Assay Detail
Functional
CHEMBL5525955
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at beta-2 AR (unknown origin) overexpressed in HEK293 cell membrane assessed as inhibition of ISO-induced cAMP production at EC80 preincubated for 15 mins followed by agonist addition measured after 30 mins by TR-FRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bitopic Ligands Support the Presence of a Metastable Binding Site at the β<sub>2</sub> Adrenergic Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.37 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1160734 | — | — | 1 | 8.64 |
| CHEMBL5564549 | — | — | 1 | 8.35 |
| CHEMBL5556781 | — | — | 1 | 8.33 |
| CHEMBL5557954 | — | — | 1 | 8.33 |
| CHEMBL5562658 | — | — | 1 | 8.27 |
| CHEMBL5568267 | — | — | 1 | 8.13 |
| CHEMBL5564461 | — | — | 1 | 8.00 |
| CHEMBL5568144 | — | — | 1 | 7.74 |
| CHEMBL5562430 | — | — | 1 | 7.10 |
| CHEMBL5561419 | — | — | 1 | 6.76 |
| CHEMBL5561967 | — | — | 1 | 5.50 |
| CHEMBL5564893 | — | — | 1 | 5.40 |
| CHEMBL5562644 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1160734 | — | IC50 | = | 2.291 | nM | 8.64 |
| CHEMBL5564549 | — | IC50 | = | 4.467 | nM | 8.35 |
| CHEMBL5556781 | — | IC50 | = | 4.677 | nM | 8.33 |
| CHEMBL5557954 | — | IC50 | = | 4.677 | nM | 8.33 |
| CHEMBL5562658 | — | IC50 | = | 5.37 | nM | 8.27 |
| CHEMBL5568267 | — | IC50 | = | 7.413 | nM | 8.13 |
| CHEMBL5564461 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5568144 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL5562430 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5561419 | — | IC50 | = | 173.78 | nM | 6.76 |
| CHEMBL5561967 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5564893 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL5562644 | — | IC50 | = | 4786.3 | nM | 5.32 |