Assay Detail
Functional
CHEMBL856828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NR2B expressed in Ltk- cells by calcium flux assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Ltk- |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 8.53 | 8.80 |
| IC50 | 1 | 6.99 | 6.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219060 | — | — | 1 | 8.80 |
| CHEMBL218713 | — | — | 1 | 8.25 |
| CHEMBL48029 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219060 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL218713 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL48029 | — | IC50 | = | 102.0 | nM | 6.99 |