Assay Detail
Binding
CHEMBL3363226
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL1903) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.94 | 4.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1446457 | — | — | 1 | 4.94 |
| CHEMBL75035 | — | — | 1 | - |
| CHEMBL3326391 | — | — | 1 | - |
| CHEMBL3040189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1446457 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL75035 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3326391 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3040189 | — | IC50 | > | 100000.0 | nM | - |