Assay Detail
Binding
CHEMBL4031734
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BGT1 Y453S/Y454A double mutant expressed in tsA201 cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method
6
Total Activities
3
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 betaine transporter (CHEMBL3715) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/γ-Aminobutyric Acid Transporter 1 (BGT1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.20 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 5.52 |
| CHEMBL1882801 | — | — | 2 | 5.26 |
| CHEMBL4060376 | — | — | 2 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL1882801 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL1882801 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4060376 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL4060376 | — | IC50 | = | 15000.0 | nM | 4.82 |