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Assay Detail

CHEMBL4423302

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Modulation activity at human mineralocorticoid receptor in human EA.hy926 cells assessed as blocking of nuclear translocation of mineralocorticoid receptor in presence of aldosterone by receptor translocation assay
7
Total Activities
7
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

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection.
Granberg KL, Yuan ZQ, Lindmark B, Edman K, Kajanus J, Hogner A, Malmgren M, O'Mahony G, Nordqvist A, Lindberg J, Tångefjord S, Kossenjans M, Löfberg C, Brånalt J, Liu D, Selmi N, Nikitidis G, Nordberg P, Hayen A, Aagaard A, Hansson E, Hermansson M, Ivarsson I, Jansson-Löfmark R, Karlsson U, Johansson U, William-Olsson L, Hartleib-Geschwindner J, Bamberg K.
J Med Chem (2019) 62 : 1385 -1406
PubMed 30596500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.13 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095097 EPLERENONE 4.0 1 7.20
CHEMBL4557032 1 7.20
CHEMBL4462110 1 7.00
CHEMBL3916929 BALCINRENONE 3.0 1 -
CHEMBL4540313 1 -
CHEMBL4455600 1 -
CHEMBL4532472 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095097 EPLERENONE IC50 = 63.1 nM 7.20
CHEMBL4557032 IC50 = 63.1 nM 7.20
CHEMBL4462110 IC50 = 100.0 nM 7.00
CHEMBL3916929 BALCINRENONE IC50 > 10000.0 nM -
CHEMBL4540313 IC50 > 10000.0 nM -
CHEMBL4455600 IC50 > 10000.0 nM -
CHEMBL4532472 IC50 > 10000.0 nM -