Assay Detail
Binding
CHEMBL751133
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Tested for the ability to inhibit [3H]MK-801 binding to NMDA receptor of rat cortical membranes in the presence of glutamate (1 uM)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| 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 |
|---|---|---|---|
| IC50 | 9 | 5.01 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50267 | — | — | 1 | 6.07 |
| CHEMBL303080 | — | — | 1 | 5.48 |
| CHEMBL413345 | — | — | 1 | 5.45 |
| CHEMBL301556 | — | — | 1 | 5.23 |
| CHEMBL299155 | TRANSTORINE | 1.0 | 1 | 4.39 |
| CHEMBL23754 | — | — | 1 | 4.34 |
| CHEMBL168873 | — | — | 1 | 4.08 |
| CHEMBL166426 | — | — | 1 | - |
| CHEMBL25599 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50267 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL303080 | — | IC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL413345 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL301556 | — | IC50 | = | 5910.0 | nM | 5.23 |
| CHEMBL299155 | TRANSTORINE | IC50 | = | 40250.0 | nM | 4.39 |
| CHEMBL23754 | — | IC50 | = | 45550.0 | nM | 4.34 |
| CHEMBL168873 | — | IC50 | = | 83430.0 | nM | 4.08 |
| CHEMBL166426 | — | IC50 | = | 102900.0 | nM | - |
| CHEMBL25599 | — | IC50 | > | 100000.0 | nM | - |