Assay Detail
Binding
CHEMBL828982
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/NR2B 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/Grin2b (CHEMBL2096666) ↗| 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 | 5.56 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273636 | — | — | 1 | 7.17 |
| CHEMBL192866 | — | — | 1 | 6.60 |
| CHEMBL47277 | — | — | 1 | 6.57 |
| CHEMBL190046 | — | — | 1 | 6.52 |
| CHEMBL372468 | — | — | 1 | 6.51 |
| CHEMBL84612 | — | — | 1 | 6.34 |
| CHEMBL365746 | — | — | 1 | 6.12 |
| CHEMBL192728 | — | — | 1 | 5.67 |
| CHEMBL193138 | — | — | 1 | 5.49 |
| CHEMBL302783 | — | — | 1 | 5.38 |
| CHEMBL371803 | — | — | 1 | 5.30 |
| CHEMBL425185 | — | — | 1 | 5.04 |
| CHEMBL365515 | — | — | 1 | 5.03 |
| CHEMBL192957 | — | — | 1 | 4.99 |
| CHEMBL372278 | — | — | 1 | 4.87 |
| CHEMBL189211 | — | — | 1 | 4.79 |
| CHEMBL363649 | — | — | 1 | 4.75 |
| CHEMBL190724 | — | — | 1 | 4.74 |
| CHEMBL191838 | — | — | 1 | 4.71 |
| CHEMBL371796 | — | — | 1 | 4.66 |
| CHEMBL191599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273636 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL192866 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL47277 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL190046 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL372468 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL84612 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL365746 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL192728 | — | Ki | = | 2150.0 | nM | 5.67 |
| CHEMBL193138 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL302783 | — | Ki | = | 4140.0 | nM | 5.38 |
| CHEMBL371803 | — | Ki | = | 5010.0 | nM | 5.30 |
| CHEMBL425185 | — | Ki | = | 9080.0 | nM | 5.04 |
| CHEMBL365515 | — | Ki | = | 9360.0 | nM | 5.03 |
| CHEMBL192957 | — | Ki | = | 10250.0 | nM | 4.99 |
| CHEMBL372278 | — | Ki | = | 13400.0 | nM | 4.87 |
| CHEMBL189211 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL363649 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL190724 | — | Ki | = | 18200.0 | nM | 4.74 |
| CHEMBL191838 | — | Ki | = | 19290.0 | nM | 4.71 |
| CHEMBL371796 | — | Ki | = | 22100.0 | nM | 4.66 |
| CHEMBL191599 | — | Ki | > | 100000.0 | nM | - |