Assay Detail
Functional
CHEMBL1046466
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Antiproliferative activity against human MDA-MB-435 cells by Brdu incorporation assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-435 |
| 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 | 23 | 5.08 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603960 | — | — | 1 | 6.62 |
| CHEMBL594117 | — | — | 1 | 6.24 |
| CHEMBL609566 | — | — | 1 | 6.14 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | 2.0 | 1 | 6.00 |
| CHEMBL608104 | — | — | 1 | 5.66 |
| CHEMBL595878 | — | — | 1 | 5.60 |
| CHEMBL595755 | — | — | 1 | 5.48 |
| CHEMBL594474 | — | — | 1 | 5.15 |
| CHEMBL605513 | — | — | 1 | 5.10 |
| CHEMBL593102 | — | — | 1 | 5.06 |
| CHEMBL593789 | — | — | 1 | 5.01 |
| CHEMBL595756 | — | — | 1 | 4.85 |
| CHEMBL604882 | — | — | 1 | 4.75 |
| CHEMBL608114 | — | — | 1 | 4.61 |
| CHEMBL595647 | — | — | 1 | 4.57 |
| CHEMBL604895 | — | — | 1 | 4.47 |
| CHEMBL595667 | — | — | 1 | 4.41 |
| CHEMBL261406 | — | — | 1 | 4.38 |
| CHEMBL594568 | — | — | 1 | 4.32 |
| CHEMBL595421 | — | — | 1 | 4.14 |
| CHEMBL594118 | — | — | 1 | 4.02 |
| CHEMBL603320 | — | — | 1 | - |
| CHEMBL595896 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603960 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL594117 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL609566 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL299613 | 2-METHOXYESTRADIOL | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL608104 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL595878 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL595755 | — | IC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL594474 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL605513 | — | IC50 | = | 7890.0 | nM | 5.10 |
| CHEMBL593102 | — | IC50 | = | 8680.0 | nM | 5.06 |
| CHEMBL593789 | — | IC50 | = | 9770.0 | nM | 5.01 |
| CHEMBL595756 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL604882 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL608114 | — | IC50 | = | 24590.0 | nM | 4.61 |
| CHEMBL595647 | — | IC50 | = | 26760.0 | nM | 4.57 |
| CHEMBL604895 | — | IC50 | = | 33470.0 | nM | 4.47 |
| CHEMBL595667 | — | IC50 | = | 39330.0 | nM | 4.41 |
| CHEMBL261406 | — | IC50 | = | 41260.0 | nM | 4.38 |
| CHEMBL594568 | — | IC50 | = | 48060.0 | nM | 4.32 |
| CHEMBL595421 | — | IC50 | = | 72540.0 | nM | 4.14 |
| CHEMBL594118 | — | IC50 | = | 95310.0 | nM | 4.02 |
| CHEMBL603320 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL595896 | — | IC50 | > | 100000.0 | nM | - |