Assay Detail
Functional
CHEMBL5034542
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at muscarinic M3 receptor in rat trachea assessed as inhibition of carbachol-induced contraction
15
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Trachea |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL320) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of M<sub>3</sub> Antagonist-PDE4 Inhibitor Dual Pharmacology Molecules for the Treatment of Chronic Obstructive Pulmonary Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.18 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5074599 | — | — | 2 | 9.00 |
| CHEMBL5074216 | — | — | 2 | 9.00 |
| CHEMBL5086393 | — | — | 2 | 8.80 |
| CHEMBL5078006 | — | — | 2 | 8.50 |
| CHEMBL5081816 | — | — | 2 | 8.30 |
| CHEMBL5076445 | — | — | 2 | 8.30 |
| CHEMBL5076886 | — | — | 1 | 8.00 |
| CHEMBL5076535 | — | — | 2 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074599 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5074216 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5086393 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5074216 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5074599 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5078006 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5081816 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5076445 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL5076886 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5076535 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5086393 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5078006 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5076445 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5081816 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5076535 | — | IC50 | = | 79.43 | nM | 7.10 |