Assay Detail
Binding
CHEMBL4031713
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BGT1 Q299L 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 | 5.56 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.07 |
| CHEMBL1882801 | — | — | 2 | 5.54 |
| CHEMBL4060376 | — | — | 2 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 851.14 | nM | 6.07 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1882801 | — | IC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL1882801 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4060376 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4060376 | — | IC50 | = | 8000.0 | nM | 5.10 |