Acute coronary syndrome (ACS) is a cardiac acute ischemic syndrome caused by the rupture or erosion of unstable atherosclerotic plaques within the coronary artery, leading to thrombus formation. Antiplatelet therapy is a key strategy in treating ACS, and although some success has been achieved, there are still limitations, such as thrombus recurrence and bleeding side effects, which limit the long-term use of drugs. Future antiplatelet therapies may achieve more effective or safer treatment methods by targeting novel targets involved in platelet function. This article focuses on potential target inhibitors, including GPVI, protease-activated receptor (PAR)-4, GPIb, 5-hydroxytryptamine receptor subtype 2A (5-HT2A), protein disulfide isomerase, P-selectin, and phosphatidylinositol 3-kinase β inhibitors.