Assay Detail
Functional
CHEMBL887787
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Antagonist activity at NMDA NR2B receptor assessed as calcium flux
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.75 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247323 | — | — | 1 | 8.23 |
| CHEMBL393670 | — | — | 1 | 7.92 |
| CHEMBL429656 | — | — | 1 | 7.41 |
| CHEMBL159279 | — | — | 1 | 7.33 |
| CHEMBL247718 | — | — | 1 | 7.31 |
| CHEMBL397784 | — | — | 1 | 6.97 |
| CHEMBL429475 | — | — | 1 | 6.58 |
| CHEMBL247114 | — | — | 1 | 5.90 |
| CHEMBL247717 | — | — | 1 | 5.70 |
| CHEMBL247115 | — | — | 1 | 5.46 |
| CHEMBL247113 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247323 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL393670 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL429656 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL159279 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL247718 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL397784 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL429475 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL247114 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL247717 | — | IC50 | = | 1976.0 | nM | 5.70 |
| CHEMBL247115 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL247113 | — | IC50 | = | 3670.0 | nM | 5.43 |