Assay Detail
Binding
CHEMBL748576
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Affinity measured by using [3H]5,7-dichlorokynurenic acid (DCKA) for the glycine binding site of NMDA receptor
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 1
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.52 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289151 | — | — | 1 | 8.85 |
| CHEMBL39881 | — | — | 1 | 8.59 |
| CHEMBL290963 | — | — | 1 | 8.52 |
| CHEMBL417514 | — | — | 1 | 8.48 |
| CHEMBL40072 | — | — | 1 | 8.42 |
| CHEMBL418055 | — | — | 1 | 8.13 |
| CHEMBL290291 | — | — | 1 | 8.08 |
| CHEMBL39773 | — | — | 1 | 8.00 |
| CHEMBL262206 | — | — | 1 | 7.77 |
| CHEMBL415866 | — | — | 1 | 7.68 |
| CHEMBL37409 | — | — | 1 | 7.53 |
| CHEMBL289307 | — | — | 1 | 7.42 |
| CHEMBL288478 | — | — | 1 | 7.38 |
| CHEMBL416970 | — | — | 2 | 6.62 |
| CHEMBL285519 | — | — | 1 | 6.35 |
| CHEMBL417335 | — | — | 2 | 6.23 |
| CHEMBL37098 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289151 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL39881 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL290963 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL417514 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL40072 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL418055 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL290291 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL39773 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL262206 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL415866 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL37409 | — | Ki | = | 29.6 | nM | 7.53 |
| CHEMBL289307 | — | Ki | = | 38.3 | nM | 7.42 |
| CHEMBL288478 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL416970 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL416970 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL285519 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL417335 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL417335 | — | Ki | = | 665.0 | nM | 6.18 |
| CHEMBL37098 | — | Ki | = | 760.0 | nM | 6.12 |