Assay Detail
Binding
CHEMBL4767586
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NO711 from mouse GAT1 expressed in HEK293 cells measured after 40 mins of incubation by LC-ESI-MS-MS method
13
Total Activities
13
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 mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 4.88 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4595698 | — | — | 1 | 8.29 |
| CHEMBL3289575 | — | — | 1 | 4.96 |
| CHEMBL4780692 | — | — | 1 | 4.93 |
| CHEMBL4796172 | — | — | 1 | 4.74 |
| CHEMBL4795631 | — | — | 1 | 4.73 |
| CHEMBL4785506 | — | — | 1 | 4.70 |
| CHEMBL4798908 | — | — | 1 | 4.66 |
| CHEMBL4792403 | — | — | 1 | 4.61 |
| CHEMBL4780841 | — | — | 1 | 4.59 |
| CHEMBL4791795 | — | — | 1 | 4.42 |
| CHEMBL4777433 | — | — | 1 | 4.41 |
| CHEMBL4787408 | — | — | 1 | 4.29 |
| CHEMBL4779532 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4595698 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL3289575 | — | Ki | = | 10964.78 | nM | 4.96 |
| CHEMBL4780692 | — | Ki | = | 11748.98 | nM | 4.93 |
| CHEMBL4796172 | — | Ki | = | 18197.01 | nM | 4.74 |
| CHEMBL4795631 | — | Ki | = | 18620.87 | nM | 4.73 |
| CHEMBL4785506 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL4798908 | — | Ki | = | 21877.62 | nM | 4.66 |
| CHEMBL4792403 | — | Ki | = | 24547.09 | nM | 4.61 |
| CHEMBL4780841 | — | Ki | = | 25703.96 | nM | 4.59 |
| CHEMBL4791795 | — | Ki | = | 38018.94 | nM | 4.42 |
| CHEMBL4777433 | — | Ki | = | 38904.51 | nM | 4.41 |
| CHEMBL4787408 | — | Ki | = | 51286.14 | nM | 4.29 |
| CHEMBL4779532 | — | Ki | = | 87096.36 | nM | 4.06 |