Classical Targets in Drug Discovery

The success of mechanism-based drug discovery depends on the definition of the drug target. This definition becomes even more important as we try to link drug response to genetic variation, understand stratified clinical efficacy and safety, rationalize the differences between drugs in the same therapeutic class, and predict drug utility in patient subgroups. As the drug discovery process has evolved, a great deal of effort has been focused on developing an understanding of the macromolecular targets. However, the pharmaceutical industry has just barely scratched the surface of drug targets and less than 10% of drug targets have been utilized. Therefore, it is very important to summarize the progress and technologies of classical drug target discovery to guide the development of new drug targets. Since built in 2006, Creative Biolabs has explored the field of novel drug development research activities and has gradually grown into a world-leading service provider in novel therapeutic molecules development including advanced drug targets discovery.

Introduction of Classical Targets in Drug Discovery

James Black famously stated in 2000 that “the best way to discover a new drug is to start with an old one.” However, various advanced drug classes and target innovation have appeared in the past two decades of the 21st century, while structural information and a true understanding of the mechanistic aspects of drug-protein interactions have been explained clearly due to the development of novel technologies. Tools such as X-ray crystallography, molecular modeling, PCR, and recombinant DNA technologies provided a sharper and sharper picture of the biological targets impacted by drugs. Nowadays, there are over 21,000 marketed drugs that contain fewer than 1400 unique molecules and create a positive impact through interaction with just 324 drug targets, while approximately 8500 potential “druggable” targets have been recognized in the Human Genome Project.

Overlap of cancer drug targets (left) and major protein families as drug targets (right). Fig.1 Overlap of cancer drug targets (left) and major protein families as drug targets (right). (Santos, 2017)

Classes of Classical Targets in Drug Discovery

Innovation patterns in major protein classes.Fig.2 Innovation patterns in major
protein classes. (Santos, 2017)

The above-mentioned Human Genome Project demonstrated that about 25,000 genes can code proteins, which suggested that the sheer number of possible macromolecular targets for drug discovery is quite large. However, an analysis of the full spectrum of marketed drugs demonstrates quite clearly that the vast majority of drugs target only four classes of macromolecules: enzymes, G-protein-coupled receptor (GPCR), ion channels, and transporters. While there are some emerging drug targets have been discovered recently, an understanding of the four major classes of drug targets is essential for success in the field of drug discovery.

Although they are all proteins, every class of drug target has different structures and functions as well as specific indications. Creative Biolabs has concentrated on the field of novel drug target development for many years and we are glad to share our experience with clients all over the world. If you are interested in drug target development or need more details, please click follow key words or contact us directly.


  1. Santos, R.; et al. A comprehensive map of molecular drug targets. Nature reviews Drug discovery. 2017, 16(1), 19-34.
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