Assay Detail
Binding
CHEMBL4254527
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Antagonist activity at GluN2B/GluN1a receptor (unknown origin) expressed in mouse L(tk-) cells assessed as cytoprotection against glycine/(S)-glutamate-induced cell death preincubated for 30 mins followed by glycine/(S)-glutamate addition measured after 6 hrs by LDH assay
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.88 | 7.75 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305195 | — | — | 1 | 7.75 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 6.23 |
| CHEMBL4284348 | — | — | 1 | 5.52 |
| CHEMBL4294991 | — | — | 2 | 5.28 |
| CHEMBL4286654 | — | — | 1 | 4.60 |
| CHEMBL4287755 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305195 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL305187 | IFENPRODIL | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4284348 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4294991 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4286654 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4287755 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4294991 | — | Inhibition | - | % | - |