Assay Detail
Binding
CHEMBL697881
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Binding affinity in rat brain cortical membranes by the displacement of [3H]AMPA at Ionotropic glutamate receptor AMPA
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.25 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 7.28 |
| CHEMBL293206 | — | — | 1 | 7.20 |
| CHEMBL123196 | — | — | 1 | 5.89 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 5.82 |
| CHEMBL286752 | — | — | 1 | 5.48 |
| CHEMBL91801 | — | — | 1 | 5.23 |
| CHEMBL333042 | — | — | 1 | 5.17 |
| CHEMBL23044 | — | — | 1 | 5.11 |
| CHEMBL92456 | — | — | 1 | 5.00 |
| CHEMBL308941 | — | — | 1 | 4.89 |
| CHEMBL123885 | — | — | 1 | 4.85 |
| CHEMBL93837 | — | — | 1 | 4.75 |
| CHEMBL122339 | — | — | 1 | 4.50 |
| CHEMBL123118 | — | — | 1 | 4.42 |
| CHEMBL21641 | — | — | 1 | 4.28 |
| CHEMBL27503 | — | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL293206 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL123196 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL286752 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL91801 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL333042 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL23044 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL92456 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL308941 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL123885 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL93837 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL122339 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL123118 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL21641 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL27503 | — | IC50 | = | 67000.0 | nM | 4.17 |