Assay Detail
Functional
CHEMBL1686738
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Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
14
Total Activities
14
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 muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.87 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1256786 | FORMOTEROL | 4.0 | 1 | 9.72 |
| CHEMBL1683933 | — | — | 1 | 9.49 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 9.48 |
| CHEMBL1683934 | — | — | 1 | 9.44 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 9.09 |
| CHEMBL1683942 | — | — | 1 | 9.05 |
| CHEMBL1683932 | — | — | 1 | 8.96 |
| CHEMBL1683938 | — | — | 1 | 8.96 |
| CHEMBL1683931 | — | — | 1 | 8.89 |
| CHEMBL1683935 | — | — | 1 | 8.59 |
| CHEMBL1683939 | — | — | 1 | 8.48 |
| CHEMBL1683940 | — | — | 1 | 8.08 |
| CHEMBL1683941 | — | — | 1 | 8.05 |
| CHEMBL1683936 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1256786 | FORMOTEROL | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL1683933 | — | EC50 | = | 0.32 | nM | 9.49 |
| CHEMBL1263 | SALMETEROL | EC50 | = | 0.33 | nM | 9.48 |
| CHEMBL1683934 | — | EC50 | = | 0.36 | nM | 9.44 |
| CHEMBL1346 | DARIFENACIN | EC50 | = | 0.82 | nM | 9.09 |
| CHEMBL1683942 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1683932 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1683938 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1683931 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1683935 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1683939 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1683940 | — | EC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1683941 | — | EC50 | = | 8.9 | nM | 8.05 |
| CHEMBL1683936 | — | EC50 | = | 14.0 | nM | 7.85 |