Assay Detail
Binding
CHEMBL4263471
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescein-tagged estrogen binding to GST-tagged ERalpha (unknown origin) ligand binding domain after 1 hr by LanthaScreen TR-FRET assay
11
Total Activities
11
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
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.36 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 9.59 |
| CHEMBL4278672 | — | — | 1 | 7.21 |
| CHEMBL4283229 | — | — | 1 | 7.02 |
| CHEMBL4293810 | — | — | 1 | 7.00 |
| CHEMBL4290786 | — | — | 1 | 6.70 |
| CHEMBL3099433 | — | — | 1 | 6.66 |
| CHEMBL4293632 | — | — | 1 | - |
| CHEMBL4283040 | — | — | 1 | - |
| CHEMBL4290239 | — | — | 1 | - |
| CHEMBL4279577 | — | — | 1 | - |
| CHEMBL4290019 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.26 | nM | 9.59 |
| CHEMBL4278672 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4283229 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4293810 | — | EC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4290786 | — | EC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3099433 | — | EC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4293632 | — | EC50 | - | — | - | |
| CHEMBL4283040 | — | EC50 | - | — | - | |
| CHEMBL4290239 | — | EC50 | - | — | - | |
| CHEMBL4279577 | — | EC50 | - | — | - | |
| CHEMBL4290019 | — | EC50 | - | — | - |