Assay Detail
Binding
CHEMBL4137353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1 assessed as reduction in GABA uptake
3
Total Activities
3
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
Development of New Photoswitchable Azobenzene Based γ-Aminobutyric Acid (GABA) Uptake Inhibitors with Distinctly Enhanced Potency upon Photoactivation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.15 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.88 |
| CHEMBL4166168 | — | — | 1 | 6.39 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL4166168 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 6456.54 | nM | 5.19 |