Assay Detail
Binding
CHEMBL4342202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as reduction in NO711 binding at incubated for 4 hrs in presence of NO711 by LC-ESI-MS/MS analysis relative to control
5
Total Activities
5
Compounds Tested
2
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 |
|---|---|---|---|
| Ki | 4 | 6.60 | 7.43 |
| Kd | 1 | 7.58 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473104 | — | — | 1 | 7.58 |
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.43 |
| CHEMBL4464729 | — | — | 1 | 6.41 |
| CHEMBL4587609 | — | — | 1 | 6.39 |
| CHEMBL4539697 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473104 | — | Kd | = | 26.5 | nM | 7.58 |
| CHEMBL1027 | TIAGABINE | Ki | = | 37.15 | nM | 7.43 |
| CHEMBL4464729 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL4587609 | — | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL4539697 | — | Ki | = | 691.83 | nM | 6.16 |