Assay Detail
Binding
CHEMBL913352
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Displacement of [3H]DHT from human AR in MDA453 cells
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA453 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.59 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | 2.0 | 1 | 9.52 |
| CHEMBL384533 | — | — | 1 | 9.00 |
| CHEMBL220359 | — | — | 2 | 8.82 |
| CHEMBL219198 | — | — | 1 | 8.82 |
| CHEMBL374121 | — | — | 1 | 8.77 |
| CHEMBL425646 | — | — | 2 | 8.49 |
| CHEMBL374781 | — | — | 1 | 8.46 |
| CHEMBL2096842 | — | — | 1 | 8.37 |
| CHEMBL218914 | — | — | 1 | 8.26 |
| CHEMBL218809 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27769 | STANOLONE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL384533 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL220359 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL219198 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL374121 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL220359 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL425646 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL374781 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL2096842 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL425646 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL218914 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL218809 | — | Ki | = | 24.0 | nM | 7.62 |