Assay Detail
Binding
CHEMBL3825097
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Antagonist activity at human iGluA1 receptor flip isoform expressed in CHO-S cells assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 NW dye based fluorescence imaging plate reader method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-S |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.61 | 5.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1214124 | PERAMPANEL | 4.0 | 1 | 5.19 |
| CHEMBL3822825 | — | — | 1 | 5.03 |
| CHEMBL3823247 | — | — | 1 | 5.03 |
| CHEMBL3823817 | — | — | 1 | 5.03 |
| CHEMBL3824269 | — | — | 1 | 5.03 |
| CHEMBL3824102 | — | — | 1 | 5.03 |
| CHEMBL3823222 | — | — | 1 | 4.08 |
| CHEMBL3822572 | — | — | 1 | 4.08 |
| CHEMBL3823445 | — | — | 1 | 4.08 |
| CHEMBL3823351 | — | — | 1 | 4.08 |
| CHEMBL3823394 | — | — | 1 | 4.08 |
| CHEMBL3823441 | — | — | 1 | - |
| CHEMBL3823274 | — | — | 1 | - |
| CHEMBL3823956 | — | — | 1 | - |
| CHEMBL3823131 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1214124 | PERAMPANEL | IC50 | = | 6510.0 | nM | 5.19 |
| CHEMBL3822825 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3823247 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3823817 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3824269 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3824102 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3823222 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL3822572 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL3823445 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL3823351 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL3823394 | — | IC50 | = | 83300.0 | nM | 4.08 |
| CHEMBL3823441 | — | IC50 | > | 83300.0 | nM | - |
| CHEMBL3823274 | — | IC50 | > | 83300.0 | nM | - |
| CHEMBL3823956 | — | IC50 | > | 83300.0 | nM | - |
| CHEMBL3823131 | — | IC50 | > | 83300.0 | nM | - |