Assay Detail
Functional
CHEMBL1833710
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
17
Total Activities
17
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 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 | 6.85 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1830618 | — | — | 1 | 7.38 |
| CHEMBL1830491 | — | — | 1 | 7.17 |
| CHEMBL1830493 | — | — | 1 | 7.13 |
| CHEMBL1830619 | — | — | 1 | 7.11 |
| CHEMBL1830485 | — | — | 1 | 7.04 |
| CHEMBL1830492 | — | — | 1 | 6.95 |
| CHEMBL1830617 | — | — | 1 | 6.92 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 6.75 |
| CHEMBL1830486 | — | — | 1 | 6.74 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 6.70 |
| CHEMBL1830489 | — | — | 1 | 6.62 |
| CHEMBL1830488 | — | — | 1 | 6.45 |
| CHEMBL1830487 | — | — | 1 | 6.10 |
| CHEMBL1830490 | — | — | 1 | - |
| CHEMBL500 | PINDOLOL | 4.0 | 1 | - |
| CHEMBL1830620 | — | — | 1 | - |
| CHEMBL1830621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1830618 | — | Kd | = | 41.69 | nM | 7.38 |
| CHEMBL1830491 | — | Kd | = | 67.61 | nM | 7.17 |
| CHEMBL1830493 | — | Kd | = | 74.13 | nM | 7.13 |
| CHEMBL1830619 | — | Kd | = | 77.62 | nM | 7.11 |
| CHEMBL1830485 | — | Kd | = | 91.2 | nM | 7.04 |
| CHEMBL1830492 | — | Kd | = | 112.2 | nM | 6.95 |
| CHEMBL1830617 | — | Kd | = | 120.23 | nM | 6.92 |
| CHEMBL266195 | ALPRENOLOL | Kd | = | 177.83 | nM | 6.75 |
| CHEMBL1830486 | — | Kd | = | 181.97 | nM | 6.74 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL1830489 | — | Kd | = | 239.88 | nM | 6.62 |
| CHEMBL1830488 | — | Kd | = | 354.81 | nM | 6.45 |
| CHEMBL1830487 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL1830490 | — | Kd | < | 1000.0 | nM | - |
| CHEMBL500 | PINDOLOL | Kd | < | 10000.0 | nM | - |
| CHEMBL1830620 | — | Kd | < | 1000.0 | nM | - |
| CHEMBL1830621 | — | Kd | < | 1000.0 | nM | - |