Related Experiment Video
Updated: May 21, 2026
Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Transformation of in vitro tools for kinase profiling: keeping an eye over the off-target liabilities
Kun Bi1, Connie S Lebakken, Kurt W Vogel
1Life Technologies Corp, Cell Systems Division, 501 Charmany Dr, Madison, WI 53719 , USA +1 608 204 5216 ; kurt.vogel@lifetech.com.
Introduction:
Over the past decade, there has been an increased number of FDA approved small molecule kinase inhibitors for the treatment of cancer. This is due, in part, to an increased understanding of the fundamental aspects of kinase biology, coupled with advances in the methods used to study the inhibitory effects of small molecules on kinase activity. Underlying the development of these inhibitors are profiling methods that are used to assess the effect of potential compounds against their desired and undesired targets. The advancement of kinase profiling has stemmed from the development of basic assay technology that allows compounds to be tested against ever larger panels of kinases in a robust, cost-effective manner. Methods have also been developed that rapidly assess compound activity against specific activation states of kinases. There has also been a development of newer methods that move beyond traditional biochemical formats, which take a 'whole cell' approach to compound profiling.
Areas Covered:
This review provides an overview of traditional biochemical-based kinase profiling as well as an introduction to advances that have been made by moving compound profiling into a cell-based format.
Expert Opinion:
While central to the appropriate prioritization and optimization of compounds during the hit to lead phase of early-stage pharmaceutical development, every compound profiling format must be critically assessed so that one can make informed decisions through an understanding of their strengths and limitations. These decisions will ultimately be balanced against cost, complexity and its biological relevance.
Insights
This review discusses kinase inhibitor profiling methods, covering traditional biochemical assays and newer cell-based approaches. Understanding the strengths and limitations of each method is crucial for effective drug development.
Area of Science:
- Pharmacology and Drug Discovery
- Biochemistry and Molecular Biology
Background:
- Small molecule kinase inhibitors are increasingly FDA-approved for cancer treatment.
- Advances in kinase biology and assay technology drive inhibitor development.
- Kinase profiling methods assess compound effects on target and off-target kinases.
Purpose of the Study:
- To review traditional biochemical kinase profiling.
- To introduce cell-based compound profiling methods.
- To compare different profiling formats for drug development.
Main Methods:
- Overview of established biochemical kinase assays.
- Introduction to cell-based assay methodologies.
- Discussion of methods for assessing compound activity against specific kinase activation states.
Main Results:
- Biochemical assays enable robust, cost-effective testing against large kinase panels.
- Cell-based assays offer a 'whole cell' approach to compound profiling.
- Advancements allow rapid assessment of compound activity against specific kinase states.
Conclusions:
- Kinase profiling is central to prioritizing and optimizing drug compounds.
- Each profiling format has unique strengths and limitations.
- Decisions on profiling methods should balance cost, complexity, and biological relevance.
