Assay Detail
Functional
CHEMBL1785592
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Agonist activity at human full-length ERbeta receptor expressed in human HEC1 cells co-expressing (ERE)2-pS2-luc gene assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEC-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 9.24 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782957 | — | — | 1 | 9.64 |
| CHEMBL1782956 | — | — | 1 | 9.30 |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.14 |
| CHEMBL1782958 | — | — | 1 | 8.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782957 | — | EC50 | = | 0.23 | nM | 9.64 |
| CHEMBL1782956 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.72 | nM | 9.14 |
| CHEMBL1782958 | — | EC50 | = | 1.3 | nM | 8.89 |