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Assay Detail

CHEMBL2423835

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

Binding
Antagonist activity at MR (unknown origin) expressed in COS1 cells after 1 day 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
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.
Hasui T, Ohra T, Ohyabu N, Asano K, Matsui H, Mizukami A, Habuka N, Sogabe S, Endo S, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S.
Bioorg Med Chem (2013) 21 : 5983 -5994
PubMed 23958516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.08 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419301 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419301 IC50 = 83.0 nM 7.08