Assay Detail
Functional
CHEMBL1833709
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 cimeterol-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 | 7.68 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.74 |
| CHEMBL500 | PINDOLOL | 4.0 | 1 | 8.62 |
| CHEMBL1830491 | — | — | 1 | 8.46 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 8.37 |
| CHEMBL1830618 | — | — | 1 | 8.12 |
| CHEMBL1830485 | — | — | 1 | 8.08 |
| CHEMBL1830486 | — | — | 1 | 7.87 |
| CHEMBL1830619 | — | — | 1 | 7.76 |
| CHEMBL1830489 | — | — | 1 | 7.51 |
| CHEMBL1830621 | — | — | 1 | 7.42 |
| CHEMBL1830492 | — | — | 1 | 7.38 |
| CHEMBL1830617 | — | — | 1 | 7.36 |
| CHEMBL1830493 | — | — | 1 | 7.33 |
| CHEMBL1830487 | — | — | 1 | 7.28 |
| CHEMBL1830488 | — | — | 1 | 7.12 |
| CHEMBL1830490 | — | — | 1 | 6.66 |
| CHEMBL1830620 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | Kd | = | 1.82 | nM | 8.74 |
| CHEMBL500 | PINDOLOL | Kd | = | 2.399 | nM | 8.62 |
| CHEMBL1830491 | — | Kd | = | 3.467 | nM | 8.46 |
| CHEMBL266195 | ALPRENOLOL | Kd | = | 4.266 | nM | 8.37 |
| CHEMBL1830618 | — | Kd | = | 7.586 | nM | 8.12 |
| CHEMBL1830485 | — | Kd | = | 8.318 | nM | 8.08 |
| CHEMBL1830486 | — | Kd | = | 13.49 | nM | 7.87 |
| CHEMBL1830619 | — | Kd | = | 17.38 | nM | 7.76 |
| CHEMBL1830489 | — | Kd | = | 30.9 | nM | 7.51 |
| CHEMBL1830621 | — | Kd | = | 38.02 | nM | 7.42 |
| CHEMBL1830492 | — | Kd | = | 41.69 | nM | 7.38 |
| CHEMBL1830617 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL1830493 | — | Kd | = | 46.77 | nM | 7.33 |
| CHEMBL1830487 | — | Kd | = | 52.48 | nM | 7.28 |
| CHEMBL1830488 | — | Kd | = | 75.86 | nM | 7.12 |
| CHEMBL1830490 | — | Kd | = | 218.78 | nM | 6.66 |
| CHEMBL1830620 | — | Kd | = | 302.0 | nM | 6.52 |