Assay Detail
Binding
CHEMBL748065
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Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]-CPP as the radioligand.
18
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.24 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42990 | — | — | 1 | 8.47 |
| CHEMBL114829 | — | — | 1 | 8.19 |
| CHEMBL114315 | — | — | 1 | 7.65 |
| CHEMBL116797 | — | — | 1 | 7.62 |
| CHEMBL39664 | SELFOTEL | 2.0 | 1 | 7.55 |
| CHEMBL324706 | — | — | 3 | 7.53 |
| CHEMBL115671 | — | — | 1 | 7.42 |
| CHEMBL22304 | — | — | 1 | 6.95 |
| CHEMBL115071 | — | — | 1 | 6.78 |
| CHEMBL117174 | — | — | 1 | 6.61 |
| CHEMBL274440 | AP-7 | — | 1 | 6.41 |
| CHEMBL117173 | — | — | 1 | 6.08 |
| CHEMBL113829 | — | — | 1 | - |
| CHEMBL326557 | — | — | 1 | - |
| CHEMBL117035 | — | — | 1 | - |
| CHEMBL323830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42990 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL114829 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL114315 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL116797 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL39664 | SELFOTEL | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL324706 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL115671 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL22304 | — | IC50 | = | 112.6 | nM | 6.95 |
| CHEMBL324706 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL115071 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL117174 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL274440 | AP-7 | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL117173 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL324706 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL113829 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL326557 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL117035 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL323830 | — | IC50 | > | 1000.0 | nM | - |