Assay Detail
Binding
CHEMBL5503899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at M3 receptor in male albino Dunkin-Hartley guinea pig trachea assessed as inhibition of carbachol-induced smooth muscle contraction in presence of propranolol
28
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Trachea |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Discovery, Multiparametric Optimization, and Solid-State Driven Identification of CHF-6550, a Novel Soft Dual Pharmacology Muscarinic Antagonist and β<sub>2</sub> Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 9.03 | 9.90 |
| pIC50 | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5557828 | — | — | 1 | 9.90 |
| CHEMBL5550055 | — | — | 1 | 9.70 |
| CHEMBL5172865 | — | — | 1 | 9.70 |
| CHEMBL5558368 | — | — | 1 | 9.70 |
| CHEMBL5555665 | — | — | 1 | 9.40 |
| CHEMBL5532029 | — | — | 1 | 9.20 |
| CHEMBL5517637 | — | — | 1 | 9.10 |
| CHEMBL5505816 | — | — | 2 | 9.10 |
| CHEMBL5556228 | — | — | 1 | 9.10 |
| CHEMBL5542735 | — | — | 1 | 9.00 |
| CHEMBL6067691 | — | — | 1 | 8.70 |
| CHEMBL5505925 | — | — | 1 | 8.60 |
| CHEMBL5527960 | — | — | 1 | 8.50 |
| CHEMBL5512435 | — | — | 1 | 8.50 |
| CHEMBL5555744 | — | — | 1 | 8.30 |
| CHEMBL6067687 | — | — | 1 | 8.00 |
| CHEMBL5523458 | — | — | 1 | - |
| CHEMBL5556756 | — | — | 1 | - |
| CHEMBL5542534 | — | — | 1 | - |
| CHEMBL5558093 | — | — | 1 | - |
| CHEMBL5557651 | — | — | 1 | - |
| CHEMBL5542670 | — | — | 1 | - |
| CHEMBL5556694 | — | — | 1 | - |
| CHEMBL5542602 | — | — | 1 | - |
| CHEMBL5527849 | — | — | 1 | - |
| CHEMBL5523340 | — | — | 1 | - |
| CHEMBL5556153 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5557828 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL5550055 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5172865 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5558368 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5555665 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5532029 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL5517637 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL5505816 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL5556228 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL5505816 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5542735 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6067691 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5505925 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL5527960 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5512435 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5555744 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL6067687 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5523458 | — | pIC50 | - | — | - | |
| CHEMBL5556756 | — | pIC50 | - | — | - | |
| CHEMBL5542534 | — | pIC50 | - | — | - | |
| CHEMBL5558093 | — | pIC50 | - | — | - | |
| CHEMBL5557651 | — | pIC50 | - | — | - | |
| CHEMBL5542670 | — | pIC50 | - | — | - | |
| CHEMBL5556694 | — | pIC50 | - | — | - | |
| CHEMBL5542602 | — | pIC50 | - | — | - | |
| CHEMBL5527849 | — | pIC50 | - | — | - | |
| CHEMBL5523340 | — | pIC50 | - | — | - | |
| CHEMBL5556153 | — | pIC50 | - | — | - |