Assay Detail
Binding
CHEMBL751885
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Displacement of [3H]dichlorokynurenate ([3H]-DCKA) from N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.38 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289832 | LICOSTINEL | 2.0 | 1 | 8.40 |
| CHEMBL80649 | — | — | 3 | 8.30 |
| CHEMBL80741 | — | — | 1 | 8.08 |
| CHEMBL80267 | — | — | 1 | 7.92 |
| CHEMBL76808 | — | — | 1 | 7.82 |
| CHEMBL310685 | — | — | 1 | 7.68 |
| CHEMBL308028 | — | — | 1 | 7.68 |
| CHEMBL420396 | — | — | 1 | 7.62 |
| CHEMBL312610 | — | — | 1 | 7.10 |
| CHEMBL306934 | — | — | 1 | 6.85 |
| CHEMBL310024 | — | — | 1 | 5.59 |
| CHEMBL311104 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289832 | LICOSTINEL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL80649 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL80741 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL80267 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL76808 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL310685 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL308028 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL420396 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL80649 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL80649 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL312610 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL306934 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL310024 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL311104 | — | IC50 | = | 4300.0 | nM | 5.37 |