Assay Detail
Binding
CHEMBL3294685
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1 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 |
Target
Sodium- and chloride-dependent GABA transporter 1 (CHEMBL5445) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 4.76 | 5.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3289578 | — | — | 1 | 5.07 |
| CHEMBL3289581 | — | — | 1 | 4.96 |
| CHEMBL3289579 | — | — | 1 | 4.96 |
| CHEMBL3289582 | — | — | 1 | 4.96 |
| CHEMBL3289586 | — | — | 1 | 4.95 |
| CHEMBL3289583 | — | — | 1 | 4.95 |
| CHEMBL3289573 | — | — | 1 | 4.91 |
| CHEMBL3289570 | — | — | 1 | 4.90 |
| CHEMBL3289575 | — | — | 1 | 4.89 |
| CHEMBL3289576 | — | — | 1 | 4.89 |
| CHEMBL3289588 | — | — | 1 | 4.88 |
| CHEMBL3289580 | — | — | 1 | 4.87 |
| CHEMBL3289577 | — | — | 1 | 4.86 |
| CHEMBL3289585 | — | — | 1 | 4.86 |
| CHEMBL3289587 | — | — | 1 | 4.80 |
| CHEMBL3289296 | — | — | 1 | 4.80 |
| CHEMBL3289566 | — | — | 1 | 4.78 |
| CHEMBL3289572 | — | — | 1 | 4.78 |
| CHEMBL3289571 | — | — | 1 | 4.76 |
| CHEMBL3289574 | — | — | 1 | 4.73 |
| CHEMBL3289568 | — | — | 1 | 4.71 |
| CHEMBL3289584 | — | — | 1 | 4.71 |
| CHEMBL3289291 | — | — | 1 | 4.68 |
| CHEMBL3289569 | — | — | 1 | 4.65 |
| CHEMBL3289293 | — | — | 1 | 4.63 |
| CHEMBL3289292 | — | — | 1 | 4.59 |
| CHEMBL3289567 | — | — | 1 | 4.56 |
| CHEMBL3289294 | — | — | 1 | 4.55 |
| CHEMBL3289295 | — | — | 1 | 4.51 |
| CHEMBL3289290 | — | — | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3289578 | — | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL3289581 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL3289579 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL3289582 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL3289586 | — | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL3289583 | — | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL3289573 | — | IC50 | = | 12302.69 | nM | 4.91 |
| CHEMBL3289570 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3289575 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL3289576 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL3289588 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL3289580 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL3289577 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL3289585 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL3289587 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3289296 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3289566 | — | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL3289572 | — | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL3289571 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL3289574 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL3289568 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL3289584 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL3289291 | — | IC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL3289569 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL3289293 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL3289292 | — | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL3289567 | — | IC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL3289294 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL3289295 | — | IC50 | = | 30902.95 | nM | 4.51 |
| CHEMBL3289290 | — | IC50 | = | 44668.36 | nM | 4.35 |
| CHEMBL75035 | — | IC50 | = | 85113.8 | nM | 4.07 |