Assay Detail
Binding
CHEMBL914284
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Displacement of [3H]Ro 25,6981 from NR2B NMDA receptor in rat forebrain
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL311) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 7.65 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222665 | — | — | 1 | 8.52 |
| CHEMBL424752 | — | — | 1 | 8.52 |
| CHEMBL219986 | — | — | 1 | 8.52 |
| CHEMBL436521 | — | — | 1 | 8.46 |
| CHEMBL220611 | — | — | 1 | 8.40 |
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.40 |
| CHEMBL223248 | — | — | 1 | 8.40 |
| CHEMBL222615 | — | — | 1 | 8.30 |
| CHEMBL219987 | — | — | 1 | 8.30 |
| CHEMBL220474 | — | — | 1 | 8.22 |
| CHEMBL126929 | — | — | 1 | 8.22 |
| CHEMBL374853 | — | — | 1 | 8.22 |
| CHEMBL305195 | — | — | 1 | 8.22 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 8.15 |
| CHEMBL127510 | — | — | 1 | 8.15 |
| CHEMBL222197 | — | — | 1 | 8.05 |
| CHEMBL375620 | — | — | 1 | 8.00 |
| CHEMBL220041 | — | — | 1 | 8.00 |
| CHEMBL373977 | — | — | 1 | 7.92 |
| CHEMBL373891 | — | — | 1 | 7.92 |
| CHEMBL333936 | — | — | 1 | 7.92 |
| CHEMBL375615 | — | — | 1 | 7.85 |
| CHEMBL374793 | — | — | 1 | 7.77 |
| CHEMBL124873 | — | — | 1 | 7.75 |
| CHEMBL374011 | — | — | 1 | 7.64 |
| CHEMBL374676 | — | — | 1 | 7.55 |
| CHEMBL126228 | — | — | 1 | 7.51 |
| CHEMBL223695 | — | — | 1 | 7.51 |
| CHEMBL419784 | — | — | 1 | 7.33 |
| CHEMBL221108 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222665 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL219986 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL424752 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL436521 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL220611 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL219631 | BESONPRODIL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL223248 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL222615 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL219987 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL220474 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL126929 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL374853 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL305195 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL127510 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL222197 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL375620 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL220041 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL373977 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL373891 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL333936 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL375615 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL374793 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL124873 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL374011 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL374676 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL223695 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL126228 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL419784 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL221108 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL375827 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL426731 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL124516 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL374012 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL373890 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL113919 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL220441 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL339570 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL123908 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL220835 | — | IC50 | = | 1084.0 | nM | 5.96 |
| CHEMBL222457 | — | IC50 | = | 1545.0 | nM | 5.81 |
| CHEMBL222458 | — | IC50 | - | — | - | |
| CHEMBL375805 | — | IC50 | - | — | - | |
| CHEMBL221045 | — | IC50 | - | — | - | |
| CHEMBL220775 | — | IC50 | - | — | - | |
| CHEMBL220786 | — | IC50 | - | — | - | |
| CHEMBL220440 | — | IC50 | - | — | - | |
| CHEMBL219742 | — | IC50 | - | — | - | |
| CHEMBL338104 | — | IC50 | - | — | - | |
| CHEMBL221107 | — | IC50 | - | — | - |