Assay Detail
Functional
CHEMBL1943768
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Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A multivalent approach to the discovery of long-acting β(2)-adrenoceptor agonists for the treatment of asthma and COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 8.66 | 10.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1940832 | MILVETEROL | 2.0 | 1 | 10.20 |
| CHEMBL1940830 | — | — | 1 | 10.00 |
| CHEMBL1940833 | — | — | 1 | 9.90 |
| CHEMBL1940815 | — | — | 1 | 9.50 |
| CHEMBL1940817 | — | — | 1 | 9.50 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 9.50 |
| CHEMBL1940831 | — | — | 1 | 9.50 |
| CHEMBL1940834 | — | — | 1 | 9.40 |
| CHEMBL1940816 | — | — | 1 | 9.40 |
| CHEMBL1940820 | — | — | 1 | 8.80 |
| CHEMBL1940821 | — | — | 1 | 8.70 |
| CHEMBL1940818 | — | — | 1 | 8.70 |
| CHEMBL1940825 | — | — | 1 | 8.60 |
| CHEMBL1940819 | — | — | 1 | 8.30 |
| CHEMBL1940823 | — | — | 1 | 8.20 |
| CHEMBL1940824 | — | — | 1 | 8.10 |
| CHEMBL714 | ALBUTEROL | 4.0 | 1 | 7.60 |
| CHEMBL1940828 | — | — | 1 | 7.40 |
| CHEMBL1940822 | — | — | 1 | 7.40 |
| CHEMBL1940829 | — | — | 1 | 7.30 |
| CHEMBL1940826 | — | — | 1 | 7.30 |
| CHEMBL1940827 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1940832 | MILVETEROL | EC50 | = | 0.0631 | nM | 10.20 |
| CHEMBL1940830 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1940833 | — | EC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL1940815 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL1940817 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL1263 | SALMETEROL | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL1940831 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL1940834 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL1940816 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL1940820 | — | EC50 | = | 1.585 | nM | 8.80 |
| CHEMBL1940821 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL1940818 | — | EC50 | = | 1.995 | nM | 8.70 |
| CHEMBL1940825 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL1940819 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL1940823 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL1940824 | — | EC50 | = | 7.943 | nM | 8.10 |
| CHEMBL714 | ALBUTEROL | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1940828 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL1940822 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL1940829 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1940826 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1940827 | — | EC50 | = | 63.1 | nM | 7.20 |