Assay Detail
Binding
CHEMBL3736956
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Antagonist activity at luciferase-fused ERalpha in human HEK293 cells expressing eYFP assessed as reduction of E2-induced estrogenic activity after 2 hrs by BRET assay
12
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.58 | 7.30 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3735770 | — | — | 2 | 7.30 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 7.16 |
| CHEMBL3735995 | — | — | 2 | 6.68 |
| CHEMBL1222035 | — | — | 1 | 6.47 |
| CHEMBL3735106 | — | — | 2 | 6.29 |
| CHEMBL3735187 | — | — | 2 | 5.59 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL27759 | ENTINOSTAT | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3735770 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3735995 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1222035 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3735106 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3735187 | — | IC50 | = | 2550.0 | nM | 5.59 |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - | |
| CHEMBL27759 | ENTINOSTAT | IC50 | - | — | - | |
| CHEMBL3735106 | — | Inhibition | - | % | - | |
| CHEMBL3735995 | — | Inhibition | - | % | - | |
| CHEMBL3735187 | — | Inhibition | - | % | - | |
| CHEMBL3735770 | — | Inhibition | - | % | - |