Assay Detail
Binding
CHEMBL752918
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In vitro binding to N-methyl-D-aspartate glutamate receptor using [3H]MK-801 (1 nM) and rat brain membrane suspensions
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and in vitro evaluation of N,N'-diphenyl and N-naphthyl-N'-phenylguanidines as N-methyl-D-aspartate receptor ion-channel ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.96 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | 8.89 |
| CHEMBL41306 | CNS-5161 | -1.0 | 1 | 8.73 |
| CHEMBL40155 | — | — | 1 | 8.46 |
| CHEMBL38936 | — | — | 1 | 8.33 |
| CHEMBL40657 | — | — | 1 | 8.28 |
| CHEMBL43132 | — | — | 1 | 8.20 |
| CHEMBL41641 | — | — | 1 | 7.85 |
| CHEMBL40410 | — | — | 1 | 7.72 |
| CHEMBL38882 | — | — | 1 | 7.66 |
| CHEMBL40131 | — | — | 1 | 7.36 |
| CHEMBL41557 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284237 | DIZOCILPINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL41306 | CNS-5161 | Ki | = | 1.87 | nM | 8.73 |
| CHEMBL40155 | — | Ki | = | 3.48 | nM | 8.46 |
| CHEMBL38936 | — | Ki | = | 4.65 | nM | 8.33 |
| CHEMBL40657 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL43132 | — | Ki | = | 6.28 | nM | 8.20 |
| CHEMBL41641 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL40410 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL38882 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL40131 | — | Ki | = | 43.5 | nM | 7.36 |
| CHEMBL41557 | — | Ki | = | 839.0 | nM | 6.08 |