Assay Detail
Binding
CHEMBL4274851
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-ifenprodil from GluN1a/GluN2B (unknown origin) expressed in L(tk-) cell membranes after 120 mins by scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.20 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 8.00 |
| CHEMBL3357784 | — | — | 1 | 8.00 |
| CHEMBL296601 | — | — | 1 | 7.80 |
| CHEMBL3357783 | — | — | 1 | 7.80 |
| CHEMBL4288091 | — | — | 1 | 6.83 |
| CHEMBL4280186 | — | — | 1 | 6.52 |
| CHEMBL4276754 | — | — | 1 | 6.35 |
| CHEMBL4284692 | — | — | 1 | 6.32 |
| CHEMBL4284122 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305187 | IFENPRODIL | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3357784 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL296601 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3357783 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4288091 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL4280186 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL4276754 | — | Ki | = | 445.0 | nM | 6.35 |
| CHEMBL4284692 | — | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL4284122 | — | Ki | > | 1000.0 | nM | - |