Assay Detail
Binding
CHEMBL680696
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Concentration required for blocking [14C]glutamate uptake in COS-1 cells expressing human Excitatory amino acid transporter 1
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 | 4.55 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1790042 | — | — | 1 | 4.82 |
| CHEMBL1790043 | — | — | 1 | 4.80 |
| CHEMBL79140 | — | — | 4 | 4.64 |
| CHEMBL475341 | — | — | 1 | 4.32 |
| CHEMBL1790044 | — | — | 1 | 4.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1790042 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1790043 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL79140 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL475341 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL1790044 | — | IC50 | = | 69000.0 | nM | 4.16 |
| CHEMBL79140 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL79140 | — | IC50 | = | 637000.0 | nM | - |
| CHEMBL79140 | — | IC50 | = | 817000.0 | nM | - |