0 | nM | 6.02 |
| CHEMBL273575 | NOMIFENSINE | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL6731 | TENAMFETAMINE | Ki | = | 2306.0 | nM | 5.64 |
| CHEMBL30713 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL370805 | COCAINE | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL2391541 | — | Ki | = | 2473.0 | nM | 5.61 |
| CHEMBL43048 | MIDOMAFETAMINE | IC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL612 | DEXTROAMPHETAMINE | Ki | = | 5728.0 | nM | 5.24 |
| CHEMBL6731 | TENAMFETAMINE | IC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL273575 | NOMIFENSINE | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL2391541 | — | IC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL612 | DEXTROAMPHETAMINE | IC50 | = | 16595.87 | nM | 4.78 |