Assay Detail
Binding
CHEMBL746546
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for N-methyl-D-aspartate glutamate receptor of cerebral cortical synaptic membranes from rats using [3H]MK-801 as radioligand
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.82 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL435424 | — | — | 1 | 6.70 |
| CHEMBL357942 | — | — | 1 | 6.38 |
| CHEMBL346658 | — | — | 1 | 6.28 |
| CHEMBL150477 | — | — | 1 | 6.28 |
| CHEMBL149158 | — | — | 1 | 6.27 |
| CHEMBL151391 | — | — | 1 | 6.13 |
| CHEMBL147451 | — | — | 1 | 6.00 |
| CHEMBL358755 | — | — | 1 | 5.96 |
| CHEMBL341635 | — | — | 1 | 5.77 |
| CHEMBL359038 | — | — | 1 | 5.44 |
| CHEMBL356009 | — | — | 1 | 5.38 |
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 5.20 |
| CHEMBL358389 | — | — | 1 | 4.89 |
| CHEMBL356831 | — | — | 1 | 4.80 |
| CHEMBL151811 | — | — | 1 | - |
| CHEMBL356656 | — | — | 1 | - |
| CHEMBL435624 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL435424 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL357942 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL346658 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL150477 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL149158 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL151391 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL147451 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL358755 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL341635 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL359038 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL356009 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL99946 | LEVOMILNACIPRAN | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL358389 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL356831 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL151811 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL356656 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL435624 | — | IC50 | = | 160000.0 | nM | - |