Assay Detail
Binding
CHEMBL5337700
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of STS in human JEG-3 cell lysates assessed as inhibition of estrone E1 formation using [3H]estrone sulfate as substrate incubated for 1 hr in presence of E1S by scintillation spectrometry
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | JEG-3 |
| Subcellular | Lysates |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.59 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286738 | IROSUSTAT | 2.0 | 1 | 8.19 |
| CHEMBL5436409 | — | — | 1 | 7.01 |
| CHEMBL5413467 | — | — | 1 | 5.68 |
| CHEMBL5408262 | — | — | 1 | 5.47 |
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | 4.0 | 1 | - |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286738 | IROSUSTAT | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5436409 | — | IC50 | = | 96.6 | nM | 7.01 |
| CHEMBL5413467 | — | IC50 | = | 2081.0 | nM | 5.68 |
| CHEMBL5408262 | — | IC50 | = | 3398.0 | nM | 5.47 |
| CHEMBL1116 | RALOXIFENE HYDROCHLORIDE | IC50 | - | — | - | |
| CHEMBL81 | RALOXIFENE | IC50 | - | — | - |