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Assay Detail

CHEMBL1259727

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Functional
Agonist activity at mineralocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase 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

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biochemical characterization of a series of 17α-perfluoroalkylated estradiols as selective ligands for estrogen receptor α.
Eignerová B, Sedlák D, Dracínský M, Bartunek P, Kotora M.
J Med Chem (2010) 53 : 6947 -6953
PubMed 20812681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 9.47 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273453 ALDOSTERONE 2.0 1 9.47
CHEMBL1258901 1 -
CHEMBL1258783 1 -
CHEMBL1256102 1 -
CHEMBL1257167 1 -
CHEMBL1258902 1 -
CHEMBL1256103 1 -
CHEMBL1257168 1 -
CHEMBL1256104 1 -
CHEMBL1257284 1 -
CHEMBL1256105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273453 ALDOSTERONE EC50 = 0.3381 nM 9.47
CHEMBL1258901 EC50 < 15848.93 nM -
CHEMBL1258783 EC50 < 15848.93 nM -
CHEMBL1256102 EC50 < 15848.93 nM -
CHEMBL1257167 EC50 < 15848.93 nM -
CHEMBL1258902 EC50 < 15848.93 nM -
CHEMBL1256103 EC50 < 15848.93 nM -
CHEMBL1257168 EC50 < 15848.93 nM -
CHEMBL1256104 EC50 < 15848.93 nM -
CHEMBL1257284 EC50 < 15848.93 nM -
CHEMBL1256105 EC50 < 15848.93 nM -