Assay Detail
Binding
CHEMBL745929
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Binding affinity towards muscarinic acetylcholine receptor M1 in rat heart using [3H]pirenzepine as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6 | 6.02 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL48366 | — | — | 1 | 6.19 |
| CHEMBL48915 | — | — | 1 | 6.18 |
| CHEMBL51594 | — | — | 1 | 6.14 |
| CHEMBL46779 | — | — | 1 | 6.05 |
| CHEMBL48743 | — | — | 1 | 6.00 |
| CHEMBL50166 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL48366 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL48915 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL51594 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL46779 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL48743 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL50166 | — | Ki | = | 2600.0 | nM | 5.58 |