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Table 2 Cell-based profile of AR antagonist compounds

From: Dose-dependent effects of small-molecule antagonists on the genomic landscape of androgen receptor binding

  AR agonism (at 1uM) AR antagonism Nuclear Translocation Cell Proliferation
FoldInduction % Inhibition IC50-nM % Inhibition at 1uM IC50-nM IC50-nM
Compound 30 0.83 -0.7 144 90 174 94
Compound 26 1.03 0.1 59 96 57 45
  1. For agonism, values obtained from the AR antagonist compounds were compared to those of untreated cells, which were assigned an arbitrary number of 1.0 to indicate no agonism. For antagonism, cells were treated with 0.1nM R1881 alone (corresponding to max receptor activation = 100%) or in combination with the antagonist compounds at various doses to determine IC50 values. Nuclear translocation and cell proliferation values were calculated as indicated under materials and methods.