Assay Detail
Binding
CHEMBL4371895
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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
Generation and screening of pseudostatic hydrazone libraries derived from 5-substituted nipecotic acid derivatives at the GABA transporter mGAT4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.29 | 4.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4566905 | — | — | 1 | 4.53 |
| CHEMBL4447559 | — | — | 1 | 4.26 |
| CHEMBL75035 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4566905 | — | IC50 | = | 29512.09 | nM | 4.53 |
| CHEMBL4447559 | — | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL75035 | — | IC50 | = | 85113.8 | nM | 4.07 |