Assay Detail
Binding
CHEMBL4041111
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Inhibition of SERT expressed in rat brain synaptosomes assessed as decrease in incorporation of [3H]serotonin measured after 15 mins by scintillation counting method
12
Total Activities
12
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
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.78 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4095555 | — | — | 1 | 8.00 |
| CHEMBL4066532 | — | — | 1 | 7.96 |
| CHEMBL4088249 | — | — | 1 | 7.92 |
| CHEMBL4104622 | — | — | 1 | 7.80 |
| CHEMBL4065568 | — | — | 1 | 7.77 |
| CHEMBL11 | IMIPRAMINE | 4.0 | 1 | 7.21 |
| CHEMBL4075673 | — | — | 1 | - |
| CHEMBL4080369 | — | — | 1 | - |
| CHEMBL4104216 | — | — | 1 | - |
| CHEMBL4095979 | — | — | 1 | - |
| CHEMBL4085802 | — | — | 1 | - |
| CHEMBL1112 | ARIPIPRAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4095555 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4066532 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4088249 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4104622 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4065568 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL11 | IMIPRAMINE | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4075673 | — | IC50 | - | — | - | |
| CHEMBL4080369 | — | IC50 | - | — | - | |
| CHEMBL4104216 | — | IC50 | - | — | - | |
| CHEMBL4095979 | — | IC50 | - | — | - | |
| CHEMBL4085802 | — | IC50 | - | — | - | |
| CHEMBL1112 | ARIPIPRAZOLE | IC50 | - | — | - |