Assay Detail
Binding
CHEMBL4024646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of selective estrogen receptor alpha degradation in human MCF7 cells after 18 to 24 hrs by in-cell Western analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.48 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069711 | — | — | 1 | 9.70 |
| CHEMBL4076124 | LSZ-102 | 1.0 | 1 | 9.70 |
| CHEMBL4091432 | — | — | 1 | 9.52 |
| CHEMBL4082510 | — | — | 1 | 9.40 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 1 | 9.30 |
| CHEMBL4098433 | — | — | 1 | 9.00 |
| CHEMBL4069567 | — | — | 1 | 9.00 |
| CHEMBL4076693 | — | — | 1 | 9.00 |
| CHEMBL4059818 | — | — | 1 | 9.00 |
| CHEMBL4063737 | — | — | 1 | 9.00 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.92 |
| CHEMBL4064146 | — | — | 1 | 8.52 |
| CHEMBL4091541 | — | — | 1 | 8.40 |
| CHEMBL4101673 | — | — | 1 | 8.40 |
| CHEMBL4091898 | — | — | 1 | 8.38 |
| CHEMBL4091321 | — | — | 1 | 8.27 |
| CHEMBL4086984 | — | — | 1 | 8.22 |
| CHEMBL4068267 | — | — | 1 | 7.96 |
| CHEMBL4087507 | — | — | 1 | 7.77 |
| CHEMBL4102815 | — | — | 1 | 7.58 |
| CHEMBL4086258 | — | — | 1 | 7.58 |
| CHEMBL4092625 | — | — | 1 | 7.51 |
| CHEMBL4087929 | — | — | 1 | 7.47 |
| CHEMBL4080411 | — | — | 1 | 7.24 |
| CHEMBL4059624 | — | — | 1 | 7.22 |
| CHEMBL4064736 | — | — | 1 | - |
| CHEMBL4080048 | — | — | 1 | - |
| CHEMBL4098078 | — | — | 1 | - |
| CHEMBL4064926 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069711 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4076124 | LSZ-102 | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4091432 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4082510 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3581693 | BRILANESTRANT | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4098433 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4069567 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4076693 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4059818 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4063737 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4064146 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4091541 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4101673 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4091898 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4091321 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4086984 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4068267 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4087507 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4102815 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4086258 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4092625 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4087929 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4080411 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4059624 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4064736 | — | IC50 | - | — | - | |
| CHEMBL4080048 | — | IC50 | - | — | - | |
| CHEMBL4098078 | — | IC50 | - | — | - | |
| CHEMBL4064926 | — | IC50 | - | — | - |