Assay Detail
Binding
CHEMBL751729
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-(+)-MK-801 binding to NMDA receptor ion-channel complex of rat cortical memembranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.99 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 6.70 |
| CHEMBL432781 | — | — | 1 | 5.25 |
| CHEMBL110664 | — | — | 1 | 4.93 |
| CHEMBL322916 | — | — | 1 | 4.78 |
| CHEMBL310014 | — | — | 1 | 4.75 |
| CHEMBL110492 | — | — | 1 | 4.37 |
| CHEMBL267276 | TQX-173 | — | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL432781 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL110664 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL322916 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL310014 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL110492 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL267276 | TQX-173 | IC50 | = | 68000.0 | nM | 4.17 |