Assay Detail
Functional
CHEMBL5581346
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Inhibition of human SERT extracted from HEK293 cell membrane assessed as inhibition of 5-HT reuptake incubated for 5 mins by fluorescent based microbeta2 scintillation counter analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dual 5-HT<sub>6</sub>/SERT ligands for mitigating neuropsychiatric symptoms of dementia exerting neuroprotection against amyloid-β toxicity, memory preservation, and antidepressant-like properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.83 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | 4.0 | 1 | 8.15 |
| CHEMBL5595193 | — | — | 1 | 7.96 |
| CHEMBL1508 | ESCITALOPRAM | 4.0 | 1 | 7.26 |
| CHEMBL5593858 | — | — | 1 | 7.19 |
| CHEMBL5589768 | — | — | 1 | 7.17 |
| CHEMBL5591924 | — | — | 1 | 7.09 |
| CHEMBL5591292 | — | — | 1 | 6.99 |
| CHEMBL5595885 | — | — | 1 | 6.97 |
| CHEMBL5594772 | — | — | 1 | 6.80 |
| CHEMBL5595197 | — | — | 1 | 6.79 |
| CHEMBL5594664 | — | — | 1 | 6.67 |
| CHEMBL5595568 | — | — | 1 | 6.61 |
| CHEMBL5595917 | — | — | 1 | 6.57 |
| CHEMBL5592369 | — | — | 1 | 6.05 |
| CHEMBL5594193 | — | — | 1 | 5.98 |
| CHEMBL5593795 | — | — | 1 | 5.97 |
| CHEMBL5592533 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL490 | PAROXETINE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5595193 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1508 | ESCITALOPRAM | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5593858 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5589768 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5591924 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5591292 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5595885 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5594772 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5595197 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5594664 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5595568 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL5595917 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL5592369 | — | IC50 | = | 886.0 | nM | 6.05 |
| CHEMBL5594193 | — | IC50 | = | 1042.0 | nM | 5.98 |
| CHEMBL5593795 | — | IC50 | = | 1075.0 | nM | 5.97 |
| CHEMBL5592533 | — | IC50 | = | 1212.0 | nM | 5.92 |