Assay Detail
Binding
CHEMBL1016589
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Inhibition of glutamate-induced depolarization in human EAAT3 expressed in HEK293 cells by FMP assay
24
Total Activities
12
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 |
|---|---|---|---|
| IC50 | 24 | 5.02 | 5.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475341 | — | — | 2 | 5.03 |
| CHEMBL500448 | — | — | 2 | - |
| CHEMBL279561 | DIHYDROKAINATE | — | 2 | - |
| CHEMBL480169 | — | — | 2 | - |
| CHEMBL518313 | — | — | 2 | - |
| CHEMBL494878 | — | — | 2 | - |
| CHEMBL500042 | — | — | 2 | - |
| CHEMBL479804 | — | — | 2 | - |
| CHEMBL482080 | — | — | 2 | - |
| CHEMBL482081 | — | — | 2 | - |
| CHEMBL479797 | — | — | 2 | - |
| CHEMBL446256 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475341 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL475341 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL500448 | — | IC50 | = | 3162277.66 | nM | - |
| CHEMBL279561 | DIHYDROKAINATE | IC50 | > | 3000000.0 | nM | - |
| CHEMBL279561 | DIHYDROKAINATE | IC50 | > | 3162277.66 | nM | - |
| CHEMBL480169 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL480169 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL518313 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL518313 | — | IC50 | = | 1000000.0 | nM | - |
| CHEMBL494878 | — | IC50 | = | 3000000.0 | nM | - |
| CHEMBL494878 | — | IC50 | = | 3162277.66 | nM | - |
| CHEMBL500448 | — | IC50 | = | 3000000.0 | nM | - |
| CHEMBL500042 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL479804 | — | IC50 | > | 3000000.0 | nM | - |
| CHEMBL479804 | — | IC50 | = | 3162277.66 | nM | - |
| CHEMBL482080 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL482080 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL482081 | — | IC50 | = | 3000000.0 | nM | - |
| CHEMBL482081 | — | IC50 | = | 3162277.66 | nM | - |
| CHEMBL479797 | — | IC50 | > | 3000000.0 | nM | - |
| CHEMBL479797 | — | IC50 | > | 3162277.66 | nM | - |
| CHEMBL446256 | — | IC50 | = | 3000000.0 | nM | - |
| CHEMBL446256 | — | IC50 | = | 3162277.66 | nM | - |
| CHEMBL500042 | — | IC50 | > | 1000000.0 | nM | - |