Assay Detail
Functional
CHEMBL907701
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Inhibition of human EAAT2 expressed in HEK293 cells by FLIPR membrane potential assay
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 4.94 | 5.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL384474 | — | — | 2 | 5.20 |
| CHEMBL217407 | — | — | 2 | 4.70 |
| CHEMBL2373300 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL384474 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL384474 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL217407 | — | Ki | = | 19952.62 | nM | 4.70 |
| CHEMBL217407 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL2373300 | — | Ki | = | 110000.0 | nM | - |
| CHEMBL2373300 | — | Ki | = | 125892.54 | nM | - |