Assay Detail
Binding
CHEMBL4838604
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]NO711 binding to mouse GAT1 expressed in human HEK293 cell line by MS binding assay
8
Total Activities
8
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
Development of tricyclic N-benzyl-4-hydroxybutanamide derivatives as inhibitors of GABA transporters mGAT1-4 with anticonvulsant, antinociceptive, and antidepressant activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.63 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4595698 | — | — | 1 | 8.29 |
| CHEMBL1027 | TIAGABINE | 4.0 | 1 | 7.43 |
| CHEMBL4861574 | — | — | 1 | 5.14 |
| CHEMBL4852705 | — | — | 1 | 4.96 |
| CHEMBL3289575 | — | — | 1 | 4.96 |
| CHEMBL4859850 | — | — | 1 | 4.87 |
| CHEMBL4854550 | — | — | 1 | 4.78 |
| CHEMBL4873878 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4595698 | — | IC50 | = | 5.129 | nM | 8.29 |
| CHEMBL1027 | TIAGABINE | IC50 | = | 37.15 | nM | 7.43 |
| CHEMBL4861574 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL4852705 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL3289575 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL4859850 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4854550 | — | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL4873878 | — | IC50 | = | 25118.86 | nM | 4.60 |