Assay Detail
Binding
CHEMBL749326
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Inhibition of [3H]MK-801 binding to N-methyl-D-aspartate glutamate receptor of rat cerebral cortical synaptic membrane
13
Total Activities
9
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
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.48 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119554 | — | — | 2 | 6.70 |
| CHEMBL326735 | — | — | 2 | 6.54 |
| CHEMBL330958 | — | — | 2 | 6.46 |
| CHEMBL742 | KETAMINE | 4.0 | 1 | 6.21 |
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 5.20 |
| CHEMBL119462 | — | — | 1 | 4.57 |
| CHEMBL431687 | — | — | 2 | 4.02 |
| CHEMBL118690 | — | — | 1 | - |
| CHEMBL117681 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119554 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL326735 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL330958 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL742 | KETAMINE | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL99946 | LEVOMILNACIPRAN | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL330958 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL119554 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL326735 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL119462 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL431687 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL118690 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL117681 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL431687 | — | IC50 | > | 100000.0 | nM | - |