Traditional Chinese medicine (TCM), the ancient medicine popular in China and surrounding areas, has been recognized as a typical representative of complementary and alternative medicine. Over long period in clinical practice, especially the progress in basic research, data on the effectiveness and beneficial contribution of TCM herbs to public health and disease control have been accumulated while the quality of the evidence is generally poor. The most common clinical practice of TCM herbs is herb combination called formula which consists of several types of medicinal herbs or minerals, which is quite different from modern medicine. Definitely, tens of hundreds of compounds could be identified in even a small formula. With the regained enthusiasm on natural products based new drug R&D, the proposed multi-target drug discovery strategy, the booming of -omics technologies, and the implementation of ambitious plan of TCM modernization in China, attempts have been made to fill the gap between TCM herbs and modern drugs. However, are we heading to the right direction?