Assay Detail
Binding
CHEMBL680698
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Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 2
8
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.34 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1790042 | — | — | 1 | 5.89 |
| CHEMBL1790044 | — | — | 1 | 5.70 |
| CHEMBL1790043 | — | — | 1 | 5.66 |
| CHEMBL79140 | — | — | 4 | 5.42 |
| CHEMBL475341 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1790042 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1790044 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1790043 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL79140 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL475341 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL79140 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL79140 | — | IC50 | = | 221000.0 | nM | - |
| CHEMBL79140 | — | IC50 | = | 164000.0 | nM | - |