Assay Detail
Binding
CHEMBL1815454
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Inhibition of human NET expressed in HEK293 cells assessed as inhibition of [3H]NE 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 noradrenaline transporter (CHEMBL222) ↗| 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 | 7.79 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812750 | — | — | 1 | 9.30 |
| CHEMBL1812746 | — | — | 1 | 9.05 |
| CHEMBL1812745 | — | — | 1 | 8.96 |
| CHEMBL1812747 | — | — | 1 | 8.20 |
| CHEMBL1812749 | — | — | 1 | 8.19 |
| CHEMBL1812741 | — | — | 1 | 7.96 |
| CHEMBL1812748 | — | — | 1 | 7.85 |
| CHEMBL1812744 | — | — | 1 | 7.72 |
| CHEMBL1812743 | — | — | 1 | 7.58 |
| CHEMBL1812739 | — | — | 1 | 7.28 |
| CHEMBL1812740 | — | — | 1 | 6.91 |
| CHEMBL1812742 | — | — | 1 | 6.51 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812750 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1812746 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1812745 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1812747 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1812749 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1812741 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1812748 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1812744 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1812743 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1812739 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1812740 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1812742 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL894 | BUPROPION | IC50 | = | 1850.0 | nM | 5.73 |