Assay Detail
Functional
CHEMBL2351584
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs
10
Total Activities
10
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 |
|---|---|---|---|
| Kd | 10 | 6.00 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3392321 | — | — | 1 | 7.25 |
| CHEMBL75753 | XAMOTEROL | 2.0 | 1 | 6.18 |
| CHEMBL2348201 | — | — | 1 | 6.10 |
| CHEMBL2348218 | — | — | 1 | 6.05 |
| CHEMBL280822 | CGP-20712A | — | 1 | 5.98 |
| CHEMBL2348211 | — | — | 1 | 5.92 |
| CHEMBL2348219 | — | — | 1 | 5.84 |
| CHEMBL207802 | LK-204545 | — | 1 | 5.54 |
| CHEMBL2348220 | — | — | 1 | 5.15 |
| CHEMBL2348217 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3392321 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL75753 | XAMOTEROL | Kd | = | 660.69 | nM | 6.18 |
| CHEMBL2348201 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL2348218 | — | Kd | = | 891.25 | nM | 6.05 |
| CHEMBL280822 | CGP-20712A | Kd | = | 1047.13 | nM | 5.98 |
| CHEMBL2348211 | — | Kd | = | 1202.26 | nM | 5.92 |
| CHEMBL2348219 | — | Kd | = | 1445.44 | nM | 5.84 |
| CHEMBL207802 | LK-204545 | Kd | = | 2884.03 | nM | 5.54 |
| CHEMBL2348220 | — | Kd | = | 7079.46 | nM | 5.15 |
| CHEMBL2348217 | — | Kd | > | 10000.0 | nM | - |