Assay Detail
Binding
CHEMBL4371753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NO711 binding to human GAT1 expressed in COS cell membranes preincubated for 25 mins by LC-ESI-MS/MS analysis
7
Total Activities
7
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
Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.59 | 6.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.81 |
| CHEMBL4525620 | — | — | 1 | 4.37 |
| CHEMBL4560424 | — | — | 1 | - |
| CHEMBL4563656 | — | — | 1 | - |
| CHEMBL4537310 | — | — | 1 | - |
| CHEMBL4436249 | — | — | 1 | - |
| CHEMBL4526583 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 154.88 | nM | 6.81 |
| CHEMBL4525620 | — | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL4560424 | — | IC50 | = | 134896.29 | nM | - |
| CHEMBL4563656 | — | IC50 | = | 134896.29 | nM | - |
| CHEMBL4537310 | — | IC50 | = | 134896.29 | nM | - |
| CHEMBL4436249 | — | IC50 | = | 134896.29 | nM | - |
| CHEMBL4526583 | — | IC50 | = | 134896.29 | nM | - |