Assay Detail
Binding
CHEMBL2399396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant GluN1/GluN2A receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of glycine/glutamate-induced inward current at -70mV by two-electrode voltage clamp assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
In vitro and in vivo evaluation of polymethylene tetraamine derivatives as NMDA receptor channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.48 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 9.02 |
| CHEMBL2398522 | — | — | 1 | 8.38 |
| CHEMBL55568 | — | — | 1 | 7.96 |
| CHEMBL2009741 | — | — | 1 | 7.05 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 6.86 |
| CHEMBL2398521 | — | — | 1 | 6.59 |
| CHEMBL2398520 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL807 | MEMANTINE | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL2398522 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL55568 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2009741 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL27673 | METHOCTRAMINE | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL2398521 | — | IC50 | = | 256.7 | nM | 6.59 |
| CHEMBL2398520 | — | IC50 | = | 315.0 | nM | 6.50 |