Chronic liver diseases are global health problems representing a significant source of morbidity and mortality worldwide. Cholestasis is one of the most common clinical manifestations of almost all types of liver diseases regardless of etiologies and promotes the pathogenesis of liver. Artemisiae Scopariae Herba (ASH, or Yin Chen) is the most commonly used Traditional Chinese Medicine (TCM) herbal for the treatment of chronic liver diseases, especially cholestatic liver diseases. Various bioactive ingredients have been isolated and identified in ASH, however, most of them were not well characterized for their pharmacological effects. In the current review, we summarize clinical evidence demonstrating the promising therapeutic effects of ASH. We then introduce the profile of bioactive ingredients found in ASH and highlight the change of their abundance during different harvest times of ASH. We further thoroughly review recent advances in the studies of major bioactive ingredients in ASH, including scoparone, capillarisin, chlorogenic acid, and representative flavonoids, for their pharmacological effects, including choleretic, antioxidant, anti-inflammation, anti-fibrosis and other hepatoprotective activities. Underlying molecular targets and signaling networks are also outlined. In conclusion, ASH-based TCM prescriptions are promising strategies for the treatment of cholestatic liver diseases and are more effective than conventional therapies. The future advancement of pharmacology and toxicology researches of ASH and its bioactive ingredients will further contribute to the discovery of novel anti-cholestasis and hepatoprotective drugs.