Assay Detail
Binding
CHEMBL5516987
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Binding affinity to human ERalpha assessed as inhibition constant incubated under dark condition for 2 hrs by competitive fluorometric binding assay
17
Total Activities
17
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 Novel ERα and Aromatase Dual-Targeting PROTAC Degraders to Overcome Endocrine-Resistant Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.94 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5396802 | — | — | 1 | 8.35 |
| CHEMBL5562607 | — | — | 1 | 7.70 |
| CHEMBL5565514 | — | — | 1 | 7.68 |
| CHEMBL5559605 | — | — | 1 | 7.62 |
| CHEMBL5568432 | — | — | 1 | 7.23 |
| CHEMBL5561738 | — | — | 1 | 7.23 |
| CHEMBL5549760 | — | — | 1 | 7.19 |
| CHEMBL5555317 | — | — | 1 | 7.11 |
| CHEMBL5558656 | — | — | 1 | 7.00 |
| CHEMBL5564308 | — | — | 1 | 6.68 |
| CHEMBL5556708 | — | — | 1 | 6.66 |
| CHEMBL5567374 | — | — | 1 | 6.60 |
| CHEMBL5561803 | — | — | 1 | 6.34 |
| CHEMBL5561336 | — | — | 1 | 6.31 |
| CHEMBL5542291 | — | — | 1 | 6.30 |
| CHEMBL5563219 | — | — | 1 | 6.06 |
| CHEMBL5568367 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5396802 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5562607 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5565514 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5559605 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL5568432 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5561738 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5549760 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL5555317 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL5558656 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL5564308 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL5556708 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5567374 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL5561803 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL5561336 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL5542291 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5563219 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL5568367 | — | Ki | = | 1100.0 | nM | 5.96 |