Assay Detail
Binding
CHEMBL4371902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT3 expressed in COS7 cells assessed as reduction in [2H6]GABA uptake preincubated for 25 mins followed by [2H6]GABA addition and measured after 6 mins by LC-MS/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 3 (CHEMBL5208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 4 | 5.29 | 5.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447559 | — | — | 1 | 5.56 |
| CHEMBL75035 | — | — | 1 | 5.48 |
| CHEMBL4566905 | — | — | 1 | 5.09 |
| CHEMBL4548691 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447559 | — | IC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL75035 | — | IC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL4566905 | — | IC50 | = | 8128.31 | nM | 5.09 |
| CHEMBL4548691 | — | IC50 | = | 9332.54 | nM | 5.03 |