Assay Detail
Binding
CHEMBL752330
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Displacement of [3H]DCKA at N-methyl-D-aspartate glutamate receptor 1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| 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 | 11 | 5.89 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.23 |
| CHEMBL293206 | — | — | 1 | 6.43 |
| CHEMBL92456 | — | — | 1 | 6.09 |
| CHEMBL286752 | — | — | 1 | 5.96 |
| CHEMBL308941 | — | — | 1 | 5.80 |
| CHEMBL21641 | — | — | 1 | 5.75 |
| CHEMBL93837 | — | — | 1 | 5.72 |
| CHEMBL123118 | — | — | 1 | 5.66 |
| CHEMBL23044 | — | — | 1 | 5.42 |
| CHEMBL122339 | — | — | 1 | 5.39 |
| CHEMBL27503 | — | — | 1 | 4.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289832 | LICOSTINEL | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL293206 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL92456 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL286752 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL308941 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL21641 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL93837 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL123118 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL23044 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL122339 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL27503 | — | IC50 | = | 41000.0 | nM | 4.39 |