Assay Detail
Functional
CHEMBL2351582
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Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.30 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3392321 | — | — | 1 | 9.09 |
| CHEMBL2348218 | — | — | 1 | 8.64 |
| CHEMBL207802 | LK-204545 | — | 1 | 8.64 |
| CHEMBL2348201 | — | — | 1 | 8.52 |
| CHEMBL2348219 | — | — | 1 | 8.44 |
| CHEMBL2348211 | — | — | 1 | 8.35 |
| CHEMBL1374751 | CIMATEROL | 2.0 | 1 | 8.13 |
| CHEMBL2348220 | — | — | 1 | 8.01 |
| CHEMBL75753 | XAMOTEROL | 2.0 | 1 | 7.96 |
| CHEMBL420746 | CGP-12177 | — | 1 | 7.91 |
| CHEMBL2348217 | — | — | 1 | 7.64 |
| CHEMBL280822 | CGP-20712A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3392321 | — | EC50 | = | 0.8128 | nM | 9.09 |
| CHEMBL2348218 | — | EC50 | = | 2.291 | nM | 8.64 |
| CHEMBL207802 | LK-204545 | EC50 | = | 2.291 | nM | 8.64 |
| CHEMBL2348201 | — | EC50 | = | 3.02 | nM | 8.52 |
| CHEMBL2348219 | — | EC50 | = | 3.631 | nM | 8.44 |
| CHEMBL2348211 | — | EC50 | = | 4.467 | nM | 8.35 |
| CHEMBL1374751 | CIMATEROL | EC50 | = | 7.413 | nM | 8.13 |
| CHEMBL2348220 | — | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL75753 | XAMOTEROL | EC50 | = | 10.96 | nM | 7.96 |
| CHEMBL420746 | CGP-12177 | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL2348217 | — | EC50 | = | 22.91 | nM | 7.64 |
| CHEMBL280822 | CGP-20712A | EC50 | - | — | - |