Assay Detail
Binding
CHEMBL3755178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Straightforward and effective synthesis of γ-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 5.72 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473104 | — | — | 1 | 6.75 |
| CHEMBL76768 | GUVACINE | — | 1 | 4.68 |
| CHEMBL3753338 | — | — | 1 | - |
| CHEMBL3752449 | — | — | 1 | - |
| CHEMBL3752733 | — | — | 1 | - |
| CHEMBL3753616 | — | — | 1 | - |
| CHEMBL3752032 | — | — | 1 | - |
| CHEMBL3752080 | — | — | 1 | - |
| CHEMBL3752039 | — | — | 1 | - |
| CHEMBL75035 | — | — | 1 | - |
| CHEMBL3753682 | — | — | 1 | - |
| CHEMBL3752695 | — | — | 1 | - |
| CHEMBL3752644 | — | — | 1 | - |
| CHEMBL3754424 | — | — | 1 | - |
| CHEMBL1887095 | — | — | 1 | - |
| CHEMBL3753828 | — | — | 1 | - |
| CHEMBL3754441 | — | — | 1 | - |
| CHEMBL3752545 | — | — | 1 | - |
| CHEMBL3753554 | — | — | 1 | - |
| CHEMBL3754254 | — | — | 1 | - |
| CHEMBL3752875 | — | — | 1 | - |
| CHEMBL3752268 | — | — | 1 | - |
| CHEMBL3751979 | — | — | 1 | - |
| CHEMBL3753545 | — | — | 1 | - |
| CHEMBL3753634 | — | — | 1 | - |
| CHEMBL3753899 | — | — | 1 | - |
| CHEMBL3752003 | — | — | 1 | - |
| CHEMBL3753440 | — | — | 1 | - |
| CHEMBL3753364 | — | — | 1 | - |
| CHEMBL3753393 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473104 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL76768 | GUVACINE | IC50 | = | 20900.0 | nM | 4.68 |
| CHEMBL3754424 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753896 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3752644 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3752695 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753682 | — | IC50 | = | 233000.0 | nM | - |
| CHEMBL75035 | — | IC50 | = | 199000.0 | nM | - |
| CHEMBL3752039 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752080 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752032 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753616 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752733 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752449 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753338 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753151 | — | IC50 | = | 2050000.0 | nM | - |
| CHEMBL3754503 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3754490 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL1887095 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3753828 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3754441 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752545 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753554 | — | IC50 | > | 5000000.0 | nM | - |
| CHEMBL3754254 | — | IC50 | = | 371000.0 | nM | - |
| CHEMBL3752875 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752268 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3751979 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753545 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753634 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753899 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3752003 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753440 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753364 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL3753393 | — | IC50 | = | 371000.0 | nM | - |