Assay Detail
Binding
CHEMBL4817490
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Agonist 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 | 8.71 | 9.80 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863525 | — | — | 1 | 9.80 |
| CHEMBL4871517 | — | — | 1 | 9.80 |
| CHEMBL4866806 | — | — | 1 | 9.50 |
| CHEMBL4854091 | — | — | 1 | 9.10 |
| CHEMBL4878138 | — | — | 1 | 9.10 |
| CHEMBL4874819 | — | — | 1 | 9.00 |
| CHEMBL4871702 | — | — | 1 | 9.00 |
| CHEMBL4854418 | — | — | 1 | 8.10 |
| CHEMBL4852629 | — | — | 1 | 7.80 |
| CHEMBL4878395 | — | — | 1 | 7.30 |
| CHEMBL4846536 | — | — | 1 | 7.30 |
| CHEMBL4857743 | — | — | 1 | - |
| CHEMBL4847910 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863525 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL4871517 | — | IC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL4866806 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4854091 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4878138 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4874819 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4871702 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4854418 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4852629 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4878395 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4846536 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4857743 | — | pIC50 | - | — | - | |
| CHEMBL4847910 | — | pIC50 | - | — | - |