Assay Detail
Binding
CHEMBL1286019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-MK-801 from NMDA receptor phencyclidine binding site in guinea pig brain cortex homogenates after 5 mins by scintillation counting
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.28 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1277697 | — | — | 1 | 8.12 |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 2 | 7.96 |
| CHEMBL26479 | DIOXADROL | 2.0 | 1 | 7.70 |
| CHEMBL1163701 | — | — | 1 | 7.57 |
| CHEMBL1277605 | — | — | 1 | 7.55 |
| CHEMBL1164041 | — | — | 1 | 7.36 |
| CHEMBL1277698 | — | — | 1 | 7.32 |
| CHEMBL1163697 | — | — | 1 | 7.09 |
| CHEMBL1277330 | — | — | 1 | 6.45 |
| CHEMBL1165686 | — | — | 1 | 6.33 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1277697 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL1165411 | DEXOXADROL | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL1165411 | DEXOXADROL | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL26479 | DIOXADROL | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1163701 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL1277605 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL1164041 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1277698 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL1163697 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL1277330 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL1165686 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL807 | MEMANTINE | Ki | = | 1200.0 | nM | 5.92 |