Assay Detail
Binding
CHEMBL1815453
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Inhibition of human DAT expressed in HEK293 cells assessed as inhibition of [3H]DA 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 dopamine transporter (CHEMBL238) ↗| 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 | 8.30 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812741 | — | — | 1 | 9.12 |
| CHEMBL1812739 | — | — | 1 | 9.08 |
| CHEMBL1812747 | — | — | 1 | 8.82 |
| CHEMBL1812745 | — | — | 1 | 8.70 |
| CHEMBL1812746 | — | — | 1 | 8.64 |
| CHEMBL1812749 | — | — | 1 | 8.52 |
| CHEMBL1812743 | — | — | 1 | 8.41 |
| CHEMBL1812740 | — | — | 1 | 8.32 |
| CHEMBL1812750 | — | — | 1 | 8.19 |
| CHEMBL1812744 | — | — | 1 | 8.14 |
| CHEMBL1812742 | — | — | 1 | 7.96 |
| CHEMBL1812748 | — | — | 1 | 7.82 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812741 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL1812739 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL1812747 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1812745 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1812746 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1812749 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1812743 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1812740 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1812750 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL1812744 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL1812742 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1812748 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL894 | BUPROPION | IC50 | = | 658.0 | nM | 6.18 |