Assay Detail
Binding
CHEMBL647749
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Inhibition of 1.0 nM [3H]mibolerone binding to human androgen receptor of PC3/AR cell lysate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC3/AR |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.19 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL146858 | — | — | 1 | 8.22 |
| CHEMBL1274 | NILUTAMIDE | 4.0 | 1 | 8.05 |
| CHEMBL151601 | — | — | 1 | 7.31 |
| CHEMBL146794 | — | — | 1 | 7.11 |
| CHEMBL2112885 | — | — | 1 | 7.05 |
| CHEMBL806 | FLUTAMIDE | 4.0 | 1 | 6.81 |
| CHEMBL348495 | — | — | 1 | 6.48 |
| CHEMBL347556 | — | — | 1 | 6.46 |
| CHEMBL27577 | SALICYLAMIDE | 2.0 | 1 | - |
| CHEMBL147457 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL146858 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1274 | NILUTAMIDE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL151601 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL146794 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL2112885 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL348495 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL347556 | — | IC50 | = | 346.0 | nM | 6.46 |
| CHEMBL27577 | SALICYLAMIDE | IC50 | > | 1000.0 | nM | - |
| CHEMBL147457 | — | IC50 | > | 1000.0 | nM | - |