Assay Detail
Binding
CHEMBL2415587
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Inhibition of mouse GAT3-mediated [3H]GABA uptake stably transfected in HEK293 cells
33
Total Activities
33
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
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 | 33 | 4.59 | 5.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2414176 | — | — | 1 | 5.14 |
| CHEMBL2414177 | — | — | 1 | 5.02 |
| CHEMBL2414178 | — | — | 1 | 4.95 |
| CHEMBL2414179 | — | — | 1 | 4.93 |
| CHEMBL2414182 | — | — | 1 | 4.88 |
| CHEMBL2414175 | — | — | 1 | 4.87 |
| CHEMBL2414187 | — | — | 1 | 4.83 |
| CHEMBL2414181 | — | — | 1 | 4.79 |
| CHEMBL2414186 | — | — | 1 | 4.74 |
| CHEMBL2414184 | — | — | 1 | 4.70 |
| CHEMBL2414171 | — | — | 1 | 4.66 |
| CHEMBL2414188 | — | — | 1 | 4.64 |
| CHEMBL2414189 | — | — | 1 | 4.63 |
| CHEMBL2414173 | — | — | 1 | 4.57 |
| CHEMBL2414193 | — | — | 1 | 4.55 |
| CHEMBL2413090 | — | — | 1 | 4.54 |
| CHEMBL2414167 | — | — | 1 | 4.51 |
| CHEMBL2414192 | — | — | 1 | 4.49 |
| CHEMBL2414180 | — | — | 1 | 4.49 |
| CHEMBL2414080 | — | — | 1 | 4.49 |
| CHEMBL2414170 | — | — | 1 | 4.48 |
| CHEMBL2414194 | — | — | 1 | 4.48 |
| CHEMBL2414081 | — | — | 1 | 4.46 |
| CHEMBL2414185 | — | — | 1 | 4.45 |
| CHEMBL2414079 | — | — | 1 | 4.44 |
| CHEMBL2414190 | — | — | 1 | 4.43 |
| CHEMBL2414183 | — | — | 1 | 4.41 |
| CHEMBL2414078 | — | — | 1 | 4.38 |
| CHEMBL2414082 | — | — | 1 | 4.37 |
| CHEMBL2414168 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2414176 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL2414177 | — | IC50 | = | 9549.93 | nM | 5.02 |
| CHEMBL2414178 | — | IC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL2414179 | — | IC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL2414182 | — | IC50 | = | 13182.57 | nM | 4.88 |
| CHEMBL2414175 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL2414187 | — | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL2414181 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL2414186 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL2414184 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL2414171 | — | IC50 | = | 21877.62 | nM | 4.66 |
| CHEMBL2414188 | — | IC50 | = | 22908.68 | nM | 4.64 |
| CHEMBL2414189 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL2414173 | — | IC50 | = | 26915.35 | nM | 4.57 |
| CHEMBL2414193 | — | IC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL2413090 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL2414167 | — | IC50 | = | 30902.95 | nM | 4.51 |
| CHEMBL2414192 | — | IC50 | = | 32359.37 | nM | 4.49 |
| CHEMBL2414180 | — | IC50 | = | 32359.37 | nM | 4.49 |
| CHEMBL2414080 | — | IC50 | = | 32359.37 | nM | 4.49 |
| CHEMBL2414170 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL2414194 | — | IC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL2414081 | — | IC50 | = | 34673.69 | nM | 4.46 |
| CHEMBL2414185 | — | IC50 | = | 35481.34 | nM | 4.45 |
| CHEMBL2414079 | — | IC50 | = | 36307.81 | nM | 4.44 |
| CHEMBL2414190 | — | IC50 | = | 37153.52 | nM | 4.43 |
| CHEMBL2414183 | — | IC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL2414078 | — | IC50 | = | 41686.94 | nM | 4.38 |
| CHEMBL2414082 | — | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL2414168 | — | IC50 | = | 42657.95 | nM | 4.37 |
| CHEMBL2414169 | — | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL2414191 | — | IC50 | = | 56234.13 | nM | 4.25 |
| CHEMBL2414174 | — | IC50 | = | 57543.99 | nM | 4.24 |