Assay Detail
Binding
CHEMBL4356683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERalpha in human MCF7:WS8 cells assessed as increase in degradation of ERalpha incubated for 24 hrs by In-Cell Western assay
19
Total Activities
19
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
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.65 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4527655 | — | — | 1 | 9.59 |
| CHEMBL4586663 | — | — | 1 | 9.15 |
| CHEMBL4532671 | — | — | 1 | 9.02 |
| CHEMBL4515212 | — | — | 1 | 8.99 |
| CHEMBL4533964 | — | — | 1 | 8.99 |
| CHEMBL4524872 | — | — | 1 | 8.91 |
| CHEMBL4543096 | — | — | 1 | 8.85 |
| CHEMBL4483006 | — | — | 1 | 8.84 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.80 |
| CHEMBL4516021 | — | — | 1 | 8.72 |
| CHEMBL4448178 | — | — | 1 | 8.59 |
| CHEMBL4436707 | — | — | 1 | 8.52 |
| CHEMBL4578883 | — | — | 1 | 8.44 |
| CHEMBL4564385 | — | — | 1 | 8.29 |
| CHEMBL4440649 | — | — | 1 | 8.23 |
| CHEMBL4436415 | — | — | 1 | 8.23 |
| CHEMBL4464171 | — | — | 1 | 8.09 |
| CHEMBL4538085 | — | — | 1 | 8.03 |
| CHEMBL4447374 | — | — | 1 | 7.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4527655 | — | IC50 | = | 0.257 | nM | 9.59 |
| CHEMBL4586663 | — | IC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL4532671 | — | IC50 | = | 0.955 | nM | 9.02 |
| CHEMBL4515212 | — | IC50 | = | 1.023 | nM | 8.99 |
| CHEMBL4533964 | — | IC50 | = | 1.023 | nM | 8.99 |
| CHEMBL4524872 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL4543096 | — | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL4483006 | — | IC50 | = | 1.445 | nM | 8.84 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4516021 | — | IC50 | = | 1.905 | nM | 8.72 |
| CHEMBL4448178 | — | IC50 | = | 2.57 | nM | 8.59 |
| CHEMBL4436707 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL4578883 | — | IC50 | = | 3.631 | nM | 8.44 |
| CHEMBL4564385 | — | IC50 | = | 5.129 | nM | 8.29 |
| CHEMBL4440649 | — | IC50 | = | 5.888 | nM | 8.23 |
| CHEMBL4436415 | — | IC50 | = | 5.888 | nM | 8.23 |
| CHEMBL4464171 | — | IC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4538085 | — | IC50 | = | 9.333 | nM | 8.03 |
| CHEMBL4447374 | — | IC50 | = | 10.47 | nM | 7.98 |