Assay Detail
Binding
CHEMBL4371734
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NO711 binding to mouse GAT1 expressed in HEK293 cell membranes assessed as residual binding preincubated for 4 hrs followed by NO711 addition and measured after 40 mins by LC-ESI-MS/MS analysis
17
Total Activities
17
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
Novel Allosteric Ligands of γ-Aminobutyric Acid Transporter 1 (GAT1) by MS Based Screening of Pseudostatic Hydrazone Libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.19 | 7.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.56 |
| CHEMBL4525620 | — | — | 1 | 6.67 |
| CHEMBL4537310 | — | — | 1 | 6.61 |
| CHEMBL4560424 | — | — | 1 | 6.35 |
| CHEMBL4563656 | — | — | 1 | 6.33 |
| CHEMBL4526583 | — | — | 1 | 6.32 |
| CHEMBL4436249 | — | — | 1 | 6.21 |
| CHEMBL4539491 | — | — | 1 | 6.19 |
| CHEMBL4448463 | — | — | 1 | 6.15 |
| CHEMBL4468482 | — | — | 1 | 6.03 |
| CHEMBL4456820 | — | — | 1 | 6.02 |
| CHEMBL4573932 | — | — | 1 | 5.91 |
| CHEMBL4539900 | — | — | 1 | 5.90 |
| CHEMBL4457922 | — | — | 1 | 5.84 |
| CHEMBL4450658 | — | — | 1 | 5.83 |
| CHEMBL4570110 | — | — | 1 | 5.73 |
| CHEMBL4455881 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL4525620 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL4537310 | — | Ki | = | 245.47 | nM | 6.61 |
| CHEMBL4560424 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL4563656 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL4526583 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL4436249 | — | Ki | = | 616.6 | nM | 6.21 |
| CHEMBL4539491 | — | Ki | = | 645.65 | nM | 6.19 |
| CHEMBL4448463 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL4468482 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL4456820 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL4573932 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL4539900 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4457922 | — | Ki | = | 1445.44 | nM | 5.84 |
| CHEMBL4450658 | — | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL4570110 | — | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL4455881 | — | Ki | = | 2290.87 | nM | 5.64 |