Assay Detail
Binding
CHEMBL4627508
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Agonist activity at ERalpha (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bisphenol AF: Halogen bonding effect is a major driving force for the dual ERα-agonist and ERβ-antagonist activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 7.63 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.68 |
| CHEMBL4642117 | — | — | 1 | 7.84 |
| CHEMBL1900054 | — | — | 1 | 7.70 |
| CHEMBL196585 | — | — | 1 | 7.51 |
| CHEMBL4646249 | — | — | 1 | 6.96 |
| CHEMBL418971 | BISPHENOL A | — | 1 | 6.10 |
| CHEMBL2392656 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4642117 | — | EC50 | = | 14.5 | nM | 7.84 |
| CHEMBL1900054 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL196585 | — | EC50 | = | 30.7 | nM | 7.51 |
| CHEMBL4646249 | — | EC50 | = | 109.0 | nM | 6.96 |
| CHEMBL418971 | BISPHENOL A | EC50 | = | 797.0 | nM | 6.10 |
| CHEMBL2392656 | — | EC50 | > | 10000.0 | nM | - |