Assay Detail
Binding
CHEMBL827429
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Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +++:highly active
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Prostate gland |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 9.61 | 10.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24778 | SILODOSIN | 4.0 | 1 | 10.44 |
| CHEMBL405355 | NIGULDIPINE | 2.0 | 1 | 9.80 |
| CHEMBL96467 | — | — | 1 | 9.77 |
| CHEMBL179334 | — | — | 1 | 9.74 |
| CHEMBL181215 | — | — | 1 | 9.70 |
| CHEMBL356584 | — | — | 1 | 9.70 |
| CHEMBL836 | TAMSULOSIN | 4.0 | 1 | 9.70 |
| CHEMBL40650 | — | — | 1 | 9.66 |
| CHEMBL56331 | — | — | 1 | 9.60 |
| CHEMBL72657 | — | — | 1 | 9.46 |
| CHEMBL182998 | — | — | 1 | 9.44 |
| CHEMBL180932 | — | — | 1 | 9.40 |
| CHEMBL25300 | — | — | 1 | 9.40 |
| CHEMBL88272 | — | — | 1 | 9.22 |
| CHEMBL12062 | RWJ-69736 | — | 1 | 9.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24778 | SILODOSIN | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL405355 | NIGULDIPINE | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL96467 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL179334 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL181215 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL356584 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL836 | TAMSULOSIN | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL40650 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL56331 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL72657 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL182998 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL180932 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL25300 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL88272 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL12062 | RWJ-69736 | Ki | = | 0.65 | nM | 9.19 |