Assay Detail
Binding
CHEMBL702546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards ionotropic glutamate receptor (high-affinity) of rat cortical synaptic membranes by using [3H]AMPA as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 6.34 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90251 | — | — | 1 | 7.72 |
| CHEMBL91677 | — | — | 1 | 7.43 |
| CHEMBL93649 | — | — | 1 | 7.17 |
| CHEMBL222519 | NBQX | — | 1 | 7.16 |
| CHEMBL328935 | — | — | 1 | 7.06 |
| CHEMBL90242 | — | — | 1 | 7.02 |
| CHEMBL327936 | — | — | 1 | 6.92 |
| CHEMBL91115 | — | — | 1 | 6.92 |
| CHEMBL267276 | TQX-173 | — | 1 | 6.85 |
| CHEMBL90722 | — | — | 1 | 6.75 |
| CHEMBL327894 | — | — | 1 | 6.70 |
| CHEMBL328272 | — | — | 1 | 6.55 |
| CHEMBL94232 | — | — | 1 | 6.46 |
| CHEMBL89957 | — | — | 1 | 6.46 |
| CHEMBL93076 | — | — | 1 | 6.43 |
| CHEMBL93584 | — | — | 1 | 6.19 |
| CHEMBL92005 | — | — | 1 | 6.16 |
| CHEMBL314956 | — | — | 1 | 6.16 |
| CHEMBL90484 | — | — | 1 | 5.94 |
| CHEMBL90940 | — | — | 1 | 5.92 |
| CHEMBL330349 | — | — | 1 | 5.92 |
| CHEMBL433392 | — | — | 1 | 5.85 |
| CHEMBL327764 | — | — | 1 | 5.66 |
| CHEMBL90705 | — | — | 1 | 5.63 |
| CHEMBL313638 | — | — | 1 | 5.26 |
| CHEMBL92433 | — | — | 1 | 5.19 |
| CHEMBL327361 | — | — | 1 | 5.05 |
| CHEMBL328353 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90251 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL91677 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL93649 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL222519 | NBQX | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL328935 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL90242 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL327936 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL91115 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL267276 | TQX-173 | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL90722 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL327894 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL328272 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL94232 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL89957 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL93076 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL93584 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL92005 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL314956 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL90484 | — | Ki | = | 1140.0 | nM | 5.94 |
| CHEMBL90940 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL330349 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL433392 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL327764 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL90705 | — | Ki | = | 2350.0 | nM | 5.63 |
| CHEMBL313638 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL92433 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL327361 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL328353 | — | Ki | = | 12800.0 | nM | 4.89 |