Assay Detail
Functional
CHEMBL1115587
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Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins
11
Total Activities
11
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 |
Publication
The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.31 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094785 | CARMOTEROL | 2.0 | 1 | 9.52 |
| CHEMBL1256786 | FORMOTEROL | 4.0 | 1 | 9.40 |
| CHEMBL1094323 | — | — | 1 | 9.08 |
| CHEMBL1094486 | — | — | 1 | 8.64 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 8.46 |
| CHEMBL1095777 | INDACATEROL | 4.0 | 1 | 8.10 |
| CHEMBL714 | ALBUTEROL | 4.0 | 1 | 7.77 |
| CHEMBL1095778 | — | — | 1 | 7.70 |
| CHEMBL1094483 | — | — | 1 | 7.32 |
| CHEMBL1094487 | — | — | 1 | 7.12 |
| CHEMBL1095779 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094785 | CARMOTEROL | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1256786 | FORMOTEROL | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1094323 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL1094486 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1263 | SALMETEROL | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1095777 | INDACATEROL | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL714 | ALBUTEROL | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1095778 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1094483 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1094487 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1095779 | — | IC50 | > | 1000.0 | nM | - |