Assay Detail
Binding
CHEMBL5531340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at GluN1/GluN2B receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of receptor-mediated current by patch clamp assay
8
Total Activities
6
Compounds Tested
2
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
Design, Synthesis, and Biological Evaluation of <i>Pierardine</i> Derivatives as Novel Brain-Penetrant and <i>In Vivo</i> Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.90 | 7.13 |
| Activity | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5570052 | — | — | 1 | 7.13 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.89 |
| CHEMBL5563730 | — | — | 2 | 6.82 |
| CHEMBL5569595 | — | — | 2 | 6.74 |
| CHEMBL5208814 | — | — | 1 | - |
| CHEMBL5567588 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5570052 | — | IC50 | = | 74.01 | nM | 7.13 |
| CHEMBL305187 | IFENPRODIL | IC50 | = | 127.8 | nM | 6.89 |
| CHEMBL5563730 | — | IC50 | = | 152.66 | nM | 6.82 |
| CHEMBL5569595 | — | IC50 | = | 183.04 | nM | 6.74 |
| CHEMBL5208814 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5563730 | — | Activity | - | — | - | |
| CHEMBL5569595 | — | Activity | - | — | - | |
| CHEMBL5567588 | — | IC50 | > | 10.0 | nM | - |