Assay Detail
Binding
CHEMBL1833706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells
19
Total Activities
17
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 characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 17 | 7.34 | 8.58 |
| Imax | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL500 | PINDOLOL | 4.0 | 1 | 8.58 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.22 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 7.95 |
| CHEMBL1830491 | — | — | 1 | 7.76 |
| CHEMBL1830618 | — | — | 1 | 7.65 |
| CHEMBL1830619 | — | — | 1 | 7.50 |
| CHEMBL1830486 | — | — | 1 | 7.48 |
| CHEMBL1830485 | — | — | 1 | 7.44 |
| CHEMBL1830617 | — | — | 1 | 7.26 |
| CHEMBL1830489 | — | — | 1 | 7.25 |
| CHEMBL1830492 | — | — | 1 | 7.14 |
| CHEMBL1830488 | — | — | 1 | 7.05 |
| CHEMBL1830493 | — | — | 1 | 7.04 |
| CHEMBL1830621 | — | — | 1 | 7.01 |
| CHEMBL1830487 | — | — | 2 | 6.73 |
| CHEMBL1830490 | — | — | 2 | 6.72 |
| CHEMBL1830620 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL500 | PINDOLOL | Kd | = | 2.63 | nM | 8.58 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 6.026 | nM | 8.22 |
| CHEMBL266195 | ALPRENOLOL | Kd | = | 11.22 | nM | 7.95 |
| CHEMBL1830491 | — | Kd | = | 17.38 | nM | 7.76 |
| CHEMBL1830618 | — | Kd | = | 22.39 | nM | 7.65 |
| CHEMBL1830619 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL1830486 | — | Kd | = | 33.11 | nM | 7.48 |
| CHEMBL1830485 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL1830617 | — | Kd | = | 54.95 | nM | 7.26 |
| CHEMBL1830489 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL1830492 | — | Kd | = | 72.44 | nM | 7.14 |
| CHEMBL1830488 | — | Kd | = | 89.13 | nM | 7.05 |
| CHEMBL1830493 | — | Kd | = | 91.2 | nM | 7.04 |
| CHEMBL1830621 | — | Kd | = | 97.72 | nM | 7.01 |
| CHEMBL1830487 | — | Kd | = | 186.21 | nM | 6.73 |
| CHEMBL1830490 | — | Kd | = | 190.55 | nM | 6.72 |
| CHEMBL1830620 | — | Kd | = | 870.96 | nM | 6.06 |
| CHEMBL1830490 | — | Imax | = | 65.9 | % | - |
| CHEMBL1830487 | — | Imax | = | 85.3 | % | - |