Lomibuvir (VX-222, VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L.
LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
Telaprevir(特拉匹韦) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
Saxagliptin(沙克列汀) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Semagacestat(司马西特) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell.
Amprenavir(安普那韦) is a potent PXR-selective agonist, and an HIV protease inhibitor, used to treat HIV.
Monobenzone(4-苄氧基苯酚) is a compound used as a topical agent for medical depigmentation. It can specifically block tyrosinase.
Deferasirox(地拉罗司) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.