Assay Detail
Functional
CHEMBL752265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-methyl-D-aspartate glutamate receptor-evoked increase of intracellular Ca+ in cells expressing NMDA glutamate receptor 1/2B
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.49 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.10 |
| CHEMBL126929 | — | — | 1 | 8.00 |
| CHEMBL127510 | — | — | 1 | 7.72 |
| CHEMBL333936 | — | — | 1 | 7.70 |
| CHEMBL339570 | — | — | 1 | 7.62 |
| CHEMBL124873 | — | — | 1 | 7.41 |
| CHEMBL126228 | — | — | 1 | 7.40 |
| CHEMBL419784 | — | — | 1 | 7.34 |
| CHEMBL124516 | — | — | 1 | 7.28 |
| CHEMBL305195 | — | — | 1 | 7.24 |
| CHEMBL123908 | — | — | 1 | 7.11 |
| CHEMBL113919 | — | — | 1 | 6.98 |
| CHEMBL338104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219631 | BESONPRODIL | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL126929 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL127510 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL333936 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL339570 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL124873 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL126228 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL419784 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL124516 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL305195 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL123908 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL113919 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL338104 | — | IC50 | > | 8000.0 | nM | - |