Assay Detail
Binding
CHEMBL1016591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]D-Asp uptake at human EAAT2 in HEK293 cells
22
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 4.11 | 4.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 2 | 4.21 |
| CHEMBL480169 | — | — | 2 | 4.02 |
| CHEMBL518313 | — | — | 2 | - |
| CHEMBL494878 | — | — | 2 | - |
| CHEMBL500042 | — | — | 2 | - |
| CHEMBL479804 | — | — | 2 | - |
| CHEMBL482080 | — | — | 2 | - |
| CHEMBL482081 | — | — | 2 | - |
| CHEMBL479797 | — | — | 2 | - |
| CHEMBL446256 | — | — | 2 | - |
| CHEMBL500448 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 62000.0 | nM | 4.21 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 63095.73 | nM | 4.20 |
| CHEMBL480169 | — | Ki | = | 95000.0 | nM | 4.02 |
| CHEMBL480169 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL518313 | — | Ki | = | 410000.0 | nM | - |
| CHEMBL518313 | — | Ki | = | 398107.17 | nM | - |
| CHEMBL494878 | — | Ki | = | 1000000.0 | nM | - |
| CHEMBL494878 | — | Ki | = | 3162277.66 | nM | - |
| CHEMBL500042 | — | Ki | = | 680000.0 | nM | - |
| CHEMBL500042 | — | Ki | = | 630957.34 | nM | - |
| CHEMBL479804 | — | Ki | = | 290000.0 | nM | - |
| CHEMBL479804 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL482080 | — | Ki | = | 180000.0 | nM | - |
| CHEMBL482080 | — | Ki | = | 158489.32 | nM | - |
| CHEMBL482081 | — | Ki | > | 3000000.0 | nM | - |
| CHEMBL482081 | — | Ki | > | 3162277.66 | nM | - |
| CHEMBL479797 | — | Ki | > | 3000000.0 | nM | - |
| CHEMBL479797 | — | Ki | > | 3162277.66 | nM | - |
| CHEMBL446256 | — | Ki | = | 290000.0 | nM | - |
| CHEMBL446256 | — | Ki | = | 316227.77 | nM | - |
| CHEMBL500448 | — | Ki | = | 140000.0 | nM | - |
| CHEMBL500448 | — | Ki | = | 125892.54 | nM | - |