Assay Detail
Binding
CHEMBL881964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 3
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 | 5.90 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113115 | — | — | 1 | 7.30 |
| CHEMBL2113112 | — | — | 1 | 6.85 |
| CHEMBL2113116 | — | — | 1 | 6.70 |
| CHEMBL2113111 | — | — | 1 | 6.52 |
| CHEMBL1628570 | — | — | 1 | 6.38 |
| CHEMBL2113118 | — | — | 1 | 6.35 |
| CHEMBL2113122 | — | — | 1 | 6.30 |
| CHEMBL424838 | — | — | 1 | 6.22 |
| CHEMBL2113113 | — | — | 1 | 6.22 |
| CHEMBL2113123 | — | — | 1 | 6.22 |
| CHEMBL2113117 | — | — | 1 | 6.19 |
| CHEMBL2113126 | — | — | 1 | 6.07 |
| CHEMBL198315 | — | — | 1 | 6.00 |
| CHEMBL373283 | — | — | 1 | 6.00 |
| CHEMBL425569 | — | — | 1 | 6.00 |
| CHEMBL2113125 | — | — | 1 | 5.82 |
| CHEMBL2113120 | — | — | 1 | 5.75 |
| CHEMBL2113130 | — | — | 1 | 5.70 |
| CHEMBL2113119 | — | — | 1 | 5.62 |
| CHEMBL2113124 | — | — | 1 | 5.52 |
| CHEMBL2113128 | — | — | 1 | 5.52 |
| CHEMBL1628669 | — | — | 1 | 5.42 |
| CHEMBL2113127 | — | — | 1 | 5.30 |
| CHEMBL2113114 | — | — | 2 | 5.25 |
| CHEMBL2113129 | — | — | 1 | 5.05 |
| CHEMBL2113110 | — | — | 1 | 5.00 |
| CHEMBL2113121 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113115 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2113112 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2113116 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2113111 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1628570 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2113118 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2113122 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL424838 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2113113 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2113123 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL2113117 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2113126 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL373283 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL198315 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL425569 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2113125 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2113120 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2113130 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2113119 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2113124 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2113128 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1628669 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL2113127 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2113114 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL2113114 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2113129 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL2113110 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2113121 | — | IC50 | = | 14500.0 | nM | 4.84 |