Assay Detail
Binding
CHEMBL3871875
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Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting method
8
Total Activities
8
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 serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of SMP-304, a novel benzylpiperidine derivative with serotonin transporter inhibitory activity and 5-HT1A weak partial agonistic activity showing the antidepressant-like effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.67 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.96 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 8.70 |
| CHEMBL259209 | MILNACIPRAN | 4.0 | 1 | 7.66 |
| CHEMBL3913541 | — | — | 1 | 7.18 |
| CHEMBL3894524 | — | — | 1 | 6.99 |
| CHEMBL3966886 | — | — | 1 | 6.67 |
| CHEMBL3892582 | — | — | 1 | 6.56 |
| CHEMBL3981001 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL11 | IMIPRAMINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL259209 | MILNACIPRAN | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3913541 | — | Ki | = | 66.4 | nM | 7.18 |
| CHEMBL3894524 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL3966886 | — | Ki | = | 212.0 | nM | 6.67 |
| CHEMBL3892582 | — | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL3981001 | — | Ki | < | 100.0 | nM | - |