Assay Detail
Binding
CHEMBL5166010
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of eGFP-tagged rat GluN1-1a/GluN2A transfected in human tsA201 cells assessed as inhibition glutamate-induced current measured at -65 mV holding potential applied for 10 secs by whole-cell patch-clamp method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | tsA201 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2a (CHEMBL2096680) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.44 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 6.00 |
| CHEMBL742 | KETAMINE | 4.0 | 1 | 6.00 |
| CHEMBL5187677 | — | — | 1 | 5.36 |
| CHEMBL660 | AMANTADINE | 4.0 | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL807 | MEMANTINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL742 | KETAMINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5187677 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL660 | AMANTADINE | IC50 | = | 40000.0 | nM | 4.40 |