Assay Detail
Binding
CHEMBL748105
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at glycine binding site of NMDA receptor in rat cortical membranes by [3H]L-689,560 displacement.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.77 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299281 | — | — | 1 | 9.12 |
| CHEMBL59894 | — | — | 1 | 9.00 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.85 |
| CHEMBL450325 | — | — | 1 | 8.59 |
| CHEMBL293831 | — | — | 1 | 8.51 |
| CHEMBL62164 | — | — | 1 | 8.40 |
| CHEMBL61720 | — | — | 1 | 8.36 |
| CHEMBL292810 | — | — | 1 | 8.30 |
| CHEMBL61364 | — | — | 1 | 8.22 |
| CHEMBL303539 | — | — | 1 | 8.12 |
| CHEMBL304436 | — | — | 1 | 7.64 |
| CHEMBL58446 | — | — | 1 | 7.62 |
| CHEMBL60822 | — | — | 1 | 7.60 |
| CHEMBL59251 | — | — | 1 | 7.52 |
| CHEMBL59161 | — | — | 1 | 7.11 |
| CHEMBL58182 | — | — | 1 | 7.09 |
| CHEMBL304459 | — | — | 1 | 6.96 |
| CHEMBL292113 | — | — | 1 | 6.72 |
| CHEMBL283819 | — | — | 1 | 5.92 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299281 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL59894 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL450325 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL293831 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL62164 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL61720 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL292810 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL61364 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL303539 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL304436 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL58446 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL60822 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL59251 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL59161 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL58182 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL304459 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL292113 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL283819 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | IC50 | = | 2000.0 | nM | 5.70 |