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Updated: Mar 16, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Comparison of FDA Approved Kinase Targets to Clinical Trial Ones: Insights from Their System Profiles and Drug-Target
Jingyu Xu1, Panpan Wang2, Hong Yang2
1Innovative Drug Research and Bioinformatics Group, School of Pharmaceutical Sciences and Innovative Drug Research Centre, Chongqing University, Chongqing 401331, China; School of Mathematics and Statistics, Beijing Institute of Technology, Beijing 100081, China.
Abstract:
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.
Insights
This study compared kinase targets in clinical trials versus established drugs. While similar, established targets more consistently fit system profiles, indicating potential for identifying new druggable targets.
Area of Science:
- Biochemistry and Pharmacology
- Drug Discovery and Development
Background:
- Kinases are a key drug target class, primarily for cancer treatment.
- Expanding kinase therapeutic applications requires identifying new targets and understanding druggability.
- No systematic comparison exists between established and clinical trial kinase targets' system profiles.
Purpose of the Study:
- To comparatively analyze system profiles of established and clinical trial kinase targets.
- To identify factors influencing the druggability of kinase targets.
- To reveal trends in kinase target selection for drug development.
Main Methods:
- Comparative analysis of system profiles for established and clinical trial kinases.
- Examination of drug-target interaction networks.
- Identification of popular kinase targets and trends.
Main Results:
- Most clinical trial kinases share system profiles with established kinases.
- Established targets show a slightly higher adherence to system profiles.
- A discernible trend shift in system profiles from clinical trial to established targets was observed.
Conclusions:
- System profiles offer insights into kinase target druggability.
- Understanding these profiles can guide the identification of new therapeutic targets.
- This analysis aids in optimizing drug discovery strategies for kinases.
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