Assay Detail
Binding
CHEMBL5525959
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Displacement of [3H]-DHA from beta-2 AR (unknown origin) overexpressed in HEK293 cell membrane assessed as dissociation constant (K) incubated for 90 mins by liquid scintillation analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Kd | 8 | 8.19 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5564549 | — | — | 1 | 9.37 |
| CHEMBL1160734 | — | — | 1 | 9.30 |
| CHEMBL5557954 | — | — | 1 | 9.10 |
| CHEMBL5562658 | — | — | 1 | 8.95 |
| CHEMBL5568144 | — | — | 1 | 8.58 |
| CHEMBL5561419 | — | — | 1 | 7.91 |
| CHEMBL5562644 | — | — | 1 | 6.23 |
| CHEMBL5561967 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5564549 | — | Kd | = | 0.4266 | nM | 9.37 |
| CHEMBL1160734 | — | Kd | = | 0.5012 | nM | 9.30 |
| CHEMBL5557954 | — | Kd | = | 0.7943 | nM | 9.10 |
| CHEMBL5562658 | — | Kd | = | 1.122 | nM | 8.95 |
| CHEMBL5568144 | — | Kd | = | 2.63 | nM | 8.58 |
| CHEMBL5561419 | — | Kd | = | 12.3 | nM | 7.91 |
| CHEMBL5562644 | — | Kd | = | 588.84 | nM | 6.23 |
| CHEMBL5561967 | — | Kd | = | 831.76 | nM | 6.08 |