Assay Detail
Binding
CHEMBL2340159
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings
27
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Trachea |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 9 | - | - |
| Emax | 9 | - | - |
| EC50 | 9 | 8.71 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2335415 | — | — | 3 | 9.20 |
| CHEMBL2335412 | — | — | 3 | 9.19 |
| CHEMBL2335413 | — | — | 3 | 9.17 |
| CHEMBL2335414 | — | — | 3 | 9.08 |
| CHEMBL2335410 | — | — | 3 | 8.71 |
| CHEMBL2335409 | — | — | 3 | 8.55 |
| CHEMBL2335411 | — | — | 3 | 8.50 |
| CHEMBL2335408 | — | — | 3 | 8.47 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 3 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2335415 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL2335412 | — | EC50 | = | 0.6457 | nM | 9.19 |
| CHEMBL2335413 | — | EC50 | = | 0.6761 | nM | 9.17 |
| CHEMBL2335414 | — | EC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL2335410 | — | EC50 | = | 1.95 | nM | 8.71 |
| CHEMBL2335409 | — | EC50 | = | 2.818 | nM | 8.55 |
| CHEMBL2335411 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL2335408 | — | EC50 | = | 3.388 | nM | 8.47 |
| CHEMBL434 | ISOPROTERENOL | EC50 | = | 28.84 | nM | 7.54 |
| CHEMBL2335414 | — | Activity | - | — | - | |
| CHEMBL2335413 | — | Activity | - | — | - | |
| CHEMBL2335412 | — | Activity | - | — | - | |
| CHEMBL2335411 | — | Activity | - | — | - | |
| CHEMBL2335410 | — | Activity | - | — | - | |
| CHEMBL2335409 | — | Activity | - | — | - | |
| CHEMBL2335408 | — | Activity | - | — | - | |
| CHEMBL434 | ISOPROTERENOL | Activity | - | — | - | |
| CHEMBL2335415 | — | Emax | = | 102.0 | % | - |
| CHEMBL2335414 | — | Emax | = | 100.0 | % | - |
| CHEMBL2335413 | — | Emax | = | 100.0 | % | - |
| CHEMBL2335412 | — | Emax | = | 102.0 | % | - |
| CHEMBL2335415 | — | Activity | - | — | - | |
| CHEMBL2335410 | — | Emax | = | 103.0 | % | - |
| CHEMBL2335409 | — | Emax | = | 103.0 | % | - |
| CHEMBL2335408 | — | Emax | = | 100.0 | % | - |
| CHEMBL434 | ISOPROTERENOL | Emax | = | 100.0 | % | - |
| CHEMBL2335411 | — | Emax | = | 105.0 | % | - |