Assay Detail
Binding
CHEMBL4390558
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Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst 33342 staining based immunofluorescence imaging analysis
30
Total Activities
30
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
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 9.22 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4591338 | — | — | 1 | 11.00 |
| CHEMBL4441471 | — | — | 1 | 10.52 |
| CHEMBL4447340 | — | — | 1 | 10.52 |
| CHEMBL4455953 | — | — | 1 | 10.30 |
| CHEMBL4463541 | — | — | 1 | 10.15 |
| CHEMBL4594150 | — | — | 1 | 10.10 |
| CHEMBL4447143 | — | — | 1 | 9.77 |
| CHEMBL4476031 | — | — | 1 | 9.70 |
| CHEMBL4567402 | — | — | 1 | 9.70 |
| CHEMBL4450730 | — | — | 1 | 9.55 |
| CHEMBL4588281 | — | — | 1 | 9.52 |
| CHEMBL4438260 | — | — | 1 | 9.52 |
| CHEMBL4456532 | — | — | 1 | 9.38 |
| CHEMBL4468700 | — | — | 1 | 9.30 |
| CHEMBL4552853 | — | — | 1 | 9.30 |
| CHEMBL4470926 | — | — | 1 | 9.30 |
| CHEMBL4462970 | — | — | 1 | 9.24 |
| CHEMBL4586333 | — | — | 1 | 9.00 |
| CHEMBL4543969 | — | — | 1 | 8.96 |
| CHEMBL4531089 | — | — | 1 | 8.60 |
| CHEMBL4534455 | — | — | 1 | 8.52 |
| CHEMBL4460089 | — | — | 1 | 8.24 |
| CHEMBL4451300 | — | — | 1 | 7.82 |
| CHEMBL4437725 | — | — | 1 | 7.57 |
| CHEMBL4578130 | — | — | 1 | 7.14 |
| CHEMBL4544038 | — | — | 1 | 7.00 |
| CHEMBL4482870 | — | — | 1 | - |
| CHEMBL4476007 | — | — | 1 | - |
| CHEMBL4543659 | — | — | 1 | - |
| CHEMBL4564477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4591338 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL4441471 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4447340 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL4455953 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4463541 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4594150 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4447143 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4476031 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4567402 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4450730 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL4588281 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4438260 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4456532 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4468700 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4552853 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4470926 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4462970 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4586333 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4543969 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4531089 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4534455 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4460089 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4451300 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4437725 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4578130 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4544038 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4482870 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4476007 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4543659 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4564477 | — | IC50 | > | 100.0 | nM | - |