Assay Detail
Binding
CHEMBL5136720
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant human GluN1/GluN2A receptor stably expressed in HEK293 cells assessed as increase in glycine/L-glutamate-induced channel current at -70 mV holding potential by whole cell patch clamp method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
SAGE-718: A First-in-Class <i>N</i>-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.82 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4555750 | — | — | 1 | 7.52 |
| CHEMBL5173240 | — | — | 1 | 7.26 |
| CHEMBL5197305 | — | — | 1 | 7.22 |
| CHEMBL5189622 | — | — | 1 | 7.13 |
| CHEMBL5095095 | DALZANEMDOR | 3.0 | 1 | 7.07 |
| CHEMBL5197411 | — | — | 1 | 7.03 |
| CHEMBL5170656 | — | — | 1 | 7.00 |
| CHEMBL5198675 | — | — | 1 | 6.92 |
| CHEMBL171804 | — | — | 1 | 6.82 |
| CHEMBL5172269 | — | — | 1 | 6.82 |
| CHEMBL5196694 | — | — | 1 | 6.80 |
| CHEMBL5204245 | — | — | 1 | 6.75 |
| CHEMBL5178963 | — | — | 1 | 6.66 |
| CHEMBL5198776 | — | — | 1 | 6.51 |
| CHEMBL5200422 | — | — | 1 | 6.38 |
| CHEMBL4448829 | — | — | 1 | 6.32 |
| CHEMBL5178281 | — | — | 1 | 5.66 |
| CHEMBL5175389 | — | — | 1 | - |
| CHEMBL5170022 | — | — | 1 | - |
| CHEMBL5174404 | — | — | 1 | - |
| CHEMBL5181802 | — | — | 1 | - |
| CHEMBL5170297 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4555750 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5173240 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5197305 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5189622 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5095095 | DALZANEMDOR | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5197411 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5170656 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5198675 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL171804 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5172269 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5196694 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5204245 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5178963 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5198776 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5200422 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4448829 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5178281 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5175389 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5170022 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5174404 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5181802 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5170297 | — | EC50 | > | 10000.0 | nM | - |