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Assay Detail

CHEMBL4028161

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

Binding
Antagonist activity at human GAL4-DBD fused MR ligand binding domain transfected in human Huh7 cells co-expressing GAL4-RE-Luc assessed as reduction in aldosterone-induced luciferase activity after 16 hrs in serum free condition by luciferase reporter gene assay
1
Total Activities
1
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 Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J.
J Med Chem (2018) 61 : 1086 -1097
PubMed 29300474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.48 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2181928 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2181928 IC50 = 33.0 nM 7.48