Assay Detail
Functional
CHEMBL1833712
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Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 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 | 7.09 | 7.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1830617 | — | — | 1 | 7.63 |
| CHEMBL1830485 | — | — | 1 | 7.58 |
| CHEMBL1830493 | — | — | 1 | 7.38 |
| CHEMBL1830619 | — | — | 1 | 7.24 |
| CHEMBL1830492 | — | — | 1 | 7.24 |
| CHEMBL1830618 | — | — | 1 | 7.21 |
| CHEMBL1830488 | — | — | 1 | 7.20 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 7.12 |
| CHEMBL1830489 | — | — | 1 | 7.10 |
| CHEMBL1830491 | — | — | 1 | 6.97 |
| CHEMBL1830490 | — | — | 1 | 6.94 |
| CHEMBL1830487 | — | — | 1 | 6.85 |
| CHEMBL1830486 | — | — | 1 | 6.82 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 6.79 |
| CHEMBL1830620 | — | — | 1 | 6.75 |
| CHEMBL1830621 | — | — | 1 | 6.54 |
| CHEMBL500 | PINDOLOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1830617 | — | Kd | = | 23.44 | nM | 7.63 |
| CHEMBL1830485 | — | Kd | = | 26.3 | nM | 7.58 |
| CHEMBL1830493 | — | Kd | = | 41.69 | nM | 7.38 |
| CHEMBL1830619 | — | Kd | = | 57.54 | nM | 7.24 |
| CHEMBL1830492 | — | Kd | = | 57.54 | nM | 7.24 |
| CHEMBL1830618 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL1830488 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL266195 | ALPRENOLOL | Kd | = | 75.86 | nM | 7.12 |
| CHEMBL1830489 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL1830491 | — | Kd | = | 107.15 | nM | 6.97 |
| CHEMBL1830490 | — | Kd | = | 114.82 | nM | 6.94 |
| CHEMBL1830487 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL1830486 | — | Kd | = | 151.36 | nM | 6.82 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL1830620 | — | Kd | = | 177.83 | nM | 6.75 |
| CHEMBL1830621 | — | Kd | = | 288.4 | nM | 6.54 |
| CHEMBL500 | PINDOLOL | Kd | < | 1000.0 | nM | - |