Assay Detail
Functional
CHEMBL5129841
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In vivo antagonist activity at muscarinic M3 receptor activity in Dunkin-Hartley guinea pig trachea assessed as inhibition of carbachol induced contraction in presence of propranolol
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 of Clinical Candidate CHF-6366: A Novel Super-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 | 8 | 9.35 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5184455 | — | — | 1 | 10.00 |
| CHEMBL5193853 | — | — | 1 | 9.90 |
| CHEMBL5172865 | — | — | 1 | 9.70 |
| CHEMBL5208201 | — | — | 1 | 9.70 |
| CHEMBL5208957 | — | — | 1 | 9.40 |
| CHEMBL5190387 | — | — | 1 | 9.30 |
| CHEMBL5200887 | — | — | 1 | 8.70 |
| CHEMBL5184598 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5184455 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5193853 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL5172865 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5208201 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL5208957 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5190387 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5200887 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5184598 | — | IC50 | = | 7.943 | nM | 8.10 |