Assay Detail
Binding
CHEMBL4401745
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Inhibition of mouse GAT-4 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
4
Total Activities
4
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 |
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 | 4 | 4.25 | 4.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4551183 | — | — | 1 | 4.49 |
| CHEMBL4565664 | — | — | 1 | 4.20 |
| CHEMBL4455995 | — | — | 1 | 4.15 |
| CHEMBL4555282 | — | — | 1 | 4.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4551183 | — | IC50 | = | 32359.37 | nM | 4.49 |
| CHEMBL4565664 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL4455995 | — | IC50 | = | 70794.58 | nM | 4.15 |
| CHEMBL4555282 | — | IC50 | = | 72443.6 | nM | 4.14 |