Assay Detail
ADMET
CHEMBL4375055
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Antagonist activity at beta1 adrenergic receptor (unknown origin) stably expressed in HEK293 cell membranes assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 30 mins by TR-FRET assay
24
Total Activities
24
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 |
|---|---|---|---|
| IC50 | 24 | 7.00 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4514723 | — | — | 1 | 8.33 |
| CHEMBL4465278 | — | — | 1 | 8.25 |
| CHEMBL1160734 | — | — | 1 | 8.23 |
| CHEMBL4434772 | — | — | 1 | 7.95 |
| CHEMBL4441975 | — | — | 1 | 7.86 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 7.86 |
| CHEMBL4564189 | — | — | 1 | 7.84 |
| CHEMBL4462252 | — | — | 1 | 7.71 |
| CHEMBL4527821 | — | — | 1 | 7.70 |
| CHEMBL4594173 | — | — | 1 | 7.58 |
| CHEMBL4473518 | — | — | 1 | 7.56 |
| CHEMBL4584173 | — | — | 1 | 7.55 |
| CHEMBL4557995 | — | — | 1 | 7.01 |
| CHEMBL4574652 | — | — | 1 | 6.90 |
| CHEMBL4472564 | — | — | 1 | 6.74 |
| CHEMBL41189 | — | — | 1 | 6.63 |
| CHEMBL4446394 | — | — | 1 | 6.43 |
| CHEMBL1395661 | — | — | 1 | 6.36 |
| CHEMBL4442559 | — | — | 1 | 6.31 |
| CHEMBL4459989 | — | — | 1 | 5.75 |
| CHEMBL4450606 | — | — | 1 | 5.69 |
| CHEMBL4530266 | — | — | 1 | 5.44 |
| CHEMBL4556017 | — | — | 1 | 5.35 |
| CHEMBL4474813 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4514723 | — | IC50 | = | 4.677 | nM | 8.33 |
| CHEMBL4465278 | — | IC50 | = | 5.623 | nM | 8.25 |
| CHEMBL1160734 | — | IC50 | = | 5.888 | nM | 8.23 |
| CHEMBL4434772 | — | IC50 | = | 11.22 | nM | 7.95 |
| CHEMBL4441975 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL266195 | ALPRENOLOL | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4564189 | — | IC50 | = | 14.45 | nM | 7.84 |
| CHEMBL4462252 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4527821 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4594173 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL4473518 | — | IC50 | = | 27.54 | nM | 7.56 |
| CHEMBL4584173 | — | IC50 | = | 28.18 | nM | 7.55 |
| CHEMBL4557995 | — | IC50 | = | 97.72 | nM | 7.01 |
| CHEMBL4574652 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4472564 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL41189 | — | IC50 | = | 234.42 | nM | 6.63 |
| CHEMBL4446394 | — | IC50 | = | 371.54 | nM | 6.43 |
| CHEMBL1395661 | — | IC50 | = | 436.52 | nM | 6.36 |
| CHEMBL4442559 | — | IC50 | = | 489.78 | nM | 6.31 |
| CHEMBL4459989 | — | IC50 | = | 1778.28 | nM | 5.75 |
| CHEMBL4450606 | — | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL4530266 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL4556017 | — | IC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL4474813 | — | IC50 | = | 10964.78 | nM | 4.96 |