Small Molecule Screening against Kinases

Small Molecule Screening against Kinases

Small Molecule Screening against Kinases


Creative BioMart offers a comprehensive selection of tools and technologies to support small molecule screening against kinases. Our talented scientific team is able to provide our customers with unparalleled expertise and experience in kinase biology and pharmaceutical research.


Kinases catalyze the transfer of the γ-phosphate of ATP onto various hydroxyl substrates such as proteins, nucleotides, lipids, and sugars. Kinases are key players in most cellular signal transductions and involved in the regulation of multiple cellular activities. Since overexpression, mutations, translocations, and dysregulation of kinases are involved in the pathogenesis of many diseases such as cancer, cardiovascular diseases, autoimmune diseases, neurological disorders and inflammation, these enzymes have become one of the most prominent therapeutic targets. It is estimated that one-quarter of the drug discovery in the world target kinases. However, these kinases represent only a small portion of the enzyme family, and the majority of the human kinome remains unexplored. Considerable progress has been made in the development of small molecule drugs targeting kinases since imatinib was approved more than 20 years ago, yet the discipline is still in its early stages.

To identify novel targets and elucidate their underlying biological mechanisms, screening for selective small molecules that act against kinases is desired. Small molecule screening aims to identify compounds that can modulate specific biological processes for further development of research tools and/or small molecule drugs. The basic premise of small molecule screening is that the techniques employed must be reliable, reproducible, relevant, and robust to ensure biological relevance. For now, advancements in screening technology present new opportunities for rapidly assaying thousands to hundreds of thousands of compounds in parallel and in an automated fashion. The development of small molecule kinase drugs is developing rapidly and has emerged as one of the most important research areas.

Targeted small-molecule screen identifies SIK inhibition as a common activity of  multikinase inhibitors that up-regulate IL-10 production by activated DCs.

Figure 1. Targeted small-molecule screen identifies SIK inhibition as a common activity of multikinase inhibitors that up-regulate IL-10 production by activated DCs. (Sundberg T B, et al., 2014)

Service Offering

Creative BioMart has set up a state-of-the-art high-throughput screening platform to help our customers identify potential new small molecules targeting kinases and thus accelerate the overall drug development process. Our experienced scientists will work closely with our customers to assist them in the selection and acquisition of high-quality small molecule libraries for subsequent screening. Our service offering includes, but is not limited to the following:

Small Molecule Inhibitor Screening

Kinase inhibitors can be used to treat diseases caused by hyperactive kinases or to modulate cellular functions to overcome other disease drivers. Novel inhibitors will probably need to exhibit actions across many kinases. We have developed and validated a variety of screening methods for follow-up study and HTS screening of kinase inhibitors.

Small Molecule Activator Screening

A kinase activator as the opposite of inhibitors can enhance phosphorylation. The use of activators to transient upregulate kinase function has been increasingly demonstrated to lead to favorable disease outcomes. Small molecule activators could also be highly useful for probing the function of hyperactive kinases. We provide a high-sensitivity and high-throughput capacity for screening of kinase activators.

Small Molecule Agonist and Antagonist Screening

Antagonist can block the activation of kinases while agonist can activate kinase activity. The identification of small molecule agonists and antagonists of kinase function is at the core of the pharmaceutical industry. We have developed a universal high-throughput screening method for direct identification of agonists and antagonists to any kinase targets of interest.

Small Molecule Modulator Screening

A growing number of small molecule modulators have been reported to target different kinases. Their mechanism of action is important for the design of drugs with enhanced efficacy, specificity, and stability. We have developed highly reproducible and robust screening methods to identify small molecules that modulate kinase functions for application in potential drug development efforts.

Creative BioMart is an advanced biotech company within the field of kinase/phosphatase biology. We offer our expertise in establishing assays for kinase screening & profiling. The extensive experience of our scientific team translates into the robust wealth of knowledge that we use to provide you with the highest quality of service. We also supply a range of high-quality small molecule inhibitors, activators, agonist, and antagonists for your research. If there are any additional requirements needed, please do not hesitate to contact us.


  • Sundberg T B, et al. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proceedings of the National Academy of Sciences, 2014, 111(34): 12468-12473.
  • Roskoski R. Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update. Pharmacological Research, 2021: 105463.
For research use only. Not intended for any clinical use.