Assay Detail
Binding
CHEMBL1073263
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Inhibition of GAT1 in mouse D8 cells assessed as [3H]GABA transport by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | D8 |
| 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
Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.43 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.72 |
| CHEMBL603863 | — | — | 1 | 6.47 |
| CHEMBL594213 | — | — | 1 | 6.40 |
| CHEMBL604056 | — | — | 1 | 6.19 |
| CHEMBL594212 | — | — | 1 | 5.59 |
| CHEMBL603646 | — | — | 1 | 5.53 |
| CHEMBL604258 | — | — | 1 | 5.50 |
| CHEMBL593278 | — | — | 1 | 5.48 |
| CHEMBL595601 | — | — | 1 | 5.40 |
| CHEMBL593736 | — | — | 1 | 5.31 |
| CHEMBL596061 | — | — | 1 | 5.31 |
| CHEMBL593039 | — | — | 1 | 5.29 |
| CHEMBL611943 | — | — | 1 | 5.24 |
| CHEMBL604341 | — | — | 1 | 4.89 |
| CHEMBL593735 | — | — | 1 | 4.75 |
| CHEMBL594452 | — | — | 1 | 4.17 |
| CHEMBL594451 | — | — | 1 | 4.10 |
| CHEMBL596528 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL603863 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL594213 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL604056 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL594212 | — | IC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL603646 | — | IC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL604258 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL593278 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL595601 | — | IC50 | = | 3960.0 | nM | 5.40 |
| CHEMBL593736 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL596061 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL593039 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL611943 | — | IC50 | = | 5810.0 | nM | 5.24 |
| CHEMBL604341 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL593735 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL594452 | — | IC50 | = | 67400.0 | nM | 4.17 |
| CHEMBL594451 | — | IC50 | = | 79600.0 | nM | 4.10 |
| CHEMBL596528 | — | IC50 | > | 100000.0 | nM | - |