Assay Detail
Binding
CHEMBL752487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potency for the N-methyl-D-aspartate glutamate receptor 1 glycine site by displacement of [3H]5,7-dichlorokynurenic acid (DCKA) binding in rat brain cortical membranes.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4-dihydroquinoxaline-2,3-diones: potent and systemically active antagonists for the glycine site of the NMDA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.26 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297881 | — | — | 1 | 8.33 |
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.23 |
| CHEMBL42426 | — | — | 1 | 8.06 |
| CHEMBL136833 | — | — | 1 | 7.70 |
| CHEMBL40652 | — | — | 1 | 7.54 |
| CHEMBL41460 | — | — | 1 | 7.54 |
| CHEMBL41691 | — | — | 1 | 7.35 |
| CHEMBL42248 | — | — | 1 | 7.19 |
| CHEMBL288839 | — | — | 1 | 7.14 |
| CHEMBL291149 | — | — | 1 | 7.09 |
| CHEMBL291148 | — | — | 1 | 7.02 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | — | 1 | 6.89 |
| CHEMBL40745 | — | — | 1 | 6.89 |
| CHEMBL42466 | — | — | 1 | 6.82 |
| CHEMBL295995 | — | — | 1 | 6.82 |
| CHEMBL41295 | — | — | 1 | 6.80 |
| CHEMBL41399 | — | — | 1 | 6.19 |
| CHEMBL288384 | — | — | 1 | 6.11 |
| CHEMBL553334 | — | — | 1 | 6.00 |
| CHEMBL42482 | — | — | 1 | 5.85 |
| CHEMBL44260 | — | — | 1 | 5.75 |
| CHEMBL40649 | — | — | 1 | 5.72 |
| CHEMBL290747 | — | — | 1 | 5.55 |
| CHEMBL296521 | — | — | 1 | 5.51 |
| CHEMBL22720 | — | — | 1 | 5.48 |
| CHEMBL44018 | — | — | 1 | 5.44 |
| CHEMBL42307 | — | — | 1 | 5.40 |
| CHEMBL43122 | — | — | 1 | 5.37 |
| CHEMBL298284 | — | — | 1 | 5.03 |
| CHEMBL43848 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297881 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL289832 | LICOSTINEL | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL42426 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL136833 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL40652 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL41460 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL41691 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL42248 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL288839 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL291149 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL291148 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL284028 | 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL40745 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL42466 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL295995 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL41295 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL41399 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL288384 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL553334 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL42482 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL44260 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL40649 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL290747 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL296521 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL22720 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL44018 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL42307 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL43122 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL298284 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL43848 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL442545 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL43869 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL42430 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL42367 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL295427 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL43910 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL43875 | — | IC50 | > | 100000.0 | nM | - |