Assay Detail
Functional
CHEMBL889737
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant NR1/NR2B receptor expressed in Xenopus laevis oocytes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| 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 tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.63 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228486 | — | — | 1 | 7.08 |
| CHEMBL228436 | — | — | 1 | 6.97 |
| CHEMBL228437 | — | — | 1 | 6.97 |
| CHEMBL228435 | — | — | 1 | 6.85 |
| CHEMBL388315 | — | — | 1 | 6.78 |
| CHEMBL390521 | — | — | 1 | 6.72 |
| CHEMBL390304 | — | — | 1 | 6.70 |
| CHEMBL228380 | — | — | 1 | 6.57 |
| CHEMBL228378 | — | — | 1 | 6.53 |
| CHEMBL228325 | — | — | 1 | 6.47 |
| CHEMBL390305 | — | — | 1 | 6.46 |
| CHEMBL228379 | — | — | 1 | 6.36 |
| CHEMBL228324 | — | — | 1 | 6.31 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228486 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL228436 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL228437 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL228435 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL388315 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL390521 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL390304 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL228380 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL228378 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL228325 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL390305 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL228379 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL228324 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL807 | MEMANTINE | IC50 | = | 1020.0 | nM | 5.99 |