Assay Detail
Functional
CHEMBL1913628
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at M3 receptor in Dunkin-Hartley guinea pig tracheal strips assessed as inhibition of electrically field-stimulated contractile response after 8 hrs
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.69 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.39 |
| CHEMBL1910856 | PF-03635659 | 2.0 | 1 | 8.81 |
| CHEMBL1910865 | — | — | 1 | 8.46 |
| CHEMBL1910850 | — | — | 1 | 8.41 |
| CHEMBL1910851 | — | — | 1 | 8.37 |
| CHEMBL1908368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL1910856 | PF-03635659 | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL1910865 | — | IC50 | = | 3.48 | nM | 8.46 |
| CHEMBL1910850 | — | IC50 | = | 3.87 | nM | 8.41 |
| CHEMBL1910851 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1908368 | — | IC50 | - | — | - |