Assay Detail
Binding
CHEMBL3636231
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against NR1-1a/NR2A NMDA receptor (unknown origin) expressed in mouse recombinant L(tk-) cells assessed as inhibition of glycine and glutamate induced excitotoxicity incubated for 12 hrs by LDH assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.73 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | 8.01 |
| CHEMBL395091 | ESKETAMINE | 4.0 | 1 | 7.94 |
| CHEMBL275528 | PHENCYCLIDINE | 2.0 | 1 | 7.93 |
| CHEMBL3633211 | — | — | 1 | 7.75 |
| CHEMBL3633387 | — | — | 1 | 7.62 |
| CHEMBL3633210 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1165411 | DEXOXADROL | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL395091 | ESKETAMINE | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL275528 | PHENCYCLIDINE | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL3633211 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL3633387 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL3633210 | — | IC50 | = | 71.2 | nM | 7.15 |