Wenxin Formula (WXF) is a well-known prescription with a significant curative effect in the treatment of cardiac disease. However, the lack of quality control standards caused by unclear quality control components limits the development of new drugs.The aims of this research were to discover the effective materials and screen the quality markers of WXF through a chinmedomics strategy to aid in efficacy evaluation.The therapeutic effect of WXF against myocardial ischaemia (MI) was evaluated by serum metabolic profiling combined with routine electrocardiography; analyses of the serum biochemical indices CK, CK-MB and α-HBDH; and histopathological tests involving TTC staining and HE staining. The raw data of serum samples were obtained by UPLC-HDMS, and multivariate statistical analysis was performed with Progenesis QI software. PCMS software was used to sift the quality markers of WXF.A total of 25 metabolites were characterized as biomarkers for myocardial ischaemia, and Wenxin Formula reversed the levels of 23 of them that were involved in arachidonic acid metabolism, glycerophospholipid metabolism, lysine degradation, and tyrosine metabolism. Eight constituents absorbed into blood were considered to form the effective material basis of Wenxin Formula for treating myocardial ischaemia, and the Q-markers selected through PCMS were ginsenoside Rb1, cinnamic acid, paeoniflorin and berberine.WXF significantly ameliorated the clinical symptoms, pathological changes and metabolic abnormalities of myocardial ischaemia. This study shows that chinmedomics is a powerful strategy to filter Q-markers from effective constituents to rationally evaluate the efficacy and safety of TCMs.