Assay Detail
Functional
CHEMBL1259734
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biochemical characterization of a series of 17α-perfluoroalkylated estradiols as selective ligands for estrogen receptor α.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.25 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273453 | ALDOSTERONE | 2.0 | 1 | 8.03 |
| CHEMBL1258901 | — | — | 1 | 5.42 |
| CHEMBL1257167 | — | — | 1 | 5.29 |
| CHEMBL1257168 | — | — | 1 | - |
| CHEMBL1257284 | — | — | 1 | - |
| CHEMBL1256104 | — | — | 1 | - |
| CHEMBL1256105 | — | — | 1 | - |
| CHEMBL1256103 | — | — | 1 | - |
| CHEMBL1258902 | — | — | 1 | - |
| CHEMBL1256102 | — | — | 1 | - |
| CHEMBL1258783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273453 | ALDOSTERONE | IC50 | = | 9.268 | nM | 8.03 |
| CHEMBL1258901 | — | IC50 | = | 3810.66 | nM | 5.42 |
| CHEMBL1257167 | — | IC50 | = | 5140.44 | nM | 5.29 |
| CHEMBL1257168 | — | IC50 | < | 14421.15 | nM | - |
| CHEMBL1257284 | — | IC50 | < | 15848.93 | nM | - |
| CHEMBL1256104 | — | IC50 | < | 15848.93 | nM | - |
| CHEMBL1256105 | — | IC50 | < | 15848.93 | nM | - |
| CHEMBL1256103 | — | IC50 | < | 4819.48 | nM | - |
| CHEMBL1258902 | — | IC50 | < | 12560.3 | nM | - |
| CHEMBL1256102 | — | IC50 | < | 5357.97 | nM | - |
| CHEMBL1258783 | — | IC50 | < | 6652.73 | nM | - |