Aliskiren is a subnanomolar inhibitor of human renin (IC50 0,6 nM) with some interspecies variance. It is highly selective with an at least 5000x lower IC50 against cathepsin, pepsin, HIV-1 peptidase and various transmitter receptors.

1. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758

2.  Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705.