Assay Detail
Binding
CHEMBL5041140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at rat GluN1/GluN2A NMDA receptor expressed in Xenopus oocytes measured after 4 days in presence of L-glutamte by two-electrode voltage-clamp recording assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; Grin1/Grin2a (CHEMBL2096680) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Derivatives of (<i>R</i>)-3-(5-Furanyl)carboxamido-2-aminopropanoic Acid as Potent NMDA Receptor Glycine Site Agonists with GluN2 Subunit-Specific Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 5.97 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081078 | — | — | 1 | 7.28 |
| CHEMBL5081008 | — | — | 1 | 7.03 |
| CHEMBL5087374 | — | — | 1 | 6.89 |
| CHEMBL5091289 | — | — | 1 | 6.75 |
| CHEMBL5085583 | — | — | 1 | 6.66 |
| CHEMBL5081203 | — | — | 1 | 6.58 |
| CHEMBL773 | GLYCINE | 4.0 | 1 | 6.00 |
| CHEMBL285123 | (D)-SERINE | 3.0 | 1 | 6.00 |
| CHEMBL5087170 | — | — | 1 | 5.51 |
| CHEMBL5093773 | — | — | 1 | 5.37 |
| CHEMBL5072895 | — | — | 1 | 5.32 |
| CHEMBL5076681 | — | — | 1 | 5.31 |
| CHEMBL5087550 | — | — | 1 | 5.18 |
| CHEMBL5081696 | — | — | 1 | 5.00 |
| CHEMBL5083882 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081078 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5081008 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5087374 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5091289 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5085583 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5081203 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL773 | GLYCINE | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL285123 | (D)-SERINE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5087170 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5093773 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5072895 | — | EC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5076681 | — | EC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5087550 | — | EC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5081696 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5083882 | — | EC50 | = | 23000.0 | nM | 4.64 |