Assay Detail
Binding
CHEMBL3294688
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT4 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake
31
Total Activities
31
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
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 4.87 | 5.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75035 | — | — | 1 | 5.71 |
| CHEMBL3289588 | — | — | 1 | 5.13 |
| CHEMBL3289573 | — | — | 1 | 5.08 |
| CHEMBL3289587 | — | — | 1 | 5.07 |
| CHEMBL3289575 | — | — | 1 | 5.04 |
| CHEMBL3289578 | — | — | 1 | 5.01 |
| CHEMBL3289586 | — | — | 1 | 4.99 |
| CHEMBL3289296 | — | — | 1 | 4.99 |
| CHEMBL3289585 | — | — | 1 | 4.99 |
| CHEMBL3289580 | — | — | 1 | 4.96 |
| CHEMBL3289570 | — | — | 1 | 4.94 |
| CHEMBL3289583 | — | — | 1 | 4.94 |
| CHEMBL3289566 | — | — | 1 | 4.93 |
| CHEMBL3289579 | — | — | 1 | 4.92 |
| CHEMBL3289292 | — | — | 1 | 4.92 |
| CHEMBL3289581 | — | — | 1 | 4.92 |
| CHEMBL3289576 | — | — | 1 | 4.90 |
| CHEMBL3289577 | — | — | 1 | 4.90 |
| CHEMBL3289582 | — | — | 1 | 4.87 |
| CHEMBL3289572 | — | — | 1 | 4.87 |
| CHEMBL3289571 | — | — | 1 | 4.84 |
| CHEMBL3289291 | — | — | 1 | 4.82 |
| CHEMBL3289568 | — | — | 1 | 4.82 |
| CHEMBL3289574 | — | — | 1 | 4.80 |
| CHEMBL3289584 | — | — | 1 | 4.70 |
| CHEMBL3289294 | — | — | 1 | 4.63 |
| CHEMBL3289569 | — | — | 1 | 4.59 |
| CHEMBL3289295 | — | — | 1 | 4.59 |
| CHEMBL3289567 | — | — | 1 | 4.50 |
| CHEMBL3289293 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75035 | — | IC50 | = | 1949.84 | nM | 5.71 |
| CHEMBL3289588 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL3289573 | — | IC50 | = | 8317.64 | nM | 5.08 |
| CHEMBL3289587 | — | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL3289575 | — | IC50 | = | 9120.11 | nM | 5.04 |
| CHEMBL3289578 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3289586 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3289296 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3289585 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3289580 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL3289570 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL3289583 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL3289566 | — | IC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL3289579 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289581 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289292 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289576 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3289577 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3289582 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL3289572 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL3289571 | — | IC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL3289568 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL3289291 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL3289574 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3289584 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL3289294 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL3289569 | — | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL3289295 | — | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL3289567 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3289293 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL3289290 | — | IC50 | = | 58884.37 | nM | 4.23 |