Zhen Gong; Guoping Hu; Qiang Li; Zhiguo Liu; Fei Wang; Xuejin Zhang; Jian Xiong; Peng Li; Yan Xu; Rujian Ma; Shuhui Chen; Jian Li
Curr. Drug Discov. Technol., 2017, 14, 216-228
https://doi.org/10.2174/1570163814666170425155154

Abstract

Hit identification is the starting point of small-molecule drug discovery and is therefore very important to the pharmaceutical industry. One of the most important approaches to identify a new hit is to screen a compound library using an in vitro assay. High-throughput screening has made great contributions to drug discovery since the 1990s but requires expensive equipment and facilities, and its success depends on the size of the compound library. Recent progress in the development of compound libraries has provided more efficient ways to identify new hits for novel drug targets, thereby helping to promote the development of the pharmaceutical industry, especially for first-in-class drugs. In this review, the sources and classification of compound libraries are summarized. The progress made in combinatorial libraries and DNA-encoded libraries is reviewed. Library design methods, especially for focused libraries, are introduced in detail. In the final part, the status of the compound libraries at WuXi is reported