Assay Detail
Binding
CHEMBL856830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](E)-N1-(2-methoxybenzyl)cinnamamidine from human NR2B expressed in Ltk- cells
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ltk- |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.86 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218713 | — | — | 1 | 8.47 |
| CHEMBL218211 | — | — | 1 | 8.43 |
| CHEMBL386184 | — | — | 1 | 8.11 |
| CHEMBL219060 | — | — | 1 | 7.97 |
| CHEMBL220660 | — | — | 1 | 7.85 |
| CHEMBL221605 | — | — | 1 | 7.75 |
| CHEMBL218275 | — | — | 1 | 7.75 |
| CHEMBL221133 | — | — | 1 | 7.64 |
| CHEMBL435316 | — | — | 1 | 7.64 |
| CHEMBL218017 | — | — | 1 | 7.43 |
| CHEMBL218068 | — | — | 1 | 7.12 |
| CHEMBL48029 | — | — | 1 | 7.03 |
| CHEMBL218547 | — | — | 1 | 6.91 |
| CHEMBL374865 | — | — | 1 | 6.82 |
| CHEMBL218067 | — | — | 1 | 6.75 |
| CHEMBL219113 | — | — | 1 | 6.72 |
| CHEMBL218104 | — | — | 1 | 6.69 |
| CHEMBL218546 | — | — | 1 | 6.66 |
| CHEMBL425462 | — | — | 1 | 6.64 |
| CHEMBL219114 | — | — | 1 | 6.64 |
| CHEMBL218075 | — | — | 1 | 6.58 |
| CHEMBL217955 | — | — | 1 | 6.51 |
| CHEMBL217904 | — | — | 1 | 6.34 |
| CHEMBL425642 | — | — | 1 | 6.27 |
| CHEMBL217940 | — | — | 1 | 6.14 |
| CHEMBL218460 | — | — | 1 | 5.93 |
| CHEMBL217992 | — | — | 1 | 5.90 |
| CHEMBL218463 | — | — | 1 | 5.68 |
| CHEMBL438994 | — | — | 1 | 5.51 |
| CHEMBL218478 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218713 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL218211 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL386184 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL219060 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL220660 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL221605 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL218275 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL221133 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL435316 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL218017 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL218068 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL48029 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL218547 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL374865 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL218067 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL219113 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL218104 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL218546 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL425462 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL219114 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL218075 | — | Ki | = | 266.0 | nM | 6.58 |
| CHEMBL217955 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL217904 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL425642 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL217940 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL218460 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL217992 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL218463 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL438994 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL218478 | — | Ki | = | 3180.0 | nM | 5.50 |
| CHEMBL217915 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL374658 | — | Ki | > | 15000.0 | nM | - |