Assay Detail
Functional
CHEMBL909225
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Inhibition of NMDA-evoked increase in intracellular calcium ion in rat cortical cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate NMDA receptor (CHEMBL1907608) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.20 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL212990 | — | — | 1 | 8.96 |
| CHEMBL214758 | — | — | 1 | 8.92 |
| CHEMBL215372 | — | — | 1 | 8.89 |
| CHEMBL212484 | — | — | 1 | 8.77 |
| CHEMBL219634 | — | — | 1 | 8.66 |
| CHEMBL220266 | — | — | 1 | 8.62 |
| CHEMBL213172 | — | — | 1 | 8.60 |
| CHEMBL380179 | — | — | 1 | 8.54 |
| CHEMBL213256 | — | — | 1 | 8.52 |
| CHEMBL220319 | — | — | 1 | 8.22 |
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.18 |
| CHEMBL436521 | — | — | 1 | 8.07 |
| CHEMBL219737 | — | — | 1 | 8.06 |
| CHEMBL214632 | — | — | 1 | 7.92 |
| CHEMBL333936 | — | — | 1 | 7.75 |
| CHEMBL215371 | — | — | 1 | 7.40 |
| CHEMBL305195 | — | — | 1 | 6.80 |
| CHEMBL113919 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL212990 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL214758 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL215372 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL212484 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL219634 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL220266 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL213172 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL380179 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL213256 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL220319 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL219631 | BESONPRODIL | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL436521 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL219737 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL214632 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL333936 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL215371 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL305195 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL113919 | — | IC50 | = | 191.0 | nM | 6.72 |