Assay Detail
Binding
CHEMBL828983
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/NR2C expressed in Xenopus oocytes
21
Total Activities
21
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/Grin2c (CHEMBL2096911) ↗| 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 | 21 | 5.79 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273636 | — | — | 1 | 7.94 |
| CHEMBL372468 | — | — | 1 | 7.02 |
| CHEMBL192866 | — | — | 1 | 7.00 |
| CHEMBL365746 | — | — | 1 | 6.54 |
| CHEMBL47277 | — | — | 1 | 6.20 |
| CHEMBL192728 | — | — | 1 | 6.18 |
| CHEMBL190046 | — | — | 1 | 6.07 |
| CHEMBL193138 | — | — | 1 | 5.93 |
| CHEMBL84612 | — | — | 1 | 5.79 |
| CHEMBL192957 | — | — | 1 | 5.57 |
| CHEMBL190724 | — | — | 1 | 5.41 |
| CHEMBL191838 | — | — | 1 | 5.38 |
| CHEMBL365515 | — | — | 1 | 5.36 |
| CHEMBL425185 | — | — | 1 | 5.31 |
| CHEMBL302783 | — | — | 1 | 5.19 |
| CHEMBL372278 | — | — | 1 | 5.13 |
| CHEMBL371796 | — | — | 1 | 5.07 |
| CHEMBL189211 | — | — | 1 | 5.06 |
| CHEMBL371803 | — | — | 1 | 5.05 |
| CHEMBL363649 | — | — | 1 | 4.57 |
| CHEMBL191599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273636 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL372468 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL192866 | — | Ki | = | 99.4 | nM | 7.00 |
| CHEMBL365746 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL47277 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL192728 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL190046 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL193138 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL84612 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL192957 | — | Ki | = | 2670.0 | nM | 5.57 |
| CHEMBL190724 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL191838 | — | Ki | = | 4220.0 | nM | 5.38 |
| CHEMBL365515 | — | Ki | = | 4420.0 | nM | 5.36 |
| CHEMBL425185 | — | Ki | = | 4880.0 | nM | 5.31 |
| CHEMBL302783 | — | Ki | = | 6420.0 | nM | 5.19 |
| CHEMBL372278 | — | Ki | = | 7380.0 | nM | 5.13 |
| CHEMBL371796 | — | Ki | = | 8490.0 | nM | 5.07 |
| CHEMBL189211 | — | Ki | = | 8670.0 | nM | 5.06 |
| CHEMBL371803 | — | Ki | = | 8980.0 | nM | 5.05 |
| CHEMBL363649 | — | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL191599 | — | Ki | > | 100000.0 | nM | - |