Assay Detail
Binding
CHEMBL909221
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Displacement of [3H]Ro25-6981 from NR2B NMDA receptor in rat forebrain membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Forebrain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL311) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.11 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL215372 | — | — | 1 | 8.52 |
| CHEMBL212990 | — | — | 1 | 8.52 |
| CHEMBL213172 | — | — | 1 | 8.49 |
| CHEMBL436521 | — | — | 1 | 8.46 |
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.40 |
| CHEMBL214758 | — | — | 1 | 8.40 |
| CHEMBL219634 | — | — | 1 | 8.40 |
| CHEMBL219737 | — | — | 1 | 8.36 |
| CHEMBL220266 | — | — | 1 | 8.30 |
| CHEMBL220319 | — | — | 1 | 8.28 |
| CHEMBL380179 | — | — | 1 | 8.22 |
| CHEMBL305195 | — | — | 1 | 8.22 |
| CHEMBL214632 | — | — | 1 | 8.08 |
| CHEMBL213256 | — | — | 1 | 8.00 |
| CHEMBL333936 | — | — | 1 | 7.92 |
| CHEMBL212484 | — | — | 1 | 7.85 |
| CHEMBL215371 | — | — | 1 | 6.84 |
| CHEMBL113919 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL215372 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL212990 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL213172 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL436521 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL219631 | BESONPRODIL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL214758 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL219634 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL219737 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL220266 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL220319 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL380179 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL305195 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL214632 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL213256 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL333936 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL212484 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL215371 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL113919 | — | IC50 | = | 196.0 | nM | 6.71 |