Assay Detail
Binding
CHEMBL4229768
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NET expressed in MDCK cells assessed as decrease in [3H]-noradrenaline reuptake after 10 mins by scintillation counting method
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent noradrenaline transporter (CHEMBL222) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.52 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251694 | — | — | 1 | 7.21 |
| CHEMBL2204341 | — | — | 1 | 6.96 |
| CHEMBL637 | VENLAFAXINE | 4.0 | 1 | 6.83 |
| CHEMBL427215 | — | — | 1 | 6.60 |
| CHEMBL2311600 | — | — | 1 | 6.56 |
| CHEMBL252720 | (S)-VENLAFAXINE | — | 1 | 6.12 |
| CHEMBL2204342 | — | — | 1 | 5.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251694 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2204341 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL637 | VENLAFAXINE | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL427215 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL2311600 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL252720 | (S)-VENLAFAXINE | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL2204342 | — | IC50 | = | 4715.0 | nM | 5.33 |