Assay Detail
Binding
CHEMBL2415586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to mouse GAT1 stably transfected in HEK293 cells by NO-711 binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| 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
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 4.71 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.41 |
| CHEMBL2414190 | — | — | 1 | 5.04 |
| CHEMBL2414193 | — | — | 1 | 4.94 |
| CHEMBL75035 | — | — | 1 | 4.56 |
| CHEMBL2414173 | — | — | 1 | 4.37 |
| CHEMBL2414194 | — | — | 1 | 4.36 |
| CHEMBL2414186 | — | — | 1 | 4.33 |
| CHEMBL2414189 | — | — | 1 | 4.29 |
| CHEMBL2414187 | — | — | 1 | 4.25 |
| CHEMBL2414192 | — | — | 1 | 4.12 |
| CHEMBL2414184 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL2414190 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL2414193 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL75035 | — | Ki | = | 27542.29 | nM | 4.56 |
| CHEMBL2414173 | — | Ki | = | 42657.95 | nM | 4.37 |
| CHEMBL2414194 | — | Ki | = | 43651.58 | nM | 4.36 |
| CHEMBL2414186 | — | Ki | = | 46773.51 | nM | 4.33 |
| CHEMBL2414189 | — | Ki | = | 51286.14 | nM | 4.29 |
| CHEMBL2414187 | — | Ki | = | 56234.13 | nM | 4.25 |
| CHEMBL2414192 | — | Ki | = | 75857.76 | nM | 4.12 |
| CHEMBL2414184 | — | Ki | = | 81283.05 | nM | 4.09 |