Assay Detail
Binding
CHEMBL4817489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at muscarinic M3 receptor in guinea pig trachea assessed as inhibition of carbachol-induced contraction
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Trachea |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β<sub>2</sub> agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.97 | 9.90 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863525 | — | — | 1 | 9.90 |
| CHEMBL4871517 | — | — | 1 | 9.70 |
| CHEMBL4866806 | — | — | 1 | 9.50 |
| CHEMBL4854418 | — | — | 1 | 9.30 |
| CHEMBL4854091 | — | — | 1 | 9.30 |
| CHEMBL4878138 | — | — | 1 | 9.30 |
| CHEMBL4852629 | — | — | 1 | 8.70 |
| CHEMBL4871702 | — | — | 1 | 8.70 |
| CHEMBL4874819 | — | — | 1 | 8.50 |
| CHEMBL4878395 | — | — | 1 | 8.30 |
| CHEMBL4846536 | — | — | 1 | 7.50 |
| CHEMBL4857743 | — | — | 1 | - |
| CHEMBL4847910 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863525 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL4871517 | — | IC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL4866806 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4854418 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4854091 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4878138 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4852629 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4871702 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4874819 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4878395 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4846536 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4857743 | — | pIC50 | - | — | - | |
| CHEMBL4847910 | — | pIC50 | - | — | - |