S1 Supporting Information Discovery of an Orally Selective Inhibitor of Signal Transducer and Activator of Transcription 3 Using Advanced Multiple Ligand Simultaneous Docking Wenying Yu, Chenglong Li, Wenda Zhang, Yuanzheng Xia, Shanshan Li, Jia-yuh Lin, Keqin Yu, Mu Liu, Lei Yang, Jianguang Luo, Yijun Chen, Hongbin Sun and Lingyi Kong* State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, Laboratory of Chemical Biology, @ Center for Drug Discovery, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. § Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States Department of Biochemistry and Molecular Biology, School of Medicine, University of Maryland, Baltimore, Maryland 21201, United States # Water Supply and Drainage, Nanchang Hangkong University, 696 Fenghe Ave. S., Nanchang 330046, China. *Corresponding Author: Phone: +86-25-8327-1405; Fax: +86-25-8327-1405; E-mail: cpu_lykong@126.com Table of contents: 1. Supplementary Design S2–S6 2. Supplementary Biological Assays S7–S11 3. Supplementary PAIN assay S11 4. Methods and Method Validation of Pharmacokinetic Study S11–S15 5. References S16