Combinatorial chemistry in conjunction with High Throughput Screening (HTS) is revolutionizing the drug discovery process. Yet, we have much to learn about the integration of these powerful techniques with information from genomics, proteomics, computation and pharmacokinetics before dramatic increases in the drug discovery/development processes can be achieved. The chapters in this book represent the state of the art regarding the integration of combinatorial chemistry and HTS in connection with anti-inflammatory targets. Obviously, there is much work to be done beyond what is described in this text, nevertheless, it should set the stage for creative thinking among scientists of many disciplines for the accomplishment of our ultimate goals in treating inflammatory diseases.