Assay Detail
Binding
CHEMBL752263
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Inhibition of [3H]25-6981 binding to N-methyl-D-aspartate glutamate receptor 2B of rat brain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.30 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299294 | — | — | 1 | 8.70 |
| CHEMBL50872 | — | — | 1 | 8.46 |
| CHEMBL51594 | — | — | 1 | 8.10 |
| CHEMBL48915 | — | — | 1 | 8.10 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 7.89 |
| CHEMBL46779 | — | — | 1 | 7.60 |
| CHEMBL48366 | — | — | 1 | 7.58 |
| CHEMBL50166 | — | — | 1 | 7.54 |
| CHEMBL48743 | — | — | 1 | 7.43 |
| CHEMBL294961 | — | — | 1 | 7.12 |
| CHEMBL433092 | — | — | 1 | 6.64 |
| CHEMBL46251 | — | — | 1 | 5.25 |
| CHEMBL48365 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299294 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL50872 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL51594 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL48915 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL49623 | (R,S)-IFENPRODIL | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL46779 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL48366 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL50166 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL48743 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL294961 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL433092 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL46251 | — | Ki | = | 5600.0 | nM | 5.25 |
| CHEMBL48365 | — | Ki | = | 28000.0 | nM | 4.55 |