Assay Detail
Binding
CHEMBL751683
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Binding affinity against NMDA receptor by displacement of [3H]Ro-256981
29
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.31 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL299294 | — | — | 1 | 8.70 |
| CHEMBL166991 | — | — | 1 | 8.52 |
| CHEMBL166935 | — | — | 1 | 8.52 |
| CHEMBL50872 | — | — | 1 | 8.46 |
| CHEMBL169695 | — | — | 1 | 8.40 |
| CHEMBL170552 | — | — | 1 | 8.40 |
| CHEMBL354482 | — | — | 1 | 8.40 |
| CHEMBL166697 | — | — | 1 | 8.30 |
| CHEMBL305195 | — | — | 1 | 8.22 |
| CHEMBL168496 | — | — | 1 | 8.10 |
| CHEMBL167004 | — | — | 1 | 8.10 |
| CHEMBL166599 | — | — | 2 | 8.10 |
| CHEMBL169469 | — | — | 1 | 8.05 |
| CHEMBL17350 | TRAXOPRODIL | 2.0 | 1 | 7.96 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 7.89 |
| CHEMBL168273 | — | — | 1 | 6.96 |
| CHEMBL352819 | — | — | 1 | 6.82 |
| CHEMBL168650 | — | — | 1 | 6.72 |
| CHEMBL170163 | — | — | 1 | 6.58 |
| CHEMBL168559 | — | — | 1 | 6.42 |
| CHEMBL353194 | — | — | 1 | 6.42 |
| CHEMBL167128 | — | — | 1 | 6.42 |
| CHEMBL168262 | — | — | 1 | 6.12 |
| CHEMBL168925 | — | — | 1 | 5.96 |
| CHEMBL354066 | — | — | 1 | 5.96 |
| CHEMBL169101 | — | — | 1 | 5.77 |
| CHEMBL168488 | — | — | 1 | 5.12 |
| CHEMBL170056 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL299294 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL166991 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL166935 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL50872 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL169695 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL170552 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL354482 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL166697 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL305195 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL168496 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL167004 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL166599 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL169469 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL17350 | TRAXOPRODIL | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL49623 | (R,S)-IFENPRODIL | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL166599 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL168273 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL352819 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL168650 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL170163 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL168559 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL353194 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL167128 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL168262 | — | Ki | = | 750.0 | nM | 6.12 |
| CHEMBL168925 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL354066 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL169101 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL168488 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL170056 | — | Ki | = | 15000.0 | nM | 4.82 |