Assay Detail
Binding
CHEMBL752332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro ability to displace [3H]L-689,560 binding to glycine site on the N-methyl-D-aspartate (NMDA) glutamate receptor 1 from rat cortical membranes
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.07 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31741 | — | — | 1 | 8.70 |
| CHEMBL165371 | — | — | 1 | 7.62 |
| CHEMBL350204 | — | — | 1 | 6.96 |
| CHEMBL349719 | — | — | 1 | 6.80 |
| CHEMBL31661 | — | — | 1 | 6.77 |
| CHEMBL167764 | — | — | 1 | 6.77 |
| CHEMBL165449 | — | — | 1 | 6.72 |
| CHEMBL423099 | — | — | 1 | 6.62 |
| CHEMBL351884 | — | — | 1 | 6.57 |
| CHEMBL165149 | — | — | 1 | 6.50 |
| CHEMBL165383 | — | — | 1 | 6.38 |
| CHEMBL163646 | — | — | 1 | 6.38 |
| CHEMBL352332 | — | — | 1 | 6.30 |
| CHEMBL166246 | — | — | 1 | 6.24 |
| CHEMBL164930 | — | — | 1 | 6.12 |
| CHEMBL165378 | — | — | 1 | 6.11 |
| CHEMBL349038 | — | — | 1 | 6.05 |
| CHEMBL164831 | — | — | 1 | 5.96 |
| CHEMBL166034 | — | — | 1 | 5.96 |
| CHEMBL433908 | — | — | 1 | 5.92 |
| CHEMBL164184 | — | — | 1 | 5.92 |
| CHEMBL351441 | — | — | 1 | 5.77 |
| CHEMBL165360 | — | — | 1 | 5.70 |
| CHEMBL352889 | — | — | 1 | 5.57 |
| CHEMBL89086 | — | — | 1 | 5.55 |
| CHEMBL167201 | — | — | 1 | 5.50 |
| CHEMBL353570 | — | — | 1 | 5.50 |
| CHEMBL164342 | — | — | 1 | 5.46 |
| CHEMBL168042 | — | — | 1 | 5.38 |
| CHEMBL335431 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31741 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL165371 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL350204 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL349719 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL31661 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL167764 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL165449 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL423099 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL351884 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL165149 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL165383 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL163646 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL352332 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL166246 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL164930 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL165378 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL349038 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL164831 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL166034 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL433908 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL164184 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL351441 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL165360 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL352889 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL89086 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL167201 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL353570 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL164342 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL168042 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL335431 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL313611 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL165845 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL164295 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL164085 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL89912 | — | IC50 | ~ | 10000.0 | nM | - |
| CHEMBL350411 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL165187 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL163647 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL423646 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL436244 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL166326 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL159906 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL165358 | — | IC50 | ~ | 50000.0 | nM | - |