Assay Detail
Functional
CHEMBL752242
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In vitro inhibitory concentration against NMDA responses at NR1A/2B receptors expressed in Xenopus oocytes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2b (CHEMBL2096666) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.74 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54778 | — | — | 1 | 7.60 |
| CHEMBL103472 | — | — | 1 | 7.55 |
| CHEMBL317229 | — | — | 1 | 7.37 |
| CHEMBL449704 | — | — | 1 | 7.30 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 6.96 |
| CHEMBL102659 | — | — | 1 | 6.20 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | 5.85 |
| CHEMBL100870 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54778 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL103472 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL317229 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL449704 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL49623 | (R,S)-IFENPRODIL | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL102659 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL28564 | ELIPRODIL | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL100870 | — | IC50 | = | 7700.0 | nM | 5.11 |