Assay Detail
Binding
CHEMBL4321003
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse NR2B receptor expressed in HEK293 cells co-expressing NR1 subunit assessed as reduction in glutamic acid/glycine-induced calcium ion influx by fluorescence based assay
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, NMDA 2B (CHEMBL3442) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of NR2B-selective antagonists via scaffold hopping and pharmacokinetic profile optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.83 | 9.00 |
| pIC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526884 | — | — | 1 | 9.00 |
| CHEMBL4534333 | — | — | 1 | 9.00 |
| CHEMBL4583880 | — | — | 1 | 8.70 |
| CHEMBL4470637 | — | — | 1 | 8.50 |
| CHEMBL182066 | RADIPRODIL | 2.0 | 1 | 8.50 |
| CHEMBL4454495 | — | — | 1 | 8.20 |
| CHEMBL4474892 | — | — | 1 | 8.20 |
| CHEMBL4442519 | — | — | 1 | 8.20 |
| CHEMBL4464831 | — | — | 1 | 8.20 |
| CHEMBL4451442 | — | — | 1 | 8.10 |
| CHEMBL4463054 | — | — | 1 | 8.00 |
| CHEMBL4455039 | — | — | 1 | 8.00 |
| CHEMBL4460020 | — | — | 1 | 8.00 |
| CHEMBL4460939 | — | — | 1 | 8.00 |
| CHEMBL4453597 | — | — | 1 | 7.90 |
| CHEMBL4531810 | — | — | 1 | 7.80 |
| CHEMBL4451235 | — | — | 1 | 7.40 |
| CHEMBL4463106 | — | — | 1 | 7.40 |
| CHEMBL4462628 | — | — | 1 | 7.30 |
| CHEMBL4471369 | — | — | 1 | 7.20 |
| CHEMBL4435364 | — | — | 1 | 7.20 |
| CHEMBL4449793 | — | — | 1 | 7.20 |
| CHEMBL4457441 | — | — | 1 | 7.00 |
| CHEMBL4448851 | — | — | 1 | 7.00 |
| CHEMBL4456965 | — | — | 1 | 6.90 |
| CHEMBL4438058 | — | — | 1 | 6.70 |
| CHEMBL4455020 | — | — | 1 | - |
| CHEMBL4558398 | — | — | 1 | - |
| CHEMBL4454452 | — | — | 1 | - |
| CHEMBL4559320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526884 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4534333 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4583880 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4470637 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL182066 | RADIPRODIL | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4454495 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4474892 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4442519 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4464831 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4451442 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4463054 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4455039 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4460020 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4460939 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4453597 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4531810 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4451235 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4463106 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4462628 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4471369 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4435364 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4449793 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4457441 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4448851 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4456965 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4438058 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4455020 | — | pIC50 | - | — | - | |
| CHEMBL4558398 | — | pIC50 | - | — | - | |
| CHEMBL4454452 | — | pIC50 | - | — | - | |
| CHEMBL4559320 | — | pIC50 | - | — | - | |
| CHEMBL4451476 | — | pIC50 | - | — | - | |
| CHEMBL4583561 | — | pIC50 | - | — | - |