Assay Detail
Binding
CHEMBL4254543
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Inhibition of [3H]serotonin reuptake in rat brain synaptosomes SERT after 15 mins by TopCount scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.10 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2104993 | VORTIOXETINE | 4.0 | 1 | 8.54 |
| CHEMBL4286174 | — | — | 1 | 8.12 |
| CHEMBL4288120 | — | — | 1 | 8.03 |
| CHEMBL4277476 | — | — | 1 | 8.00 |
| CHEMBL4289783 | — | — | 1 | 7.60 |
| CHEMBL4289605 | — | — | 1 | 7.51 |
| CHEMBL4278933 | — | — | 1 | 7.38 |
| CHEMBL4294077 | — | — | 1 | 7.02 |
| CHEMBL4291322 | — | — | 1 | 6.96 |
| CHEMBL4279099 | — | — | 1 | 6.92 |
| CHEMBL4285796 | — | — | 1 | 6.82 |
| CHEMBL4277854 | — | — | 1 | 6.80 |
| CHEMBL4283479 | — | — | 1 | 6.72 |
| CHEMBL4279592 | — | — | 1 | 6.68 |
| CHEMBL4288753 | — | — | 1 | 6.23 |
| CHEMBL4278094 | — | — | 1 | 5.77 |
| CHEMBL4294729 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2104993 | VORTIOXETINE | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4286174 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4288120 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4277476 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4289783 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4289605 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4278933 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4294077 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4291322 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4279099 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4285796 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4277854 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4283479 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4279592 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4288753 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4278094 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4294729 | — | IC50 | = | 2900.0 | nM | 5.54 |