Assay Detail
Binding
CHEMBL792304
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Inhibition of [3H]- DA reuptake into rat striatal synaptosomes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.07 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539564 | — | — | 1 | 8.21 |
| CHEMBL539050 | — | — | 1 | 7.92 |
| CHEMBL543925 | — | — | 1 | 7.22 |
| CHEMBL545557 | — | — | 1 | 6.92 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 6.58 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 6.44 |
| CHEMBL538053 | — | — | 1 | 6.19 |
| CHEMBL542501 | — | — | 1 | 5.92 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 5.85 |
| CHEMBL540333 | — | — | 1 | 5.84 |
| CHEMBL556025 | — | — | 1 | 5.81 |
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 5.77 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 5.62 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 5.52 |
| CHEMBL555280 | — | — | 1 | 5.34 |
| CHEMBL544633 | — | — | 1 | 5.31 |
| CHEMBL539054 | — | — | 1 | 5.28 |
| CHEMBL542746 | — | — | 1 | 5.18 |
| CHEMBL306700 | VILOXAZINE | 4.0 | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539564 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL539050 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL543925 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL545557 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL809 | SERTRALINE | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL538053 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL542501 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL641 | ATOMOXETINE | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL540333 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL556025 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL490 | PAROXETINE | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL623 | NEFAZODONE | Ki | = | 2380.0 | nM | 5.62 |
| CHEMBL41 | FLUOXETINE | Ki | = | 3050.0 | nM | 5.52 |
| CHEMBL555280 | — | Ki | = | 4570.0 | nM | 5.34 |
| CHEMBL544633 | — | Ki | = | 4880.0 | nM | 5.31 |
| CHEMBL539054 | — | Ki | = | 5310.0 | nM | 5.28 |
| CHEMBL542746 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL306700 | VILOXAZINE | Ki | = | 48000.0 | nM | 4.32 |