Assay Detail
Binding
CHEMBL748772
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Inhibition of [3H]glycine binding to N-methyl-D-aspartate glutamate receptor in synaptic membranes of rat cerebral cortex
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Substituted analogues of GV150526 as potent glycine binding site antagonists in animal models of cerebral ischemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.22 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL117691 | — | — | 1 | 8.80 |
| CHEMBL325457 | — | — | 1 | 8.67 |
| CHEMBL325034 | — | — | 1 | 8.62 |
| CHEMBL418862 | — | — | 1 | 8.57 |
| CHEMBL419045 | GAVESTINEL SODIUM | — | 1 | 8.49 |
| CHEMBL331968 | — | — | 1 | 8.25 |
| CHEMBL326734 | — | — | 1 | 8.20 |
| CHEMBL119896 | — | — | 1 | 8.20 |
| CHEMBL323643 | — | — | 1 | 8.15 |
| CHEMBL117419 | — | — | 1 | 7.93 |
| CHEMBL117693 | — | — | 1 | 7.91 |
| CHEMBL119876 | — | — | 1 | 7.83 |
| CHEMBL326101 | — | — | 1 | 7.70 |
| CHEMBL115753 | — | — | 1 | 7.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL117691 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL325457 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL325034 | — | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL418862 | — | Ki | = | 2.692 | nM | 8.57 |
| CHEMBL419045 | GAVESTINEL SODIUM | Ki | = | 3.236 | nM | 8.49 |
| CHEMBL331968 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL326734 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL119896 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL323643 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL117419 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL117693 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL119876 | — | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL326101 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL115753 | — | Ki | = | 20.42 | nM | 7.69 |