Assay Detail
Binding
CHEMBL753124
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Inhibition of [3H]-MK-801 binding to NMDA receptor from rat cerebral cortical synaptic membrane
15
Total Activities
11
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 analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.67 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275528 | PHENCYCLIDINE | 2.0 | 1 | 8.01 |
| CHEMBL434836 | — | — | 1 | 6.80 |
| CHEMBL119554 | — | — | 2 | 6.70 |
| CHEMBL330958 | — | — | 2 | 6.46 |
| CHEMBL742 | KETAMINE | 4.0 | 1 | 6.21 |
| CHEMBL343694 | — | — | 1 | 6.00 |
| CHEMBL145378 | — | — | 1 | 5.38 |
| CHEMBL99946 | LEVOMILNACIPRAN | 4.0 | 1 | 5.20 |
| CHEMBL356782 | — | — | 2 | 5.09 |
| CHEMBL145226 | — | — | 1 | 4.77 |
| CHEMBL145773 | — | — | 2 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275528 | PHENCYCLIDINE | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL434836 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL119554 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL330958 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL742 | KETAMINE | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL343694 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL145378 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL99946 | LEVOMILNACIPRAN | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL330958 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL119554 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL356782 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL356782 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL145226 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL145773 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL145773 | — | IC50 | = | 31000.0 | nM | 4.51 |