Assay Detail
Binding
CHEMBL1815455
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Inhibition of human SERTexpressed in HEK293 cells assessed as inhibition of [3H]5HT reuptake after 10 mins by scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.68 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812745 | — | — | 1 | 9.00 |
| CHEMBL1812746 | — | — | 1 | 8.21 |
| CHEMBL1812749 | — | — | 1 | 6.98 |
| CHEMBL1812750 | — | — | 1 | 6.96 |
| CHEMBL1812747 | — | — | 1 | 6.94 |
| CHEMBL1812748 | — | — | 1 | 6.16 |
| CHEMBL1812743 | — | — | 1 | 5.70 |
| CHEMBL1812740 | — | — | 1 | 5.70 |
| CHEMBL1812741 | — | — | 1 | 5.58 |
| CHEMBL1812739 | — | — | 1 | 5.55 |
| CHEMBL1812744 | — | — | 1 | - |
| CHEMBL1812742 | — | — | 1 | - |
| CHEMBL894 | BUPROPION | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812745 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1812746 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1812749 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1812750 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1812747 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL1812748 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1812743 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1812740 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL1812741 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1812739 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL1812744 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1812742 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL894 | BUPROPION | IC50 | > | 100000.0 | nM | - |