Assay Detail
Functional
CHEMBL3428930
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and β₂ agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 9.34 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3426706 | — | — | 1 | 10.00 |
| CHEMBL3426697 | — | — | 1 | 9.90 |
| CHEMBL3426701 | — | — | 1 | 9.80 |
| CHEMBL3426698 | — | — | 1 | 9.80 |
| CHEMBL3426693 | — | — | 1 | 9.70 |
| CHEMBL3426694 | — | — | 1 | 9.70 |
| CHEMBL3426687 | — | — | 1 | 9.60 |
| CHEMBL3426688 | — | — | 1 | 9.60 |
| CHEMBL3426691 | — | — | 1 | 9.60 |
| CHEMBL3039518 | BATEFENTEROL | 2.0 | 1 | 9.60 |
| CHEMBL3426695 | — | — | 1 | 9.60 |
| CHEMBL3426702 | — | — | 1 | 9.60 |
| CHEMBL3426696 | — | — | 1 | 9.50 |
| CHEMBL1683934 | — | — | 1 | 9.40 |
| CHEMBL3426692 | — | — | 1 | 9.40 |
| CHEMBL3426699 | — | — | 1 | 9.30 |
| CHEMBL3426690 | — | — | 1 | 9.30 |
| CHEMBL3426689 | — | — | 1 | 9.30 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 9.10 |
| CHEMBL3426703 | — | — | 1 | 9.10 |
| CHEMBL3426708 | — | — | 1 | 9.10 |
| CHEMBL3426707 | — | — | 1 | 8.90 |
| CHEMBL3426700 | — | — | 1 | 8.80 |
| CHEMBL3426705 | — | — | 1 | 8.40 |
| CHEMBL3426704 | — | — | 1 | 7.30 |
| CHEMBL1900528 | TIOTROPIUM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3426706 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3426697 | — | EC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL3426701 | — | EC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL3426698 | — | EC50 | = | 0.1585 | nM | 9.80 |
| CHEMBL3426693 | — | EC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL3426694 | — | EC50 | = | 0.1995 | nM | 9.70 |
| CHEMBL3426687 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3426688 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3426691 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3039518 | BATEFENTEROL | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3426695 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3426702 | — | EC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL3426696 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL1683934 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL3426692 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL3426699 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3426690 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3426689 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL1346 | DARIFENACIN | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3426703 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3426708 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL3426707 | — | EC50 | = | 1.259 | nM | 8.90 |
| CHEMBL3426700 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL3426705 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL3426704 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1900528 | TIOTROPIUM | EC50 | > | 10000.0 | nM | - |