Bioinformatics refers to the continuous emerging field that incorporates and analyzes data using miscellaneous scientific disciplines. The continuous achievements in the field of bioinformatics along with the parallel advancements in the receptor biology or cell biology resulted with the evolution of expansion and technology advancements, sequence analysis, high-throughput technologies, big data and cloud computing, machine learning and artificial intelligence, and many more. Bioinformatics can broadly be divided into various disciplines including genomics, proteomics, transcriptomics, system biology, structural bioinformatics, metabolomics, and agricultural and environmental bioinformatics. In current scenario, bioinformatics finds a wide range of applications in the rapidly evolving fields of receptor biology, drug discovery, and personalized medicines. This chapter, in brief, covers the history and development, various disciplines, and primary goals of bioinformatics and receptor biology. The applications of bioinformatics in relation to receptor biology and drug discovery are also discussed in this chapter.