Assay Detail
Binding
CHEMBL3294686
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Inhibition of mouse GAT2 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake
31
Total Activities
31
Compounds Tested
2
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 | 30 | 4.93 | 5.23 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3289583 | — | — | 1 | 5.23 |
| CHEMBL3289585 | — | — | 1 | 5.23 |
| CHEMBL3289575 | — | — | 1 | 5.19 |
| CHEMBL3289296 | — | — | 1 | 5.16 |
| CHEMBL3289570 | — | — | 1 | 5.11 |
| CHEMBL3289588 | — | — | 1 | 5.10 |
| CHEMBL3289295 | — | — | 1 | 5.10 |
| CHEMBL3289568 | — | — | 1 | 5.05 |
| CHEMBL3289587 | — | — | 1 | 5.03 |
| CHEMBL3289566 | — | — | 1 | 5.02 |
| CHEMBL3289578 | — | — | 1 | 5.02 |
| CHEMBL3289569 | — | — | 1 | 5.02 |
| CHEMBL3289586 | — | — | 1 | 5.01 |
| CHEMBL3289576 | — | — | 1 | 5.01 |
| CHEMBL3289582 | — | — | 1 | 4.99 |
| CHEMBL3289580 | — | — | 1 | 4.99 |
| CHEMBL3289581 | — | — | 1 | 4.98 |
| CHEMBL3289572 | — | — | 1 | 4.94 |
| CHEMBL3289574 | — | — | 1 | 4.92 |
| CHEMBL3289567 | — | — | 1 | 4.92 |
| CHEMBL3289584 | — | — | 1 | 4.92 |
| CHEMBL3289577 | — | — | 1 | 4.89 |
| CHEMBL3289573 | — | — | 1 | 4.85 |
| CHEMBL3289579 | — | — | 1 | 4.81 |
| CHEMBL3289571 | — | — | 1 | 4.76 |
| CHEMBL3289292 | — | — | 1 | 4.68 |
| CHEMBL3289291 | — | — | 1 | 4.66 |
| CHEMBL3289294 | — | — | 1 | 4.52 |
| CHEMBL3289293 | — | — | 1 | 4.51 |
| CHEMBL3289290 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3289583 | — | IC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL3289585 | — | IC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL3289575 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL3289296 | — | IC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL3289570 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL3289588 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3289295 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3289568 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL3289587 | — | IC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL3289566 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL3289578 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL3289569 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL3289586 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3289576 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3289582 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3289580 | — | IC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3289581 | — | IC50 | = | 10471.29 | nM | 4.98 |
| CHEMBL3289572 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL3289574 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289567 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289584 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL3289577 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL3289573 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL3289579 | — | IC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL3289571 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL3289292 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL3289291 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL3289294 | — | IC50 | = | 30199.52 | nM | 4.52 |
| CHEMBL3289293 | — | IC50 | = | 30902.95 | nM | 4.51 |
| CHEMBL3289290 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL75035 | — | Inhibition | = | 56.0 | % | - |