Assay Detail
Binding
CHEMBL4424724
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by Alexafluor-488 conjugate anti-mouse IgG antibody/Hoechst 33342 staining based immunofluorescence imaging analysis
13
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 9.84 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439408 | — | — | 2 | 10.68 |
| CHEMBL4447340 | — | — | 1 | 10.52 |
| CHEMBL4464224 | — | — | 1 | 10.35 |
| CHEMBL4449709 | — | — | 1 | 10.29 |
| CHEMBL4437985 | — | — | 1 | 10.26 |
| CHEMBL4464058 | — | — | 1 | 10.23 |
| CHEMBL4539802 | — | — | 1 | 10.12 |
| CHEMBL4443826 | — | — | 2 | 9.62 |
| CHEMBL1087419 | — | — | 1 | 9.55 |
| CHEMBL4464146 | — | — | 2 | 9.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439408 | — | IC50 | = | 0.021 | nM | 10.68 |
| CHEMBL4439408 | — | IC50 | = | 0.024 | nM | 10.62 |
| CHEMBL4447340 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4464224 | — | IC50 | = | 0.045 | nM | 10.35 |
| CHEMBL4449709 | — | IC50 | = | 0.051 | nM | 10.29 |
| CHEMBL4437985 | — | IC50 | = | 0.055 | nM | 10.26 |
| CHEMBL4464058 | — | IC50 | = | 0.059 | nM | 10.23 |
| CHEMBL4539802 | — | IC50 | = | 0.076 | nM | 10.12 |
| CHEMBL4443826 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL1087419 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4464146 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4443826 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4464146 | — | IC50 | = | 9.6 | nM | 8.02 |