Assay Detail
Binding
CHEMBL701547
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of the specific binding of [3H]AMPA to Ionotropic glutamate receptor AMPA in rat whole brain membranes in the presence of 100 uM KSCN
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.21 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13260 | YM-90K | — | 1 | 7.08 |
| CHEMBL27653 | — | — | 1 | 6.85 |
| CHEMBL25922 | — | — | 1 | 6.16 |
| CHEMBL26699 | — | — | 1 | 6.07 |
| CHEMBL282417 | — | — | 1 | 6.04 |
| CHEMBL286752 | — | — | 1 | 5.96 |
| CHEMBL27715 | — | — | 1 | 5.80 |
| CHEMBL23044 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13260 | YM-90K | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL27653 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL25922 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL26699 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL282417 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL286752 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL27715 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL23044 | — | Ki | = | 2000.0 | nM | 5.70 |