Assay Detail
Binding
CHEMBL3871160
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of GluN1/GluN2A receptor (unknown origin) expressed in CHO cells assessed as increase in glutamate-induced calcium flux measured at time interval of 5 mins in presence of saturating glycine by calcium dye-based fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.79 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3970291 | — | — | 1 | 7.68 |
| CHEMBL3891918 | — | — | 1 | 7.62 |
| CHEMBL3799878 | — | — | 1 | 7.52 |
| CHEMBL3938522 | — | — | 1 | 7.43 |
| CHEMBL3976578 | — | — | 1 | 7.41 |
| CHEMBL3983039 | — | — | 1 | 7.39 |
| CHEMBL3968067 | — | — | 1 | 7.10 |
| CHEMBL3948381 | — | — | 1 | 6.92 |
| CHEMBL3944810 | — | — | 1 | 6.89 |
| CHEMBL3945685 | — | — | 1 | 6.57 |
| CHEMBL3975050 | — | — | 1 | 6.55 |
| CHEMBL3799694 | — | — | 1 | 6.36 |
| CHEMBL3985768 | — | — | 1 | 5.85 |
| CHEMBL3955420 | — | — | 1 | 5.60 |
| CHEMBL3966561 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3970291 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3891918 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3799878 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3938522 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3976578 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3983039 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3968067 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3948381 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3944810 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3945685 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3975050 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3799694 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3985768 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3955420 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3966561 | — | EC50 | = | 9800.0 | nM | 5.01 |