Assay Detail
Binding
CHEMBL2351860
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 28 | 6.02 | 9.17 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513389 | ZENIDOLOL | 2.0 | 1 | 9.17 |
| CHEMBL3392321 | — | — | 1 | 6.84 |
| CHEMBL2348198 | — | — | 1 | 6.54 |
| CHEMBL2348212 | — | — | 1 | 6.27 |
| CHEMBL2348203 | — | — | 1 | 6.10 |
| CHEMBL2348213 | — | — | 1 | 6.06 |
| CHEMBL2348216 | — | — | 1 | 6.05 |
| CHEMBL2348204 | — | — | 1 | 5.99 |
| CHEMBL2348209 | — | — | 1 | 5.96 |
| CHEMBL2348197 | — | — | 1 | 5.94 |
| CHEMBL2348215 | — | — | 1 | 5.93 |
| CHEMBL2348199 | — | — | 1 | 5.92 |
| CHEMBL2348202 | — | — | 1 | 5.91 |
| CHEMBL2348218 | — | — | 1 | 5.91 |
| CHEMBL2348205 | — | — | 1 | 5.86 |
| CHEMBL2348207 | — | — | 1 | 5.86 |
| CHEMBL2348196 | — | — | 1 | 5.86 |
| CHEMBL2348210 | — | — | 1 | 5.85 |
| CHEMBL2348206 | — | — | 1 | 5.84 |
| CHEMBL280822 | CGP-20712A | — | 1 | 5.82 |
| CHEMBL2348214 | — | — | 1 | 5.80 |
| CHEMBL2348208 | — | — | 1 | 5.76 |
| CHEMBL75753 | XAMOTEROL | 2.0 | 1 | 5.76 |
| CHEMBL2348201 | — | — | 1 | 5.69 |
| CHEMBL2348211 | — | — | 1 | 5.58 |
| CHEMBL2348200 | — | — | 1 | 5.54 |
| CHEMBL2348219 | — | — | 1 | 5.45 |
| CHEMBL207802 | LK-204545 | — | 1 | 5.29 |
| CHEMBL2348217 | — | — | 1 | - |
| CHEMBL2348220 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513389 | ZENIDOLOL | Kd | = | 0.6761 | nM | 9.17 |
| CHEMBL3392321 | — | Kd | = | 144.54 | nM | 6.84 |
| CHEMBL2348198 | — | Kd | = | 288.4 | nM | 6.54 |
| CHEMBL2348212 | — | Kd | = | 537.03 | nM | 6.27 |
| CHEMBL2348203 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL2348213 | — | Kd | = | 870.96 | nM | 6.06 |
| CHEMBL2348216 | — | Kd | = | 891.25 | nM | 6.05 |
| CHEMBL2348204 | — | Kd | = | 1023.29 | nM | 5.99 |
| CHEMBL2348209 | — | Kd | = | 1096.48 | nM | 5.96 |
| CHEMBL2348197 | — | Kd | = | 1148.15 | nM | 5.94 |
| CHEMBL2348215 | — | Kd | = | 1174.9 | nM | 5.93 |
| CHEMBL2348199 | — | Kd | = | 1202.26 | nM | 5.92 |
| CHEMBL2348202 | — | Kd | = | 1230.27 | nM | 5.91 |
| CHEMBL2348218 | — | Kd | = | 1230.27 | nM | 5.91 |
| CHEMBL2348205 | — | Kd | = | 1380.38 | nM | 5.86 |
| CHEMBL2348207 | — | Kd | = | 1380.38 | nM | 5.86 |
| CHEMBL2348196 | — | Kd | = | 1380.38 | nM | 5.86 |
| CHEMBL2348210 | — | Kd | = | 1412.54 | nM | 5.85 |
| CHEMBL2348206 | — | Kd | = | 1445.44 | nM | 5.84 |
| CHEMBL280822 | CGP-20712A | Kd | = | 1513.56 | nM | 5.82 |
| CHEMBL2348214 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL2348208 | — | Kd | = | 1737.8 | nM | 5.76 |
| CHEMBL75753 | XAMOTEROL | Kd | = | 1737.8 | nM | 5.76 |
| CHEMBL2348201 | — | Kd | = | 2041.74 | nM | 5.69 |
| CHEMBL2348211 | — | Kd | = | 2630.27 | nM | 5.58 |
| CHEMBL2348200 | — | Kd | = | 2884.03 | nM | 5.54 |
| CHEMBL2348219 | — | Kd | = | 3548.13 | nM | 5.45 |
| CHEMBL207802 | LK-204545 | Kd | = | 5128.61 | nM | 5.29 |
| CHEMBL2348217 | — | Inhibition | - | % | - | |
| CHEMBL2348220 | — | Inhibition | - | % | - |