Assay Detail
Binding
CHEMBL4393301
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Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 8.08 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 9.70 |
| CHEMBL4473971 | — | — | 1 | 8.89 |
| CHEMBL4449497 | — | — | 1 | 7.70 |
| CHEMBL138061 | — | — | 1 | 6.04 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | - |
| CHEMBL418971 | BISPHENOL A | — | 1 | - |
| CHEMBL2403354 | — | — | 1 | - |
| CHEMBL2392777 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411 | DIETHYLSTILBESTROL | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4473971 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4449497 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL138061 | — | EC50 | = | 909.0 | nM | 6.04 |
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.13 | nM | - |
| CHEMBL418971 | BISPHENOL A | EC50 | > | 10000.0 | nM | - |
| CHEMBL2403354 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2392777 | — | EC50 | > | 10000.0 | nM | - |