Assay Detail
Functional
CHEMBL615181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Functional antagonism by electrical assays in Xenopus oocytes expressing the 1A/2B NMDA receptor
13
Total Activities
13
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
Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.70 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119778 | — | — | 1 | 8.10 |
| CHEMBL42414 | — | — | 1 | 7.82 |
| CHEMBL420530 | — | — | 1 | 7.46 |
| CHEMBL118969 | — | — | 1 | 7.37 |
| CHEMBL334003 | — | — | 1 | 7.35 |
| CHEMBL333339 | — | — | 1 | 7.02 |
| CHEMBL444851 | — | — | 1 | 6.75 |
| CHEMBL545284 | — | — | 1 | 6.70 |
| CHEMBL327075 | — | — | 1 | 6.52 |
| CHEMBL553596 | — | — | 1 | 5.96 |
| CHEMBL280111 | — | — | 1 | 5.46 |
| CHEMBL119100 | — | — | 1 | 5.43 |
| CHEMBL283775 | — | — | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119778 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL42414 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL420530 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL118969 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL334003 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL333339 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL444851 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL545284 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL327075 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL553596 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL280111 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL119100 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL283775 | — | IC50 | = | 7300.0 | nM | 5.14 |