Assay Detail
Binding
CHEMBL752855
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Ability to enhance [3H]MK-801 binding to NMDA receptors in rat forebrain membranes was calculated with respect to spermine
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis of N,N'-substituted piperazine and homopiperazine derivatives with polyamine-like actions at N-methyl-D-aspartate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 4.44 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23194 | SPERMINE | 0.5 | 1 | 5.28 |
| CHEMBL145680 | — | — | 1 | 4.75 |
| CHEMBL144699 | — | — | 1 | 4.67 |
| CHEMBL143613 | — | — | 1 | 4.61 |
| CHEMBL147313 | — | — | 1 | 4.45 |
| CHEMBL144094 | — | — | 1 | 4.43 |
| CHEMBL144873 | — | — | 1 | 4.43 |
| CHEMBL144518 | — | — | 1 | 4.34 |
| CHEMBL41307 | — | — | 1 | 4.30 |
| CHEMBL144067 | — | — | 1 | 4.29 |
| CHEMBL144822 | — | — | 1 | 4.25 |
| CHEMBL144255 | — | — | 1 | 4.19 |
| CHEMBL144520 | — | — | 1 | 4.11 |
| CHEMBL415535 | — | — | 1 | 4.01 |
| CHEMBL144354 | — | — | 1 | - |
| CHEMBL142725 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23194 | SPERMINE | EC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL145680 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL144699 | — | EC50 | = | 21400.0 | nM | 4.67 |
| CHEMBL143613 | — | EC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL147313 | — | EC50 | = | 35300.0 | nM | 4.45 |
| CHEMBL144094 | — | EC50 | = | 36800.0 | nM | 4.43 |
| CHEMBL144873 | — | EC50 | = | 37500.0 | nM | 4.43 |
| CHEMBL144518 | — | EC50 | = | 45900.0 | nM | 4.34 |
| CHEMBL41307 | — | EC50 | = | 50100.0 | nM | 4.30 |
| CHEMBL144067 | — | EC50 | = | 50700.0 | nM | 4.29 |
| CHEMBL144822 | — | EC50 | = | 55900.0 | nM | 4.25 |
| CHEMBL144255 | — | EC50 | = | 64500.0 | nM | 4.19 |
| CHEMBL144520 | — | EC50 | = | 77500.0 | nM | 4.11 |
| CHEMBL415535 | — | EC50 | = | 96500.0 | nM | 4.01 |
| CHEMBL144354 | — | EC50 | = | 238500.0 | nM | - |
| CHEMBL142725 | — | EC50 | = | 112200.0 | nM | - |