Assay Detail
Binding
CHEMBL748110
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for the NMDA receptor site was assessed by its ability to displace [3H]TCP from its binding site in rat brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.87 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL37949 | — | — | 1 | 6.14 |
| CHEMBL39532 | — | — | 1 | 4.96 |
| CHEMBL39524 | — | — | 1 | 4.87 |
| CHEMBL289142 | — | — | 1 | 4.81 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 4.65 |
| CHEMBL22304 | — | — | 1 | 4.35 |
| CHEMBL441967 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL37949 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL39532 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL39524 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL289142 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL22304 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL441967 | — | IC50 | = | 46500.0 | nM | 4.33 |