Assay Detail
Binding
CHEMBL2415588
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cells
32
Total Activities
32
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
2-Substituted 4-hydroxybutanamides as potential inhibitors of γ-aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 4.62 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 6.88 |
| CHEMBL2414171 | — | — | 1 | 5.11 |
| CHEMBL2414193 | — | — | 1 | 5.01 |
| CHEMBL2414175 | — | — | 1 | 4.98 |
| CHEMBL2414078 | — | — | 1 | 4.88 |
| CHEMBL2414190 | — | — | 1 | 4.83 |
| CHEMBL2414173 | — | — | 1 | 4.79 |
| CHEMBL2414081 | — | — | 1 | 4.74 |
| CHEMBL2414176 | — | — | 1 | 4.72 |
| CHEMBL2414079 | — | — | 1 | 4.71 |
| CHEMBL2414178 | — | — | 1 | 4.66 |
| CHEMBL2414179 | — | — | 1 | 4.65 |
| CHEMBL2414187 | — | — | 1 | 4.63 |
| CHEMBL2414177 | — | — | 1 | 4.63 |
| CHEMBL2414167 | — | — | 1 | 4.62 |
| CHEMBL2414080 | — | — | 1 | 4.62 |
| CHEMBL2414082 | — | — | 1 | 4.52 |
| CHEMBL2414186 | — | — | 1 | 4.48 |
| CHEMBL2414192 | — | — | 1 | 4.47 |
| CHEMBL2414169 | — | — | 1 | 4.46 |
| CHEMBL2414181 | — | — | 1 | 4.43 |
| CHEMBL2414184 | — | — | 1 | 4.43 |
| CHEMBL2414194 | — | — | 1 | 4.42 |
| CHEMBL2414188 | — | — | 1 | 4.41 |
| CHEMBL2414182 | — | — | 1 | 4.41 |
| CHEMBL2414170 | — | — | 1 | 4.27 |
| CHEMBL2414189 | — | — | 1 | 4.26 |
| CHEMBL2414180 | — | — | 1 | 4.23 |
| CHEMBL2414185 | — | — | 1 | 4.21 |
| CHEMBL2414168 | — | — | 1 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1027 | TIAGABINE | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL2414171 | — | IC50 | = | 7762.47 | nM | 5.11 |
| CHEMBL2414193 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL2414175 | — | IC50 | = | 10471.29 | nM | 4.98 |
| CHEMBL2414078 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL2414190 | — | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL2414173 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL2414081 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL2414176 | — | IC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL2414079 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL2414178 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL2414179 | — | IC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL2414187 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL2414177 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL2414080 | — | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL2414167 | — | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL2414082 | — | IC50 | = | 30199.52 | nM | 4.52 |
| CHEMBL2414186 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL2414192 | — | IC50 | = | 33884.42 | nM | 4.47 |
| CHEMBL2414169 | — | IC50 | = | 34673.69 | nM | 4.46 |
| CHEMBL2414181 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL2414184 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL2414194 | — | IC50 | = | 38018.94 | nM | 4.42 |
| CHEMBL2414188 | — | IC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL2414182 | — | IC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL2414170 | — | IC50 | = | 53703.18 | nM | 4.27 |
| CHEMBL2414189 | — | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL2414180 | — | IC50 | = | 58884.37 | nM | 4.23 |
| CHEMBL2414185 | — | IC50 | = | 61659.5 | nM | 4.21 |
| CHEMBL2414168 | — | IC50 | = | 66069.34 | nM | 4.18 |
| CHEMBL75035 | — | IC50 | = | 85113.8 | nM | 4.07 |
| CHEMBL2414183 | — | IC50 | = | 97723.72 | nM | 4.01 |