Assay Detail
ADMET
CHEMBL4375059
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DHA from beta1 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes measured after 90 mins by scintillation counting analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Probing the Existence of a Metastable Binding Site at the β<sub>2</sub>-Adrenergic Receptor with Homobivalent Bitopic Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.84 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514723 | — | — | 1 | 8.96 |
| CHEMBL4441975 | — | — | 1 | 8.90 |
| CHEMBL1160734 | — | — | 1 | 8.84 |
| CHEMBL4434772 | — | — | 1 | 8.74 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 8.55 |
| CHEMBL4462252 | — | — | 1 | 8.54 |
| CHEMBL4564189 | — | — | 1 | 8.40 |
| CHEMBL4527821 | — | — | 1 | 8.38 |
| CHEMBL4473518 | — | — | 1 | 8.19 |
| CHEMBL4594173 | — | — | 1 | 8.05 |
| CHEMBL4574652 | — | — | 1 | 7.71 |
| CHEMBL4446394 | — | — | 1 | 7.35 |
| CHEMBL1395661 | — | — | 1 | 7.19 |
| CHEMBL4442559 | — | — | 1 | 7.08 |
| CHEMBL4450606 | — | — | 1 | 6.57 |
| CHEMBL4530266 | — | — | 1 | 6.32 |
| CHEMBL4474813 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514723 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL4441975 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL1160734 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL4434772 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL266195 | ALPRENOLOL | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL4462252 | — | Ki | = | 2.884 | nM | 8.54 |
| CHEMBL4564189 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4527821 | — | Ki | = | 4.169 | nM | 8.38 |
| CHEMBL4473518 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL4594173 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL4574652 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL4446394 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL1395661 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL4442559 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL4450606 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL4530266 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL4474813 | — | Ki | = | 2570.4 | nM | 5.59 |