Comparison of FDA Approved Kinase Targets to Clinical Trial Ones: Insights from Their System Profiles and Drug-Target Interaction Networks

Biomed Res Int. 2016;2016:2509385. doi: 10.1155/2016/2509385. Epub 2016 Jul 28.


Kinase is one of the most productive classes of established targets, but the majority of approved drugs against kinase were developed only for cancer. Intensive efforts were therefore exerted for releasing its therapeutic potential by discovering new therapeutic area. Kinases in clinical trial could provide great opportunities for treating various diseases. However, no systematic comparison between system profiles of established targets and those of clinical trial ones was conducted. The reveal of probable difference or shift of trend would help to identify key factors defining druggability of established targets. In this study, a comparative analysis of system profiles of both types of targets was conducted. Consequently, the systems profiles of the majority of clinical trial kinases were identified to be very similar to those of established ones, but percentages of established targets obeying the system profiles appeared to be slightly but consistently higher than those of clinical trial targets. Moreover, a shift of trend in the system profiles from the clinical trial to the established targets was identified, and popular kinase targets were discovered. In sum, this comparative study may help to facilitate the identification of the druggability of established drug targets by their system profiles and drug-target interaction networks.

MeSH terms

  • Antineoplastic Agents* / pharmacokinetics
  • Antineoplastic Agents* / therapeutic use
  • Drug Approval / methods
  • Drug Delivery Systems / methods*
  • Drug Interactions
  • Humans
  • Neoplasm Proteins / antagonists & inhibitors*
  • Neoplasms* / drug therapy
  • Neoplasms* / enzymology
  • Protein Kinase Inhibitors* / pharmacokinetics
  • Protein Kinase Inhibitors* / therapeutic use
  • Protein Kinases*
  • United States
  • United States Food and Drug Administration


  • Antineoplastic Agents
  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • Protein Kinases