Assay Detail
Binding
CHEMBL749381
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Tested for the ability to displace [3H]glycine, by greater than 50%, from NMDA receptor of rat cortical membranes at a dose of 10 uM
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 a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.94 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50267 | — | — | 1 | 7.40 |
| CHEMBL31344 | — | — | 1 | 6.85 |
| CHEMBL303080 | — | — | 1 | 6.47 |
| CHEMBL413345 | — | — | 1 | 6.19 |
| CHEMBL301556 | — | — | 1 | 6.01 |
| CHEMBL23754 | — | — | 1 | 5.28 |
| CHEMBL299155 | TRANSTORINE | 1.0 | 1 | 5.27 |
| CHEMBL166426 | — | — | 1 | 5.15 |
| CHEMBL168873 | — | — | 1 | 4.83 |
| CHEMBL25599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50267 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL31344 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL303080 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL413345 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL301556 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL23754 | — | Ki | = | 5240.0 | nM | 5.28 |
| CHEMBL299155 | TRANSTORINE | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL166426 | — | Ki | = | 7040.0 | nM | 5.15 |
| CHEMBL168873 | — | Ki | = | 14800.0 | nM | 4.83 |
| CHEMBL25599 | — | Ki | > | 100000.0 | nM | - |