Assay Detail
Functional
CHEMBL836811
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Inhibition of 10e-9 M E2 stimulated transcriptional activation in ER+MCF-7/2a breast cancer cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Cancer cell lines |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.10 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.30 |
| CHEMBL184285 | — | — | 1 | 8.00 |
| CHEMBL185209 | — | — | 1 | 8.00 |
| CHEMBL184074 | — | — | 1 | 7.70 |
| CHEMBL365089 | — | — | 1 | 7.30 |
| CHEMBL426065 | — | — | 1 | 6.89 |
| CHEMBL186667 | — | — | 1 | 6.70 |
| CHEMBL181484 | — | — | 1 | 6.51 |
| CHEMBL183345 | — | — | 1 | 6.43 |
| CHEMBL184217 | — | — | 1 | 6.22 |
| CHEMBL366280 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1358 | FULVESTRANT | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL184285 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL185209 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL184074 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL365089 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL426065 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL186667 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL181484 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL183345 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL184217 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL366280 | — | IC50 | = | 790.0 | nM | 6.10 |