Assay Detail
Binding
CHEMBL752502
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards N-methyl-D-aspartate glutamate receptor 1 (high affinity) of rat cortical synaptic membranes by using [3H]Gly as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| 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 | 21 | 4.87 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50267 | — | — | 1 | 7.05 |
| CHEMBL90940 | — | — | 1 | 5.82 |
| CHEMBL91115 | — | — | 1 | 5.58 |
| CHEMBL92005 | — | — | 1 | 5.57 |
| CHEMBL90242 | — | — | 1 | 5.44 |
| CHEMBL330349 | — | — | 1 | 5.43 |
| CHEMBL90705 | — | — | 1 | 5.36 |
| CHEMBL313638 | — | — | 1 | 5.26 |
| CHEMBL328272 | — | — | 1 | 5.08 |
| CHEMBL328353 | — | — | 1 | 4.96 |
| CHEMBL327936 | — | — | 1 | 4.47 |
| CHEMBL267276 | TQX-173 | — | 1 | 4.47 |
| CHEMBL91677 | — | — | 1 | 4.46 |
| CHEMBL89957 | — | — | 1 | 4.27 |
| CHEMBL327361 | — | — | 1 | 4.21 |
| CHEMBL90484 | — | — | 1 | 4.20 |
| CHEMBL328935 | — | — | 1 | 4.19 |
| CHEMBL93076 | — | — | 1 | 4.15 |
| CHEMBL327764 | — | — | 1 | 4.12 |
| CHEMBL433392 | — | — | 1 | 4.08 |
| CHEMBL92433 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50267 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL90940 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL91115 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL92005 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL90242 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL330349 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL90705 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL313638 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL328272 | — | Ki | = | 8300.0 | nM | 5.08 |
| CHEMBL328353 | — | Ki | = | 10900.0 | nM | 4.96 |
| CHEMBL327936 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL267276 | TQX-173 | Ki | = | 33500.0 | nM | 4.47 |
| CHEMBL91677 | — | Ki | = | 35000.0 | nM | 4.46 |
| CHEMBL89957 | — | Ki | = | 54000.0 | nM | 4.27 |
| CHEMBL327361 | — | Ki | = | 62000.0 | nM | 4.21 |
| CHEMBL90484 | — | Ki | = | 63000.0 | nM | 4.20 |
| CHEMBL328935 | — | Ki | = | 65000.0 | nM | 4.19 |
| CHEMBL93076 | — | Ki | = | 71000.0 | nM | 4.15 |
| CHEMBL327764 | — | Ki | = | 75000.0 | nM | 4.12 |
| CHEMBL433392 | — | Ki | = | 84000.0 | nM | 4.08 |
| CHEMBL92433 | — | Ki | = | 85000.0 | nM | 4.07 |