Assay Detail
Functional
CHEMBL840560
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Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes
25
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.45 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98894 | — | — | 1 | 7.10 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 3 | 7.00 |
| CHEMBL99175 | — | — | 1 | 6.96 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 6.92 |
| CHEMBL101819 | — | — | 1 | 6.89 |
| CHEMBL1118 | DESVENLAFAXINE | 4.0 | 1 | 6.75 |
| CHEMBL420644 | — | — | 1 | 6.75 |
| CHEMBL101055 | — | — | 1 | 6.72 |
| CHEMBL99503 | — | — | 1 | 6.70 |
| CHEMBL319142 | — | — | 1 | 6.64 |
| CHEMBL101056 | — | — | 1 | 6.62 |
| CHEMBL101899 | — | — | 1 | 6.50 |
| CHEMBL419533 | — | — | 1 | 6.40 |
| CHEMBL100774 | — | — | 1 | 6.40 |
| CHEMBL100773 | — | — | 1 | 6.31 |
| CHEMBL100191 | — | — | 1 | 6.30 |
| CHEMBL329923 | — | — | 1 | 6.24 |
| CHEMBL98842 | — | — | 1 | 6.17 |
| CHEMBL99653 | — | — | 1 | 5.84 |
| CHEMBL99670 | — | — | 1 | 5.81 |
| CHEMBL1628258 | N-DESMETHYLVENLAFAXINE CHLORIDE | — | 1 | 5.80 |
| CHEMBL98660 | — | — | 1 | 5.59 |
| CHEMBL72 | DESIPRAMINE | 4.0 | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98894 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL99175 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL101819 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1118 | DESVENLAFAXINE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL420644 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL101055 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL99503 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL319142 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL101056 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL101899 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL419533 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL100774 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL100773 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL100191 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL329923 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL98842 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL99653 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL99670 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL1628258 | N-DESMETHYLVENLAFAXINE CHLORIDE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL98660 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL72 | DESIPRAMINE | IC50 | = | 3000.0 | nM | 5.52 |