Assay Detail
Functional
CHEMBL914283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at NR2B NMDA receptor in Wistar rat neocortical cells assessed as inhibition of NMDA-evoked elevation of intracellular calcium concentration
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 7.22 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219986 | — | — | 1 | 8.96 |
| CHEMBL220611 | — | — | 1 | 8.92 |
| CHEMBL424752 | — | — | 1 | 8.89 |
| CHEMBL375615 | — | — | 1 | 8.77 |
| CHEMBL223248 | — | — | 1 | 8.66 |
| CHEMBL222615 | — | — | 1 | 8.62 |
| CHEMBL222665 | — | — | 1 | 8.60 |
| CHEMBL220474 | — | — | 1 | 8.54 |
| CHEMBL375620 | — | — | 1 | 8.52 |
| CHEMBL373977 | — | — | 1 | 8.37 |
| CHEMBL126929 | — | — | 1 | 8.19 |
| CHEMBL219631 | BESONPRODIL | -1.0 | 1 | 8.18 |
| CHEMBL436521 | — | — | 1 | 8.07 |
| CHEMBL220041 | — | — | 1 | 8.07 |
| CHEMBL419784 | — | — | 1 | 7.80 |
| CHEMBL124873 | — | — | 1 | 7.80 |
| CHEMBL374011 | — | — | 1 | 7.77 |
| CHEMBL333936 | — | — | 1 | 7.75 |
| CHEMBL219987 | — | — | 1 | 7.70 |
| CHEMBL126228 | — | — | 1 | 7.60 |
| CHEMBL222197 | — | — | 1 | 7.52 |
| CHEMBL124516 | — | — | 1 | 7.51 |
| CHEMBL223695 | — | — | 1 | 7.42 |
| CHEMBL374012 | — | — | 1 | 7.40 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.39 |
| CHEMBL127510 | — | — | 1 | 7.39 |
| CHEMBL373890 | — | — | 1 | 7.33 |
| CHEMBL374853 | — | — | 1 | 7.30 |
| CHEMBL375827 | — | — | 1 | 7.24 |
| CHEMBL374793 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219986 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL220611 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL424752 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL375615 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL223248 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL222615 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL222665 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL220474 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL375620 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL373977 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL126929 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL219631 | BESONPRODIL | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL220041 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL436521 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL124873 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL419784 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL374011 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL333936 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL219987 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL126228 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL222197 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL124516 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL223695 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL374012 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL127510 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL17350 | TRAXOPRODIL | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL373890 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL374853 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL375827 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL374793 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL373891 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL426731 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL221108 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL220441 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL113919 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL305195 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL123908 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL219985 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL374676 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL222458 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL373907 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL220835 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL375805 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL222457 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL221045 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL221107 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL339570 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL220775 | — | IC50 | = | 1158.0 | nM | 5.94 |
| CHEMBL222459 | — | IC50 | = | 1901.0 | nM | 5.72 |
| CHEMBL220440 | — | IC50 | = | 2206.0 | nM | 5.66 |