Assay Detail
Binding
CHEMBL4401736
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GAT1 expressed in COS cells assessed as decrease in [3H]GABA uptake after 10 mins by scintillation counting analysis
6
Total Activities
6
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 1 (CHEMBL1903) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Screening oxime libraries by means of mass spectrometry (MS) binding assays: Identification of new highly potent inhibitors to optimized inhibitors γ-aminobutyric acid transporter 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.47 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38686 | — | — | 1 | 6.89 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | — | 1 | 5.22 |
| CHEMBL277498 | NIPECOTIC ACID | — | 1 | 5.10 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.85 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38686 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL77575 | (R)-NIPECOTIC ACID | IC50 | = | 5960.0 | nM | 5.22 |
| CHEMBL277498 | NIPECOTIC ACID | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL76768 | GUVACINE | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL77484 | (S)-NIPECOTIC ACID | IC50 | = | 116000.0 | nM | - |