Assay Detail
Binding
CHEMBL3399460
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT1 expressed in HEK293 cells by [3H]GABA uptake assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.70 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.42 |
| CHEMBL3398501 | — | — | 1 | 6.14 |
| CHEMBL3398499 | — | — | 1 | 5.72 |
| CHEMBL3398500 | — | — | 1 | 5.38 |
| CHEMBL3398498 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 380.19 | nM | 6.42 |
| CHEMBL3398501 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL3398499 | — | IC50 | = | 1905.46 | nM | 5.72 |
| CHEMBL3398500 | — | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL3398498 | — | IC50 | = | 13803.84 | nM | 4.86 |