Assay Detail
Binding
CHEMBL700341
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Displacement of [3H]kainate from rat brain cortical membrane Ionotropic glutamate receptor kainate
13
Total Activities
13
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 receptor ionotropic, kainate (CHEMBL2094119) ↗| 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 | 13 | 5.16 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293206 | — | — | 1 | 6.44 |
| CHEMBL123196 | — | — | 1 | 5.62 |
| CHEMBL333042 | — | — | 1 | 5.47 |
| CHEMBL286752 | — | — | 1 | 5.36 |
| CHEMBL92456 | — | — | 1 | 5.28 |
| CHEMBL91801 | — | — | 1 | 5.12 |
| CHEMBL123885 | — | — | 1 | 4.92 |
| CHEMBL122339 | — | — | 1 | 4.80 |
| CHEMBL93837 | — | — | 1 | 4.80 |
| CHEMBL123118 | — | — | 1 | 4.66 |
| CHEMBL27503 | — | — | 1 | 4.31 |
| CHEMBL23044 | — | — | 1 | - |
| CHEMBL21641 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293206 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL123196 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL333042 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL286752 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL92456 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL91801 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL123885 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL122339 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL93837 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL123118 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL27503 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL23044 | — | IC50 | = | 15000000.0 | nM | - |
| CHEMBL21641 | — | IC50 | = | 52000000.0 | nM | - |