Assay Detail
Binding
CHEMBL3399458
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Inhibition of mouse GAT4 expressed in HEK293 cells by [3H]GABA uptake assay
12
Total Activities
12
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 |
Publication
Design, synthesis and SAR studies of GABA uptake inhibitors derived from 2-substituted pyrrolidine-2-yl-acetic acids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.88 | 5.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.81 |
| CHEMBL3398502 | — | — | 1 | 5.24 |
| CHEMBL3398503 | — | — | 1 | 5.18 |
| CHEMBL3398494 | — | — | 1 | 4.85 |
| CHEMBL3398504 | — | — | 1 | 4.76 |
| CHEMBL3398496 | — | — | 1 | 4.67 |
| CHEMBL3398506 | — | — | 1 | 4.50 |
| CHEMBL3398507 | — | — | 1 | 4.00 |
| CHEMBL1163348 | — | — | 1 | - |
| CHEMBL1164855 | — | — | 1 | - |
| CHEMBL3398490 | — | — | 1 | - |
| CHEMBL3398497 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL3398502 | — | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL3398503 | — | IC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL3398494 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL3398504 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL3398496 | — | IC50 | = | 21379.62 | nM | 4.67 |
| CHEMBL3398506 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3398507 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL1163348 | — | IC50 | = | 1122018.45 | nM | - |
| CHEMBL1164855 | — | IC50 | = | 173780.08 | nM | - |
| CHEMBL3398490 | — | IC50 | = | 338844.16 | nM | - |
| CHEMBL3398497 | — | IC50 | = | 371535.23 | nM | - |