Assay Detail
Functional
CHEMBL740058
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Concentration necessary for 50% inhibition of depolarization induced by 5 uM S-AMPA in mouse cortical wedge preparation
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
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 |
|---|---|---|---|
| IC50 | 11 | 5.63 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 6.70 |
| CHEMBL90242 | — | — | 1 | 6.10 |
| CHEMBL328935 | — | — | 1 | 6.00 |
| CHEMBL91115 | — | — | 1 | 6.00 |
| CHEMBL91677 | — | — | 1 | 5.89 |
| CHEMBL328272 | — | — | 1 | 5.82 |
| CHEMBL267276 | TQX-173 | — | 1 | 5.64 |
| CHEMBL90722 | — | — | 1 | 5.51 |
| CHEMBL93076 | — | — | 1 | 5.11 |
| CHEMBL327894 | — | — | 1 | 4.92 |
| CHEMBL50267 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL90242 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL328935 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL91115 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL91677 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL328272 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL267276 | TQX-173 | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL90722 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL93076 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL327894 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL50267 | — | IC50 | = | 52000.0 | nM | 4.28 |