Assay Detail
Binding
CHEMBL3744075
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Antagonist activity at adrenergic alpha1D receptor (unknown origin) by firefly and renilla dual glo luciferase assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.62 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3742276 | — | — | 1 | 8.00 |
| CHEMBL3739533 | — | — | 1 | 7.95 |
| CHEMBL3742253 | — | — | 1 | 7.89 |
| CHEMBL3739762 | — | — | 1 | 7.78 |
| CHEMBL3742103 | — | — | 1 | 7.50 |
| CHEMBL3741483 | — | — | 1 | 7.45 |
| CHEMBL3742198 | — | — | 1 | 7.44 |
| CHEMBL142635 | NAFTOPIDIL | 4.0 | 1 | 7.26 |
| CHEMBL3741260 | — | — | 1 | 7.20 |
| CHEMBL3739900 | — | — | 1 | 6.94 |
| CHEMBL3740847 | — | — | 1 | 6.91 |
| CHEMBL3739542 | — | — | 1 | 6.79 |
| CHEMBL3740351 | — | — | 1 | 6.62 |
| CHEMBL3740019 | — | — | 1 | 6.46 |
| CHEMBL3741161 | — | — | 1 | 6.31 |
| CHEMBL3740558 | — | — | 1 | 6.06 |
| CHEMBL3740874 | — | — | 1 | 6.02 |
| CHEMBL3741318 | — | — | 1 | 5.91 |
| CHEMBL3741658 | — | — | 1 | 5.75 |
| CHEMBL3739513 | — | — | 1 | 5.73 |
| CHEMBL3741079 | — | — | 1 | 5.13 |
| CHEMBL3739505 | — | — | 1 | 4.97 |
| CHEMBL3740042 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3742276 | — | IC50 | = | 10.07 | nM | 8.00 |
| CHEMBL3739533 | — | IC50 | = | 11.31 | nM | 7.95 |
| CHEMBL3742253 | — | IC50 | = | 12.87 | nM | 7.89 |
| CHEMBL3739762 | — | IC50 | = | 16.73 | nM | 7.78 |
| CHEMBL3742103 | — | IC50 | = | 31.28 | nM | 7.50 |
| CHEMBL3741483 | — | IC50 | = | 35.16 | nM | 7.45 |
| CHEMBL3742198 | — | IC50 | = | 36.62 | nM | 7.44 |
| CHEMBL142635 | NAFTOPIDIL | IC50 | = | 55.2 | nM | 7.26 |
| CHEMBL3741260 | — | IC50 | = | 63.54 | nM | 7.20 |
| CHEMBL3739900 | — | IC50 | = | 115.5 | nM | 6.94 |
| CHEMBL3740847 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3739542 | — | IC50 | = | 163.7 | nM | 6.79 |
| CHEMBL3740351 | — | IC50 | = | 239.9 | nM | 6.62 |
| CHEMBL3740019 | — | IC50 | = | 343.6 | nM | 6.46 |
| CHEMBL3741161 | — | IC50 | = | 493.3 | nM | 6.31 |
| CHEMBL3740558 | — | IC50 | = | 866.4 | nM | 6.06 |
| CHEMBL3740874 | — | IC50 | = | 957.2 | nM | 6.02 |
| CHEMBL3741318 | — | IC50 | = | 1235.0 | nM | 5.91 |
| CHEMBL3741658 | — | IC50 | = | 1758.0 | nM | 5.75 |
| CHEMBL3739513 | — | IC50 | = | 1862.0 | nM | 5.73 |
| CHEMBL3741079 | — | IC50 | = | 7426.0 | nM | 5.13 |
| CHEMBL3739505 | — | IC50 | = | 10630.0 | nM | 4.97 |
| CHEMBL3740042 | — | IC50 | = | 80550.0 | nM | 4.09 |