Efficiency in the drug discovery process relies on timely knowledge of biological drug-response in the course of disease and treatment, which ultimately rests on knowledge of protein function and regulation. As proteomics deals with the root level of the protein function, there is a very high probability that this will be one of the major tools of modern drug discovery process. Proteomics is being considered as one of the major drug discovery tools by the scientists. Global gene expression profiling by genomic and proteomic analyses has changed the face of drug discovery and biological research. Global pharmaceutical companies are ready to invest ~20% of their R&D investment for getting new biological entities through the use of new scientific methods such as genomics, proteomics and combinatorial chemistry. Attempt for implementation of these technologies increased day by day in the area of design and optimization of drug through biological target identification and validation. Soon, proteomics along with other new technologies will be in use to introduce novel ideas for developing new drugs and improving the quality of existing ones.