Assay Detail
Binding
CHEMBL1775994
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells
16
Total Activities
16
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
Development of imidazole alkanoic acids as mGAT3 selective GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.69 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1773934 | — | — | 1 | 5.40 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.14 |
| CHEMBL1164505 | — | — | 1 | 4.72 |
| CHEMBL284116 | 5-AMINOVALERIC ACID | 1.0 | 1 | 4.13 |
| CHEMBL75035 | — | — | 1 | 4.07 |
| CHEMBL1773947 | — | — | 1 | - |
| CHEMBL543494 | — | — | 1 | - |
| CHEMBL554597 | — | — | 1 | - |
| CHEMBL557994 | — | — | 1 | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 1 | - |
| CHEMBL1773944 | — | — | 1 | - |
| CHEMBL1773945 | — | — | 1 | - |
| CHEMBL1773946 | — | — | 1 | - |
| CHEMBL1773939 | — | — | 1 | - |
| CHEMBL1773942 | — | — | 1 | - |
| CHEMBL297569 | BETA-ALANINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1773934 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL1164505 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL284116 | 5-AMINOVALERIC ACID | IC50 | = | 74131.02 | nM | 4.13 |
| CHEMBL75035 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL1773947 | — | IC50 | = | 117489.76 | nM | - |
| CHEMBL543494 | — | IC50 | = | 114815.36 | nM | - |
| CHEMBL554597 | — | IC50 | = | 1023292.99 | nM | - |
| CHEMBL557994 | — | IC50 | = | 676082.98 | nM | - |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | IC50 | = | 616595.0 | nM | - |
| CHEMBL1773944 | — | IC50 | = | 416869.38 | nM | - |
| CHEMBL1773945 | — | IC50 | = | 416869.38 | nM | - |
| CHEMBL1773946 | — | IC50 | = | 123026.88 | nM | - |
| CHEMBL1773939 | — | IC50 | = | 724435.96 | nM | - |
| CHEMBL1773942 | — | IC50 | = | 323593.66 | nM | - |
| CHEMBL297569 | BETA-ALANINE | IC50 | = | 2570395.78 | nM | - |