Assay Detail
Binding
CHEMBL4822809
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Antagonist activity at ERalpha (unknown origin) expressed in human HEK293T cells assessed as inhibition of 17beta-estradiol-induced transcriptional activities by measuring ERE driven reporter gene expression measured after 24 hrs by dual luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.74 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800654 | — | — | 1 | 7.38 |
| CHEMBL4875988 | — | — | 1 | 7.37 |
| CHEMBL4852827 | — | — | 1 | 5.96 |
| CHEMBL4853571 | — | — | 1 | 5.90 |
| CHEMBL4851145 | — | — | 1 | 5.86 |
| CHEMBL4869951 | — | — | 1 | 5.73 |
| CHEMBL4874175 | — | — | 1 | 5.68 |
| CHEMBL4849015 | — | — | 1 | 5.63 |
| CHEMBL4878251 | — | — | 1 | 5.58 |
| CHEMBL4870293 | — | — | 1 | 5.50 |
| CHEMBL4873312 | — | — | 1 | 5.43 |
| CHEMBL4855392 | — | — | 1 | 5.29 |
| CHEMBL4868001 | — | — | 1 | 5.28 |
| CHEMBL4849503 | — | — | 1 | 5.25 |
| CHEMBL4851237 | — | — | 1 | 5.24 |
| CHEMBL4874242 | — | — | 1 | 5.23 |
| CHEMBL4859208 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800654 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4875988 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4852827 | — | IC50 | = | 1106.0 | nM | 5.96 |
| CHEMBL4853571 | — | IC50 | = | 1254.0 | nM | 5.90 |
| CHEMBL4851145 | — | IC50 | = | 1396.0 | nM | 5.86 |
| CHEMBL4869951 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL4874175 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4849015 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL4878251 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL4870293 | — | IC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL4873312 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL4855392 | — | IC50 | = | 5075.0 | nM | 5.29 |
| CHEMBL4868001 | — | IC50 | = | 5270.0 | nM | 5.28 |
| CHEMBL4849503 | — | IC50 | = | 5670.0 | nM | 5.25 |
| CHEMBL4851237 | — | IC50 | = | 5781.0 | nM | 5.24 |
| CHEMBL4874242 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4859208 | — | IC50 | = | 6120.0 | nM | 5.21 |