Assay Detail
Binding
CHEMBL3778906
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Inhibition of mouse GAT1 expressed in HEK293 cells assessed as [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA/unlabeled GABA addition measured after 4 mins by liquid scintillation counting analysis
16
Total Activities
16
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
Synthesis of 4-substituted nipecotic acid derivatives and their evaluation as potential GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.44 | 4.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 4.88 |
| CHEMBL3774606 | — | — | 1 | 4.61 |
| CHEMBL3775938 | — | — | 1 | 4.61 |
| CHEMBL3775303 | — | — | 1 | 4.59 |
| CHEMBL3775848 | — | — | 1 | 4.58 |
| CHEMBL3775466 | — | — | 1 | 4.46 |
| CHEMBL3774755 | — | — | 1 | 4.43 |
| CHEMBL3774662 | — | — | 1 | 4.43 |
| CHEMBL3775354 | — | — | 1 | 4.39 |
| CHEMBL3774577 | — | — | 1 | 4.22 |
| CHEMBL3775673 | — | — | 1 | 4.19 |
| CHEMBL3775725 | — | — | 1 | 4.17 |
| CHEMBL3775361 | — | — | 1 | 4.12 |
| CHEMBL3774505 | — | — | 1 | - |
| CHEMBL3774496 | — | — | 1 | - |
| CHEMBL3775515 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 13304.54 | nM | 4.88 |
| CHEMBL3774606 | — | IC50 | = | 24717.24 | nM | 4.61 |
| CHEMBL3775938 | — | IC50 | = | 24490.63 | nM | 4.61 |
| CHEMBL3775303 | — | IC50 | = | 25941.79 | nM | 4.59 |
| CHEMBL3775848 | — | IC50 | = | 26546.06 | nM | 4.58 |
| CHEMBL3775466 | — | IC50 | = | 34753.62 | nM | 4.46 |
| CHEMBL3774755 | — | IC50 | = | 36728.23 | nM | 4.43 |
| CHEMBL3774662 | — | IC50 | = | 37411.06 | nM | 4.43 |
| CHEMBL3775354 | — | IC50 | = | 40831.94 | nM | 4.39 |
| CHEMBL3774577 | — | IC50 | = | 60534.09 | nM | 4.22 |
| CHEMBL3775673 | — | IC50 | = | 64120.96 | nM | 4.19 |
| CHEMBL3775725 | — | IC50 | = | 66834.39 | nM | 4.17 |
| CHEMBL3775361 | — | IC50 | = | 75509.22 | nM | 4.12 |
| CHEMBL3774505 | — | IC50 | = | 106905.49 | nM | - |
| CHEMBL3774496 | — | IC50 | = | 1150800.39 | nM | - |
| CHEMBL3775515 | — | IC50 | = | 739605.28 | nM | - |