Abstract: In the present work, we propose drug-target co-screening strategy, a novel technique for Chinese medicine development and evaluation, which leverages whole-genome pan-receptors and genetically encoded natural compound libraries from medicinal plants and animals. This paper outlines the core components of the strategy, focusing on the identification of novel disease and syndrome-related targets based on clinical efficacy of Chinese medicine, multi-component target screening technologies for herbal medicine, technologies for multi-component identification and target screening and artificial intelligence-powered approaches for discovering active ingredients and elucidating their mechanisms. The strategy demonstrates broad applicability in areas such as the discovery of disease (syndrome) targets, the development of new Chinese medicine drugs, the analysis of multi-target, multi-pathway mechanism of action of Chinese medicine, and the study of drug properties including the five flavors. Centered on whole-genome pan-receptors, drug-target co-screening strategy provides a powerful framework to address key challenges in Chinese medicine research—namely, the ambiguity of therapeutic targets and unclear mechanisms of action. This approach offers strong support for mechanistic studies and paves the way for a new paradigm in modernizing and innovating Chinese medicine drug development.