Assay Detail
Binding
CHEMBL746993
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Inhibitory activity against Xenopus laevis oocyte expressing 1A/2B 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/GRIN2B (CHEMBL1907603) ↗| 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 | 6.07 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274422 | — | — | 1 | 9.15 |
| CHEMBL12513 | — | — | 1 | 8.74 |
| CHEMBL536107 | — | — | 1 | 7.47 |
| CHEMBL273686 | — | — | 1 | 6.24 |
| CHEMBL12301 | — | — | 1 | 6.09 |
| CHEMBL268920 | — | — | 1 | 6.05 |
| CHEMBL543252 | — | — | 1 | 6.03 |
| CHEMBL543489 | — | — | 1 | 5.89 |
| CHEMBL536106 | — | — | 1 | 5.89 |
| CHEMBL268714 | — | — | 1 | 5.85 |
| CHEMBL276670 | — | — | 1 | 5.82 |
| CHEMBL12256 | — | — | 1 | 5.80 |
| CHEMBL12546 | — | — | 1 | 5.21 |
| CHEMBL12728 | — | — | 1 | 5.21 |
| CHEMBL273889 | — | — | 1 | 4.62 |
| CHEMBL273636 | — | — | 1 | 4.53 |
| CHEMBL12733 | — | — | 1 | 4.52 |
| CHEMBL12414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274422 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL12513 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL536107 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL273686 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL12301 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL268920 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL543252 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL543489 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL536106 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL268714 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL276670 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL12256 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL12546 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL12728 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL273889 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL273636 | — | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL12733 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL12414 | — | IC50 | > | 30000.0 | nM | - |