Assay Detail
Binding
CHEMBL5136722
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of recombinant human GluN1/GluN2B 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
20
Total Activities
20
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/GRIN2B (CHEMBL1907603) ↗| 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 | 20 | 6.79 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5197305 | — | — | 1 | 7.64 |
| CHEMBL4448829 | — | — | 1 | 7.42 |
| CHEMBL5189622 | — | — | 1 | 7.31 |
| CHEMBL5200422 | — | — | 1 | 7.22 |
| CHEMBL5095095 | DALZANEMDOR | 3.0 | 1 | 7.10 |
| CHEMBL5198675 | — | — | 1 | 7.09 |
| CHEMBL5173240 | — | — | 1 | 7.00 |
| CHEMBL5204245 | — | — | 1 | 6.96 |
| CHEMBL5198776 | — | — | 1 | 6.75 |
| CHEMBL5196694 | — | — | 1 | 6.72 |
| CHEMBL5197411 | — | — | 1 | 6.60 |
| CHEMBL5172269 | — | — | 1 | 6.52 |
| CHEMBL5170656 | — | — | 1 | 6.35 |
| CHEMBL5178963 | — | — | 1 | 6.23 |
| CHEMBL5170022 | — | — | 1 | 5.96 |
| CHEMBL5178281 | — | — | 1 | 5.82 |
| CHEMBL5170297 | — | — | 1 | - |
| CHEMBL5174404 | — | — | 1 | - |
| CHEMBL5175389 | — | — | 1 | - |
| CHEMBL5181802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5197305 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4448829 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5189622 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5200422 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5095095 | DALZANEMDOR | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5198675 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5173240 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5204245 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5198776 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5196694 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5197411 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5172269 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5170656 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5178963 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5170022 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5178281 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5170297 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5174404 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5175389 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5181802 | — | EC50 | > | 10000.0 | nM | - |