Assay Detail
Binding
CHEMBL829801
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory constant against (S)-glutamate and glycine evoked currents mediated by N-methyl-D-aspartate glutamate receptor NR1a/NR2A expressed in Xenopus oocytes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2a (CHEMBL2096680) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 5.66 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273636 | — | — | 1 | 8.27 |
| CHEMBL47277 | — | — | 1 | 7.39 |
| CHEMBL84612 | — | — | 1 | 6.55 |
| CHEMBL192866 | — | — | 1 | 6.50 |
| CHEMBL302783 | — | — | 1 | 6.31 |
| CHEMBL372468 | — | — | 1 | 6.26 |
| CHEMBL190046 | — | — | 1 | 6.08 |
| CHEMBL365746 | — | — | 1 | 5.81 |
| CHEMBL192728 | — | — | 1 | 5.41 |
| CHEMBL365515 | — | — | 1 | 5.10 |
| CHEMBL372278 | — | — | 1 | 5.06 |
| CHEMBL190724 | — | — | 1 | 5.02 |
| CHEMBL425185 | — | — | 1 | 4.98 |
| CHEMBL192957 | — | — | 1 | 4.95 |
| CHEMBL363649 | — | — | 1 | 4.88 |
| CHEMBL189211 | — | — | 1 | 4.87 |
| CHEMBL191838 | — | — | 1 | 4.85 |
| CHEMBL371803 | — | — | 1 | 4.80 |
| CHEMBL371796 | — | — | 1 | 4.37 |
| CHEMBL191599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273636 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL47277 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL84612 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL192866 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL302783 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL372468 | — | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL190046 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL365746 | — | Ki | = | 1540.0 | nM | 5.81 |
| CHEMBL192728 | — | Ki | = | 3880.0 | nM | 5.41 |
| CHEMBL365515 | — | Ki | = | 7970.0 | nM | 5.10 |
| CHEMBL372278 | — | Ki | = | 8780.0 | nM | 5.06 |
| CHEMBL190724 | — | Ki | = | 9600.0 | nM | 5.02 |
| CHEMBL425185 | — | Ki | = | 10480.0 | nM | 4.98 |
| CHEMBL192957 | — | Ki | = | 11180.0 | nM | 4.95 |
| CHEMBL363649 | — | Ki | = | 13200.0 | nM | 4.88 |
| CHEMBL189211 | — | Ki | = | 13600.0 | nM | 4.87 |
| CHEMBL191838 | — | Ki | = | 14190.0 | nM | 4.85 |
| CHEMBL371803 | — | Ki | = | 15790.0 | nM | 4.80 |
| CHEMBL371796 | — | Ki | = | 42900.0 | nM | 4.37 |
| CHEMBL191599 | — | Ki | > | 100000.0 | nM | - |