As productivity of pharmaceutical research and development (R&D) for small-molecule drugs declines, the trend in drug discovery strategies is shifting towards biologics, which predominantly target secreted or cell surface proteins. Receptors and ligands are the most-valuable drug targets. In contrast to conventional approaches of discovering one ligand at a time, the emerging technology of ligandomics can systematically map disease-selective cellular ligands in the absence of molecular probes. Biologics targeting these ligands with disease selectivity have the advantages of high efficacy, minimal adverse effects, wide therapeutic indices, and low safety-related attrition rates. Therefore, ligandomics represents a paradigm shift to address the bottleneck of target discovery for biologics development.

随着小分子药物的药物研发（R＆D）生产率下降，药物发现策略的趋势正在转向生物制剂，主要针对分泌的或细胞表面蛋白。受体和配体是最有价值的药物靶标。与一次发现一个配体的常规方法相比，新兴的配体组学技术可以在没有分子探针的情况下系统地绘制疾病选择性细胞配体的图谱。以疾病选择性靶向这些配体的生物制剂具有高功效，最小的副作用，广泛的治疗指数以及与安全性相关的消耗率低的优点。因此，配体组学代表了范式转变，以解决生物开发中靶标发现的瓶颈。