The druggable genome: Evaluation of drug targets in clinical trials suggests major shifts in molecular class and indication

Annu Rev Pharmacol Toxicol. 2014;54:9-26. doi: 10.1146/annurev-pharmtox-011613-135943. Epub 2013 Aug 30.


The largest innovations within pharmaceutical development come through new compounds that have unique and novel modes of action. These innovations commonly involve expanding the protein space targeted by pharmaceutical agents. At present, information about drugs and drug targets is available online via public databases such as DrugBank and the Therapeutic Targets Database. However, this information is biased, understandably so, toward established drugs and drug-target interactions. To gain a better overview of the drug-targeted portion of the human proteome and the directions of current drug development, we developed a data set of clinical trial drug-target interactions based on CenterWatch's Drugs in Clinical Trials Database, one of the largest databases of its kind. Our curation identified 475 potentially novel clinical trial drug targets. This review aims to identify trends in drug development based on the potentially novel targets currently being explored in clinical trials.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alzheimer Disease / drug therapy
  • Anti-Inflammatory Agents / pharmacology
  • Antineoplastic Agents / pharmacology
  • Appetite Regulation / drug effects
  • Clinical Trials as Topic
  • Databases, Factual
  • Evaluation Studies as Topic
  • G-Protein-Coupled Receptor Kinases / genetics
  • G-Protein-Coupled Receptor Kinases / metabolism
  • Genome, Human*
  • Humans
  • Hypoglycemic Agents / pharmacology
  • Molecular Targeted Therapy*
  • Proteome / metabolism


  • Anti-Inflammatory Agents
  • Antineoplastic Agents
  • Hypoglycemic Agents
  • Proteome
  • G-Protein-Coupled Receptor Kinases