Assay Detail
Functional
CHEMBL1046468
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Antiproliferative activity against human PC3 cells by Brdu incorporation assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PC-3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis of 2- and 17-substituted estrone analogs and their antiproliferative structure-activity relationships compared to 2-methoxyestradiol.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.88 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL609566 | — | — | 1 | 6.21 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | 2.0 | 1 | 5.58 |
| CHEMBL595755 | — | — | 1 | 5.19 |
| CHEMBL593102 | — | — | 1 | 5.09 |
| CHEMBL608104 | — | — | 1 | 5.07 |
| CHEMBL594568 | — | — | 1 | 5.06 |
| CHEMBL593789 | — | — | 1 | 4.86 |
| CHEMBL595878 | — | — | 1 | 4.67 |
| CHEMBL261406 | — | — | 1 | 4.66 |
| CHEMBL595647 | — | — | 1 | 4.64 |
| CHEMBL604882 | — | — | 1 | 4.63 |
| CHEMBL595667 | — | — | 1 | 4.58 |
| CHEMBL608114 | — | — | 1 | 4.58 |
| CHEMBL595421 | — | — | 1 | 4.57 |
| CHEMBL604895 | — | — | 1 | 4.54 |
| CHEMBL594118 | — | — | 1 | 4.07 |
| CHEMBL603320 | — | — | 1 | - |
| CHEMBL595896 | — | — | 1 | - |
| CHEMBL594474 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL609566 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL595755 | — | IC50 | = | 6460.0 | nM | 5.19 |
| CHEMBL593102 | — | IC50 | = | 8110.0 | nM | 5.09 |
| CHEMBL608104 | — | IC50 | = | 8490.0 | nM | 5.07 |
| CHEMBL594568 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL593789 | — | IC50 | = | 13820.0 | nM | 4.86 |
| CHEMBL595878 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL261406 | — | IC50 | = | 21990.0 | nM | 4.66 |
| CHEMBL595647 | — | IC50 | = | 22820.0 | nM | 4.64 |
| CHEMBL604882 | — | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL595667 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL608114 | — | IC50 | = | 25990.0 | nM | 4.58 |
| CHEMBL595421 | — | IC50 | = | 27190.0 | nM | 4.57 |
| CHEMBL604895 | — | IC50 | = | 28820.0 | nM | 4.54 |
| CHEMBL594118 | — | IC50 | = | 85440.0 | nM | 4.07 |
| CHEMBL603320 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL595896 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL594474 | — | IC50 | - | — | - |