Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice.
References:
[1]. Henry M C et al. Synthesis and evaluation of small molecule inhibitors of the androgen receptor N-terminal domain[J]. ACS Medicinal Chemistry Letters, 2023.