Assay Detail
Binding
CHEMBL749378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for the glycine binding site of the NMDA receptor using [3H]- 5,7- dichloro -kynurenic acid as radio-ligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 1 (CHEMBL330) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 2
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.11 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290738 | — | — | 1 | 8.59 |
| CHEMBL290963 | — | — | 1 | 8.52 |
| CHEMBL290649 | — | — | 1 | 8.51 |
| CHEMBL417514 | — | — | 1 | 8.48 |
| CHEMBL40730 | — | — | 1 | 8.36 |
| CHEMBL38994 | — | — | 1 | 8.29 |
| CHEMBL289607 | — | — | 1 | 8.18 |
| CHEMBL290555 | — | — | 1 | 8.00 |
| CHEMBL39408 | — | — | 1 | 7.33 |
| CHEMBL39627 | — | — | 1 | 6.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290738 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL290963 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL290649 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL417514 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL40730 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL38994 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL289607 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL290555 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL39408 | — | Ki | = | 46.6 | nM | 7.33 |
| CHEMBL39627 | — | Ki | = | 134.0 | nM | 6.87 |