Assay Detail
Functional
CHEMBL889736
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant NR1/NR2A 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/GRIN2A (CHEMBL1907604) ↗| 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 | 6.69 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228435 | — | — | 1 | 7.14 |
| CHEMBL228436 | — | — | 1 | 7.11 |
| CHEMBL388315 | — | — | 1 | 6.96 |
| CHEMBL228380 | — | — | 1 | 6.93 |
| CHEMBL228437 | — | — | 1 | 6.90 |
| CHEMBL228486 | — | — | 1 | 6.84 |
| CHEMBL228325 | — | — | 1 | 6.70 |
| CHEMBL390304 | — | — | 1 | 6.69 |
| CHEMBL390521 | — | — | 1 | 6.68 |
| CHEMBL390305 | — | — | 1 | 6.67 |
| CHEMBL228378 | — | — | 1 | 6.62 |
| CHEMBL228324 | — | — | 1 | 6.41 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 6.04 |
| CHEMBL228379 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228435 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL228436 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL388315 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL228380 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL228437 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL228486 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL228325 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL390304 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL390521 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL390305 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL228378 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL228324 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL807 | MEMANTINE | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL228379 | — | IC50 | = | 958.0 | nM | 6.02 |