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Assay Detail

CHEMBL1929758

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

Binding
Displacement of [3H]testosterone from AR
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.
Hasui T, Matsunaga N, Ora T, Ohyabu N, Nishigaki N, Imura Y, Igata Y, Matsui H, Motoyaji T, Tanaka T, Habuka N, Sogabe S, Ono M, Siedem CS, Tang TP, Gauthier C, De Meese LA, Boyd SA, Fukumoto S.
J Med Chem (2011) 54 : 8616 -8631
PubMed 22074142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.89 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1928877 1 7.02
CHEMBL1393 SPIRONOLACTONE 4.0 1 6.92
CHEMBL1928878 1 5.92
CHEMBL1928872 1 5.44
CHEMBL1929041 1 5.35
CHEMBL1928875 1 5.33
CHEMBL1928874 1 5.23
CHEMBL1928870 1 -
CHEMBL1928871 1 -
CHEMBL1928873 1 -
CHEMBL1928876 1 -
CHEMBL1928869 1 -
CHEMBL1928880 1 -
CHEMBL1928881 1 -
CHEMBL1928882 1 -
CHEMBL1929036 1 -
CHEMBL1929039 1 -
CHEMBL1929040 1 -
CHEMBL1929042 1 -
CHEMBL1095097 EPLERENONE 4.0 1 -
CHEMBL1928879 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1928877 IC50 = 95.0 nM 7.02
CHEMBL1393 SPIRONOLACTONE IC50 = 120.0 nM 6.92
CHEMBL1928878 IC50 = 1200.0 nM 5.92
CHEMBL1928872 IC50 = 3600.0 nM 5.44
CHEMBL1929041 IC50 = 4500.0 nM 5.35
CHEMBL1928875 IC50 = 4700.0 nM 5.33
CHEMBL1928874 IC50 = 5900.0 nM 5.23
CHEMBL1928870 IC50 - -
CHEMBL1928871 IC50 - -
CHEMBL1928873 IC50 - -
CHEMBL1928876 IC50 > 10000.0 nM -
CHEMBL1928869 IC50 > 10000.0 nM -
CHEMBL1928880 IC50 - -
CHEMBL1928881 IC50 > 10000.0 nM -
CHEMBL1928882 IC50 > 10000.0 nM -
CHEMBL1929036 IC50 > 10000.0 nM -
CHEMBL1929039 IC50 > 10000.0 nM -
CHEMBL1929040 IC50 > 10000.0 nM -
CHEMBL1929042 IC50 > 10000.0 nM -
CHEMBL1095097 EPLERENONE IC50 > 10000.0 nM -
CHEMBL1928879 IC50 - -