Assay Detail
Binding
CHEMBL696376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of specific binding of [3H]kainate to Ionotropic glutamate receptor kainate in rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate (CHEMBL2094119) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structure--activity studies for alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid receptors: acidic hydroxyphenylalanines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.46 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 8.27 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.16 |
| CHEMBL155265 | DNQX | — | 1 | 5.66 |
| CHEMBL9790 | — | — | 1 | 5.62 |
| CHEMBL366588 | — | — | 1 | 5.43 |
| CHEMBL108147 | — | — | 1 | 4.47 |
| CHEMBL276815 | (S)-AMPA | — | 1 | 4.04 |
| CHEMBL366489 | — | — | 1 | 4.01 |
| CHEMBL427991 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275040 | KAINIC ACID | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL575060 | GLUTAMIC ACID | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL155265 | DNQX | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL9790 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL366588 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL108147 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL276815 | (S)-AMPA | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL366489 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL427991 | — | IC50 | > | 100000.0 | nM | - |