Assay Detail
Binding
CHEMBL2317635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human M4 muscarinic receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.39 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL326450 | — | — | 1 | 9.00 |
| CHEMBL215180 | — | — | 1 | 7.38 |
| CHEMBL12098 | SCH-211803 | — | 1 | 7.21 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 6.98 |
| CHEMBL17045 | OTENZEPAD | 2.0 | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL326450 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL215180 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL12098 | SCH-211803 | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL17045 | OTENZEPAD | Ki | = | 407.0 | nM | 6.39 |