Assay Detail
Binding
CHEMBL750473
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Inhibition of NMDA receptor binding affinity in rat brain synaptosomal membrane using [3H]glutamate as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonists are substrates for a neutral amino acid uptake system in Chinese hamster ovary cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.48 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL60181 | — | — | 1 | 7.85 |
| CHEMBL62030 | — | — | 1 | 7.82 |
| CHEMBL1907813 | — | — | 1 | 6.89 |
| CHEMBL61650 | — | — | 1 | 6.50 |
| CHEMBL294173 | — | — | 1 | 6.19 |
| CHEMBL22304 | — | — | 1 | 6.08 |
| CHEMBL59566 | — | — | 1 | 5.64 |
| CHEMBL58365 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL60181 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL62030 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1907813 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL61650 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL294173 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL22304 | — | IC50 | = | 837.0 | nM | 6.08 |
| CHEMBL59566 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL58365 | — | IC50 | = | 13500.0 | nM | 4.87 |