Assay Detail
Binding
CHEMBL792306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]5-HT reuptake into rat frontal cortex 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 serotonin transporter (CHEMBL313) ↗| 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 | 7.25 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 9.14 |
| CHEMBL543925 | — | — | 1 | 8.59 |
| CHEMBL809 | SERTRALINE | 4.0 | 1 | 8.47 |
| CHEMBL539050 | — | — | 1 | 8.39 |
| CHEMBL545557 | — | — | 1 | 7.85 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 7.85 |
| CHEMBL539564 | — | — | 1 | 7.57 |
| CHEMBL538053 | — | — | 1 | 7.52 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 7.43 |
| CHEMBL641 | ATOMOXETINE | 4.0 | 1 | 7.37 |
| CHEMBL544633 | — | — | 1 | 7.24 |
| CHEMBL542501 | — | — | 1 | 7.22 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 6.86 |
| CHEMBL540333 | — | — | 1 | 6.79 |
| CHEMBL556025 | — | — | 1 | 6.68 |
| CHEMBL539054 | — | — | 1 | 6.19 |
| CHEMBL555280 | — | — | 1 | 6.16 |
| CHEMBL542746 | — | — | 1 | 5.56 |
| CHEMBL306700 | VILOXAZINE | 4.0 | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL543925 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL809 | SERTRALINE | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL539050 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL545557 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL41 | FLUOXETINE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL539564 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL538053 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL637 | VENLAFAXINE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL641 | ATOMOXETINE | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL544633 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL542501 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL623 | NEFAZODONE | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL540333 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL556025 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL539054 | — | Ki | = | 643.0 | nM | 6.19 |
| CHEMBL555280 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL542746 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL306700 | VILOXAZINE | Ki | = | 16500.0 | nM | 4.78 |