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Assay Detail

CHEMBL930491

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

Functional
Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay
46
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Zhao S, Shen Y, van Oeveren A, Marschke KB, Zhi L.
Bioorg Med Chem Lett (2008) 18 : 3431 -3435
PubMed 18442912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Efficacy 23 - -
IC50 23 7.33 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427731 2 7.72
CHEMBL253746 2 7.72
CHEMBL256768 2 7.70
CHEMBL258241 2 7.57
CHEMBL258397 2 7.32
CHEMBL253744 2 7.21
CHEMBL402136 2 7.11
CHEMBL258384 2 6.84
CHEMBL409 BICALUTAMIDE 4.0 2 6.79
CHEMBL27769 STANOLONE 2.0 2 -
CHEMBL450933 2 -
CHEMBL257751 2 -
CHEMBL403219 2 -
CHEMBL253535 2 -
CHEMBL401629 2 -
CHEMBL258190 2 -
CHEMBL257151 2 -
CHEMBL256947 2 -
CHEMBL256977 2 -
CHEMBL256769 2 -
CHEMBL427898 2 -
CHEMBL450334 2 -
CHEMBL401711 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427731 IC50 = 19.0 nM 7.72
CHEMBL253746 IC50 = 19.0 nM 7.72
CHEMBL256768 IC50 = 20.0 nM 7.70
CHEMBL258241 IC50 = 27.0 nM 7.57
CHEMBL258397 IC50 = 48.0 nM 7.32
CHEMBL253744 IC50 = 62.0 nM 7.21
CHEMBL402136 IC50 = 78.0 nM 7.11
CHEMBL258384 IC50 = 144.0 nM 6.84
CHEMBL409 BICALUTAMIDE IC50 = 162.0 nM 6.79
CHEMBL258384 Efficacy = 63.0 % -
CHEMBL403219 IC50 > 10000.0 nM -
CHEMBL450334 IC50 > 10000.0 nM -
CHEMBL27769 STANOLONE IC50 > 10000.0 nM -
CHEMBL27769 STANOLONE Efficacy < 20.0 % -
CHEMBL450933 IC50 > 10000.0 nM -
CHEMBL450933 Efficacy < 20.0 % -
CHEMBL258241 Efficacy = 57.0 % -
CHEMBL409 BICALUTAMIDE Efficacy = 85.0 % -
CHEMBL402136 Efficacy = 68.0 % -
CHEMBL403219 Efficacy < 20.0 % -
CHEMBL253744 Efficacy = 63.0 % -
CHEMBL253746 Efficacy = 49.0 % -
CHEMBL427731 Efficacy = 47.0 % -
CHEMBL256768 Efficacy = 29.0 % -
CHEMBL450334 Efficacy < 20.0 % -
CHEMBL257751 IC50 > 10000.0 nM -
CHEMBL257751 Efficacy < 20.0 % -
CHEMBL256947 IC50 > 10000.0 nM -
CHEMBL258190 Efficacy < 20.0 % -
CHEMBL253535 IC50 > 10000.0 nM -
CHEMBL258190 IC50 > 10000.0 nM -
CHEMBL401629 Efficacy < 20.0 % -
CHEMBL257151 IC50 > 10000.0 nM -
CHEMBL401629 IC50 > 10000.0 nM -
CHEMBL253535 Efficacy < 20.0 % -
CHEMBL258397 Efficacy = 62.0 % -
CHEMBL257151 Efficacy < 20.0 % -
CHEMBL401711 Efficacy < 20.0 % -
CHEMBL256947 Efficacy < 20.0 % -
CHEMBL256977 IC50 > 10000.0 nM -
CHEMBL256977 Efficacy < 20.0 % -
CHEMBL256769 IC50 > 10000.0 nM -
CHEMBL256769 Efficacy < 20.0 % -
CHEMBL427898 IC50 > 10000.0 nM -
CHEMBL427898 Efficacy < 20.0 % -
CHEMBL401711 IC50 > 10000.0 nM -