Assay Detail
Binding
CHEMBL748261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CPP from rat synaptic membrane glutamate NMDA receptor
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 12 | 6.82 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL37949 | — | — | 1 | 8.15 |
| CHEMBL285281 | — | — | 2 | 7.75 |
| CHEMBL39524 | — | — | 1 | 7.66 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.55 |
| CHEMBL289142 | — | — | 1 | 7.25 |
| CHEMBL39532 | — | — | 1 | 7.11 |
| CHEMBL22304 | — | — | 1 | 6.95 |
| CHEMBL441967 | — | — | 1 | 6.82 |
| CHEMBL39743 | — | — | 1 | 6.12 |
| CHEMBL39943 | — | — | 2 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL37949 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL285281 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL39524 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL289142 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL39532 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL22304 | — | IC50 | = | 112.6 | nM | 6.95 |
| CHEMBL441967 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL39743 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL285281 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL39943 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL39943 | — | IC50 | = | 6800.0 | nM | 5.17 |