Assay Detail
Binding
CHEMBL881963
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Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 2
28
Total Activities
27
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 | Expert |
Publication
Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.46 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113122 | — | — | 1 | 7.22 |
| CHEMBL2113115 | — | — | 1 | 7.10 |
| CHEMBL1628669 | — | — | 1 | 7.10 |
| CHEMBL2113112 | — | — | 1 | 7.00 |
| CHEMBL2113126 | — | — | 1 | 7.00 |
| CHEMBL2113116 | — | — | 1 | 7.00 |
| CHEMBL2113119 | — | — | 1 | 7.00 |
| CHEMBL2113110 | — | — | 1 | 7.00 |
| CHEMBL2113121 | — | — | 1 | 6.89 |
| CHEMBL424838 | — | — | 1 | 6.70 |
| CHEMBL2113113 | — | — | 1 | 6.70 |
| CHEMBL2113125 | — | — | 1 | 6.70 |
| CHEMBL2113117 | — | — | 1 | 6.70 |
| CHEMBL425569 | — | — | 1 | 6.52 |
| CHEMBL2113118 | — | — | 1 | 6.52 |
| CHEMBL2113124 | — | — | 1 | 6.52 |
| CHEMBL2113128 | — | — | 1 | 6.52 |
| CHEMBL2113123 | — | — | 1 | 6.40 |
| CHEMBL2113120 | — | — | 1 | 6.30 |
| CHEMBL373283 | — | — | 1 | 6.30 |
| CHEMBL2113111 | — | — | 1 | 6.22 |
| CHEMBL198315 | — | — | 1 | 6.16 |
| CHEMBL2113114 | — | — | 2 | 6.16 |
| CHEMBL1628570 | — | — | 1 | 6.16 |
| CHEMBL2113127 | — | — | 1 | 6.00 |
| CHEMBL2113129 | — | — | 1 | 6.00 |
| CHEMBL2113130 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113122 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2113115 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1628669 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2113112 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113126 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113116 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113119 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113110 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2113121 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL424838 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2113113 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2113125 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2113117 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2113128 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2113118 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2113124 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL425569 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2113123 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2113120 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL373283 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2113111 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL198315 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2113114 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1628570 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2113127 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2113129 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2113130 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2113114 | — | IC50 | = | 67000.0 | nM | 4.17 |