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Assay Detail

CHEMBL5136125

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

Binding
Displacement of [3H]-methyltrienolene from human androgen receptor incubated overnight by liquid scintillation counting analysis
3
Total Activities
3
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

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist.
Iijima T, Katoh M, Takedomi K, Yamamoto Y, Akatsuka H, Shirata N, Nishi A, Takakuwa M, Watanabe Y, Munakata H, Koyama N, Ikeda T, Iguchi T, Kato H, Kikkawa K, Kawaguchi T.
J Med Chem (2022) 65 : 8127 -8143
PubMed 35652647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.05 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1393 SPIRONOLACTONE 4.0 1 7.32
CHEMBL1095097 EPLERENONE 4.0 1 4.77
CHEMBL2181929 MT-3995 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1393 SPIRONOLACTONE IC50 = 48.0 nM 7.32
CHEMBL1095097 EPLERENONE IC50 = 17000.0 nM 4.77
CHEMBL2181929 MT-3995 IC50 > 100000.0 nM -