Assay Detail
Binding
CHEMBL5336807
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Inhibition of NO 711 marker binding to mouse GAT1 by LC-ESI-MS/MS based competitive MS binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 4.28 | 4.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5424877 | — | — | 1 | 4.61 |
| CHEMBL5404846 | — | — | 1 | 4.55 |
| CHEMBL5409309 | — | — | 1 | 4.39 |
| CHEMBL5423316 | — | — | 1 | 4.34 |
| CHEMBL5423337 | — | — | 1 | 4.24 |
| CHEMBL5411369 | — | — | 1 | 4.17 |
| CHEMBL5411905 | — | — | 1 | 4.11 |
| CHEMBL5419680 | — | — | 1 | 4.10 |
| CHEMBL5416293 | — | — | 1 | 4.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5424877 | — | Ki | = | 24547.09 | nM | 4.61 |
| CHEMBL5404846 | — | Ki | = | 28183.83 | nM | 4.55 |
| CHEMBL5409309 | — | Ki | = | 40738.03 | nM | 4.39 |
| CHEMBL5423316 | — | Ki | = | 45708.82 | nM | 4.34 |
| CHEMBL5423337 | — | Ki | = | 57543.99 | nM | 4.24 |
| CHEMBL5411369 | — | Ki | = | 67608.3 | nM | 4.17 |
| CHEMBL5411905 | — | Ki | = | 77624.71 | nM | 4.11 |
| CHEMBL5419680 | — | Ki | = | 79432.82 | nM | 4.10 |
| CHEMBL5416293 | — | Ki | = | 93325.43 | nM | 4.03 |