Assay Detail
Binding
CHEMBL4356686
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Antagonist activity at ERalpha in human MCF7:WS8 cells incubated for 18 hrs by dual luciferase reporter gene assay relative to control
15
Total Activities
15
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 | 15 | 8.29 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4586663 | — | — | 1 | 9.30 |
| CHEMBL4532671 | — | — | 1 | 8.82 |
| CHEMBL4527655 | — | — | 1 | 8.72 |
| CHEMBL4448178 | — | — | 1 | 8.68 |
| CHEMBL4578883 | — | — | 1 | 8.57 |
| CHEMBL4533964 | — | — | 1 | 8.51 |
| CHEMBL4543096 | — | — | 1 | 8.46 |
| CHEMBL4515212 | — | — | 1 | 8.37 |
| CHEMBL4538085 | — | — | 1 | 8.28 |
| CHEMBL4483006 | — | — | 1 | 8.13 |
| CHEMBL4436415 | — | — | 1 | 7.96 |
| CHEMBL4440649 | — | — | 1 | 7.92 |
| CHEMBL4564385 | — | — | 1 | 7.85 |
| CHEMBL4524872 | — | — | 1 | 7.55 |
| CHEMBL4464171 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4586663 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4532671 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4527655 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4448178 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4578883 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4533964 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4543096 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4515212 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4538085 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4483006 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4436415 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4440649 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4564385 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4524872 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4464171 | — | IC50 | = | 64.0 | nM | 7.19 |