Assay Detail
Binding
CHEMBL1073264
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Inhibition of GAT3 in mouse D8 cells assessed as [3H]GABA transport by liquid scintillation counting
6
Total Activities
6
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 |
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 | 6 | 4.39 | 4.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603863 | — | — | 1 | 4.58 |
| CHEMBL594213 | — | — | 1 | 4.19 |
| CHEMBL594212 | — | — | 1 | - |
| CHEMBL604258 | — | — | 1 | - |
| CHEMBL593278 | — | — | 1 | - |
| CHEMBL594451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603863 | — | IC50 | = | 26600.0 | nM | 4.58 |
| CHEMBL594213 | — | IC50 | = | 64800.0 | nM | 4.19 |
| CHEMBL594212 | — | IC50 | = | 309000.0 | nM | - |
| CHEMBL604258 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL593278 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL594451 | — | IC50 | > | 100000.0 | nM | - |