Assay Detail
Functional
CHEMBL746994
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against rat 1A/2B subtype of N-methyl-D-aspartate (NMDA) receptor in xenopus oocytes.
9
Total Activities
9
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 relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.55 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305195 | — | — | 1 | 8.05 |
| CHEMBL42414 | — | — | 1 | 7.70 |
| CHEMBL44301 | — | — | 1 | 7.30 |
| CHEMBL44412 | — | — | 1 | 7.06 |
| CHEMBL43928 | — | — | 1 | 6.85 |
| CHEMBL40454 | — | — | 1 | 6.25 |
| CHEMBL40465 | — | — | 1 | 5.48 |
| CHEMBL41073 | — | — | 1 | 5.42 |
| CHEMBL42274 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305195 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL42414 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL44301 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL44412 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL43928 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL40454 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL40465 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL41073 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL42274 | — | IC50 | = | 14000.0 | nM | 4.85 |