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Assay Detail

CHEMBL4423287

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 induction of nuclear translocation of mineralocorticoid receptor in absence 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
EC50 7 8.42 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4532472 1 10.30
CHEMBL4540313 1 9.00
CHEMBL3916929 BALCINRENONE 3.0 1 7.90
CHEMBL4455600 1 7.90
CHEMBL1095097 EPLERENONE 4.0 1 7.00
CHEMBL4557032 1 -
CHEMBL4462110 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4532472 EC50 = 0.05012 nM 10.30
CHEMBL4540313 EC50 = 1.0 nM 9.00
CHEMBL3916929 BALCINRENONE EC50 = 12.59 nM 7.90
CHEMBL4455600 EC50 = 12.59 nM 7.90
CHEMBL1095097 EPLERENONE EC50 = 100.0 nM 7.00
CHEMBL4557032 EC50 > 10000.0 nM -
CHEMBL4462110 EC50 > 10000.0 nM -