Assay Detail
Binding
CHEMBL4342200
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method
7
Total Activities
7
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
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of γ-aminobutyric acid transporter 1 (GAT1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.47 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.88 |
| CHEMBL4587609 | — | — | 1 | 5.72 |
| CHEMBL4464729 | — | — | 1 | 5.64 |
| CHEMBL351355 | — | — | 1 | 5.39 |
| CHEMBL4539697 | — | — | 1 | 5.32 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.14 |
| CHEMBL4586784 | — | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL4587609 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL4464729 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL351355 | — | IC50 | = | 4073.8 | nM | 5.39 |
| CHEMBL4539697 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4586784 | — | IC50 | = | 67608.3 | nM | 4.17 |