Assay Detail
Binding
CHEMBL4024644
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 harboring TK-ERE-Luc assessed as reduction in estradiol-induced transcriptional activity after 24 hrs by luciferase reporter gene assay
46
Total Activities
46
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 | 46 | 6.95 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059624 | — | — | 1 | 9.00 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 8.52 |
| CHEMBL4087929 | — | — | 1 | 8.52 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.47 |
| CHEMBL4076124 | LSZ-102 | 1.0 | 1 | 8.22 |
| CHEMBL4082510 | — | — | 1 | 8.22 |
| CHEMBL4098433 | — | — | 1 | 8.00 |
| CHEMBL4069711 | — | — | 1 | 7.96 |
| CHEMBL4069567 | — | — | 1 | 7.92 |
| CHEMBL4076693 | — | — | 1 | 7.64 |
| CHEMBL3581693 | BRILANESTRANT | 2.0 | 1 | 7.62 |
| CHEMBL4091432 | — | — | 1 | 7.60 |
| CHEMBL4059818 | — | — | 1 | 7.44 |
| CHEMBL4063737 | — | — | 1 | 7.44 |
| CHEMBL4064926 | — | — | 1 | 7.40 |
| CHEMBL4068267 | — | — | 1 | 7.28 |
| CHEMBL4080411 | — | — | 1 | 7.28 |
| CHEMBL4091898 | — | — | 1 | 7.28 |
| CHEMBL4098078 | — | — | 1 | 7.26 |
| CHEMBL4101673 | — | — | 1 | 7.11 |
| CHEMBL4091541 | — | — | 1 | 7.05 |
| CHEMBL4064736 | — | — | 1 | 6.91 |
| CHEMBL4064146 | — | — | 1 | 6.91 |
| CHEMBL4087507 | — | — | 1 | 6.90 |
| CHEMBL4086984 | — | — | 1 | 6.75 |
| CHEMBL4094916 | — | — | 1 | 6.67 |
| CHEMBL4080048 | — | — | 1 | 6.66 |
| CHEMBL4078392 | — | — | 1 | 6.50 |
| CHEMBL4067493 | — | — | 1 | 6.49 |
| CHEMBL4092625 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059624 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4087929 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4076124 | LSZ-102 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4082510 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4098433 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4069711 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4069567 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4076693 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3581693 | BRILANESTRANT | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4091432 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4063737 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4059818 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4064926 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4068267 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4091898 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4080411 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4098078 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4101673 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4091541 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4064736 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4064146 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4087507 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4086984 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4094916 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL4080048 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL4078392 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4067493 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4092625 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL4073373 | — | IC50 | = | 647.0 | nM | 6.19 |
| CHEMBL4091321 | — | IC50 | = | 669.0 | nM | 6.17 |
| CHEMBL4102815 | — | IC50 | = | 748.0 | nM | 6.13 |
| CHEMBL4102660 | — | IC50 | = | 886.0 | nM | 6.05 |
| CHEMBL4064785 | — | IC50 | = | 941.0 | nM | 6.03 |
| CHEMBL4086994 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4103381 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 1605.0 | nM | 5.79 |
| CHEMBL4074192 | — | IC50 | = | 1823.0 | nM | 5.74 |
| CHEMBL4086258 | — | IC50 | = | 2306.0 | nM | 5.64 |
| CHEMBL4069258 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4065563 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4079134 | — | IC50 | = | 7750.0 | nM | 5.11 |
| CHEMBL4076526 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4090303 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4067222 | — | IC50 | > | 10000.0 | nM | - |