Assay Detail
Binding
CHEMBL4371741
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Inhibition of mouse GAT4 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by liquid scintillation counting method
3
Total Activities
3
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
Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.44 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526583 | — | — | 1 | 4.82 |
| CHEMBL4436249 | — | — | 1 | 4.38 |
| CHEMBL4525620 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526583 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL4436249 | — | IC50 | = | 41686.94 | nM | 4.38 |
| CHEMBL4525620 | — | IC50 | = | 75857.76 | nM | 4.12 |