Assay Detail
Binding
CHEMBL750561
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Inhibitory activity against Xenopus laevis oocyte expressing 1A/2A heteromeric human NMDA (hNMDA) receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2A (CHEMBL1907604) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.11 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12513 | — | — | 1 | 9.70 |
| CHEMBL274422 | — | — | 1 | 8.96 |
| CHEMBL536107 | — | — | 1 | 8.38 |
| CHEMBL268920 | — | — | 1 | 7.75 |
| CHEMBL12256 | — | — | 1 | 7.40 |
| CHEMBL543489 | — | — | 1 | 7.30 |
| CHEMBL273686 | — | — | 1 | 7.30 |
| CHEMBL12301 | — | — | 1 | 7.22 |
| CHEMBL543252 | — | — | 1 | 7.05 |
| CHEMBL268714 | — | — | 1 | 6.96 |
| CHEMBL276670 | — | — | 1 | 6.77 |
| CHEMBL536106 | — | — | 1 | 6.70 |
| CHEMBL273636 | — | — | 1 | 6.57 |
| CHEMBL12546 | — | — | 1 | 6.31 |
| CHEMBL12733 | — | — | 1 | 6.22 |
| CHEMBL12728 | — | — | 1 | 6.10 |
| CHEMBL12414 | — | — | 1 | 5.77 |
| CHEMBL273889 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12513 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL274422 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL536107 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL268920 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL12256 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL543489 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL273686 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL12301 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL543252 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL268714 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL276670 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL536106 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL273636 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL12546 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL12733 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL12728 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL12414 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL273889 | — | IC50 | = | 2800.0 | nM | 5.55 |