Assay Detail
Binding
CHEMBL4401742
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT-1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by scintillation counting analysis
10
Total Activities
10
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
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.32 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439989 | — | — | 1 | 8.27 |
| CHEMBL4555282 | — | — | 1 | 7.55 |
| CHEMBL4452694 | — | — | 1 | 7.49 |
| CHEMBL4455995 | — | — | 1 | 7.41 |
| CHEMBL4520656 | — | — | 1 | 7.25 |
| CHEMBL4565664 | — | — | 1 | 7.22 |
| CHEMBL4565745 | — | — | 1 | 7.18 |
| CHEMBL4475547 | — | — | 1 | 7.07 |
| CHEMBL4554639 | — | — | 1 | 6.99 |
| CHEMBL4551183 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439989 | — | IC50 | = | 5.37 | nM | 8.27 |
| CHEMBL4555282 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL4452694 | — | IC50 | = | 32.36 | nM | 7.49 |
| CHEMBL4455995 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL4520656 | — | IC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4565664 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL4565745 | — | IC50 | = | 66.07 | nM | 7.18 |
| CHEMBL4475547 | — | IC50 | = | 85.11 | nM | 7.07 |
| CHEMBL4554639 | — | IC50 | = | 102.33 | nM | 6.99 |
| CHEMBL4551183 | — | IC50 | = | 169.82 | nM | 6.77 |