Assay Detail
Binding
CHEMBL3744074
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at adrenergic alpha1B 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 | 6.58 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3739533 | — | — | 1 | 7.90 |
| CHEMBL3742253 | — | — | 1 | 7.71 |
| CHEMBL3740019 | — | — | 1 | 7.54 |
| CHEMBL3742103 | — | — | 1 | 7.50 |
| CHEMBL3740874 | — | — | 1 | 7.46 |
| CHEMBL3741318 | — | — | 1 | 7.00 |
| CHEMBL3740558 | — | — | 1 | 6.91 |
| CHEMBL3739762 | — | — | 1 | 6.75 |
| CHEMBL3742276 | — | — | 1 | 6.70 |
| CHEMBL3739542 | — | — | 1 | 6.60 |
| CHEMBL3739513 | — | — | 1 | 6.39 |
| CHEMBL3740351 | — | — | 1 | 6.36 |
| CHEMBL142635 | NAFTOPIDIL | 4.0 | 1 | 6.20 |
| CHEMBL3740847 | — | — | 1 | 6.17 |
| CHEMBL3742198 | — | — | 1 | 6.11 |
| CHEMBL3741260 | — | — | 1 | 6.11 |
| CHEMBL3741483 | — | — | 1 | 6.10 |
| CHEMBL3741161 | — | — | 1 | 6.10 |
| CHEMBL3741658 | — | — | 1 | 6.06 |
| CHEMBL3740042 | — | — | 1 | 6.02 |
| CHEMBL3741079 | — | — | 1 | 6.00 |
| CHEMBL3739900 | — | — | 1 | 6.00 |
| CHEMBL3739505 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3739533 | — | IC50 | = | 12.57 | nM | 7.90 |
| CHEMBL3742253 | — | IC50 | = | 19.69 | nM | 7.71 |
| CHEMBL3740019 | — | IC50 | = | 28.91 | nM | 7.54 |
| CHEMBL3742103 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3740874 | — | IC50 | = | 34.76 | nM | 7.46 |
| CHEMBL3741318 | — | IC50 | = | 100.9 | nM | 7.00 |
| CHEMBL3740558 | — | IC50 | = | 121.9 | nM | 6.91 |
| CHEMBL3739762 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3742276 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3739542 | — | IC50 | = | 250.4 | nM | 6.60 |
| CHEMBL3739513 | — | IC50 | = | 406.2 | nM | 6.39 |
| CHEMBL3740351 | — | IC50 | = | 433.3 | nM | 6.36 |
| CHEMBL142635 | NAFTOPIDIL | IC50 | = | 634.0 | nM | 6.20 |
| CHEMBL3740847 | — | IC50 | = | 684.0 | nM | 6.17 |
| CHEMBL3742198 | — | IC50 | = | 781.5 | nM | 6.11 |
| CHEMBL3741260 | — | IC50 | = | 769.4 | nM | 6.11 |
| CHEMBL3741483 | — | IC50 | = | 794.4 | nM | 6.10 |
| CHEMBL3741161 | — | IC50 | = | 787.5 | nM | 6.10 |
| CHEMBL3741658 | — | IC50 | = | 875.3 | nM | 6.06 |
| CHEMBL3740042 | — | IC50 | = | 948.8 | nM | 6.02 |
| CHEMBL3741079 | — | IC50 | = | 1003.0 | nM | 6.00 |
| CHEMBL3739900 | — | IC50 | = | 1007.0 | nM | 6.00 |
| CHEMBL3739505 | — | IC50 | = | 1876.0 | nM | 5.73 |