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Kinase Screening and Profiling Services

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Creative Enzymes offers comprehensive kinase screening and profiling solutions, ranging from assay development and high-throughput screening to selectivity analysis and compound profiling. With expertise in both biochemical and cell-based assays, we support clients across biotechnology, pharmaceutical, and academic sectors in accelerating kinase-focused research and therapeutic development.

Understanding Kinases

Kinases represent the most critical and largest superfamily of drug targets, with over 518 known members, and remain a major focus in both pharmaceutical research and academic studies. Kinase signaling pathways regulate essential cellular processes such as proliferation, metabolism, differentiation, and apoptosis. Dysregulation of kinase activity has been strongly implicated in numerous pathological conditions, including cancer, diabetes, cardiovascular diseases, and neurodegenerative disorders such as Alzheimer's disease.

Over the past decade, kinases have gained increasing prominence as therapeutic targets. The U.S. FDA has already approved numerous kinase inhibitors, underscoring the clinical importance of this enzyme family in drug discovery and development. Properly functioning kinases are central to normal cell physiology, but their malfunction can lead to aberrant signaling pathways and disease. Therefore, reliable kinase screening and profiling services are indispensable for drug discovery pipelines and translational research.

Kinase families and hit kinases linked to Alzheimer's diseaseFigure 1. Hit kinases separated into kinase families. (Cavallini et al., 2013)

Comprehensive Service Offerings

At Creative Enzymes, we provide a complete portfolio of kinase screening and profiling services, tailored to the unique requirements of each client.

Biochemical assays for kinase screening and profiling

Biochemical-Based Assays

  • Enzyme activity assays to evaluate phosphorylation activity.
  • Binding affinity assays to assess compound–kinase interactions.
  • Inhibition studies including IC50 and Ki determination.
  • High-throughput screening (HTS) for rapid evaluation of compound libraries.
  • Selectivity profiling across hundreds of kinases to identify off-target interactions.

Cell-based assays for kinase screening and profiling

Cell-Based Assays

  • Functional cell assays to study kinase signaling in a physiological context.
  • Cell viability and proliferation assays to evaluate compound effects.
  • Target engagement and mechanistic studies to understand kinase–compound interactions in living cells.
  • Cellular selectivity assays to assess compound activity across multiple cell types.

Specialized services for kinase screening and profiling

Specialized Services

  • Custom assay development tailored to specific kinases or signaling pathways.
  • Mechanism of action studies for candidate compounds.
  • Phosphorylation site detection using advanced analytical methods.
  • Integrated drug discovery support combining screening, profiling, and lead optimization.

Workflow and Process

Service workflow of kinase screening and profiling

Service Details

  • Routine and custom assay development
  • Single enzyme or pathway-level analysis
  • Support for high-throughput screening
  • Optional mechanistic studies (active-site mapping, inhibitor profiling, structural-functional integration)

Contact Our Team

Why Choose Creative Enzymes

Extensive Coverage

Assays available for over 600 kinases, spanning multiple families.

Versatility

Support for both single-point and multi-concentration IC50 assays.

Advanced Technologies

Cutting-edge biochemical and cell-based platforms.

Customization

One-stop and tailored services to meet diverse project needs.

Expert Team

Dedicated scientists with deep expertise in kinase biology and drug discovery.

High Reproducibility

Rigorous validation ensures accuracy and reliability.

Representative Case Studies

Case 1: Heading: Advancing Kinase Inhibitors with Furo[3,2-b]pyridines

The furo[3,2-b]pyridine scaffold, a relatively unexplored pharmacophore in kinase inhibitor design, was leveraged to develop novel compounds through chemoselective couplings of 5-chloro-3-iodofuro[3,2-b]pyridine. This versatile synthetic strategy enabled an efficient second-generation synthesis of MU1210, a leading chemical biology probe for CLK1/2/4, and facilitated the discovery of highly selective HIPK inhibitors MU135 and MU1787. Structural studies, including the X-ray crystal structure of MU135 bound to HIPK2, provided mechanistic insights. These findings highlight furo[3,2-b]pyridines as valuable scaffolds for next-generation kinase inhibitors with strong selectivity and therapeutic potential.

Table 1. CLK, DYRK and HIPK IC50 values (in nM) of compounds 12a-e; the data were determined using a radiometric assay. (Němec et al., 2021)

IC50 values of six compounds against CLK, DYRK, and HIPK kinases

Case 2: VF16 Emerges as a Potent EGFR-TK Inhibitor

EGFR, a key driver of cancer cell growth and survival, is an established target for cancer therapy. In this study, 78 designed vinyl sulfone derivatives were screened against EGFR tyrosine kinase (EGFR-TK) through computational and experimental approaches. Molecular docking identified eight promising candidates, with VF16 showing the strongest inhibitory effect. VF16 demonstrated potent EGFR-TK inhibition (IC50= 7.85 ± 0.88 nM) and notable cytotoxicity against A431, A549, and H1975 cancer cell lines. A 500-ns molecular dynamics simulation confirmed the stability of VF16 binding at the ATP site, highlighting it as a promising novel small-molecule EGFR-TK inhibitor.

Inhibition of EGFR tyrosine kinase by vinyl sulfone derivativesFigure 2. (A) Kinase inhibitory activity screening of VFs towards EGFR-TK at 1 μM. **** p ≤ 0.0001 vs. erlotinib. (B) Kinase inhibitory activity of VFs towards EGFR-TK. (Aiebchun et al., 2021)

FAQs

  • Q: How many kinases are included in your profiling panel?

    A: We provide coverage of over 600 kinases, enabling comprehensive profiling across diverse kinase families.

  • Q: Do you support both biochemical and cell-based assays?

    A: Yes. We provide biochemical activity and binding assays, as well as physiologically relevant cell-based assays.

  • Q: What data formats do you deliver?

    A: We provide raw data, processed results, statistical validation, and expert interpretation. Custom reporting formats can be arranged.

  • Q: Can you perform custom assay development for less-studied kinases?

    A: Absolutely. Our scientific team routinely designs and validates custom assays tailored to novel or rare kinases.

  • Q: What is the typical project timeline?

    A: Timelines depend on assay complexity. Standard kinase activity or IC50 assays can be completed in 2–4 weeks, while larger profiling projects may require additional time.

  • Q: Do you assist in drug discovery beyond screening?

    A: Yes. In addition to screening and profiling, we provide mechanism of action studies, lead optimization support, and integrated solutions for drug discovery projects.

References:

  1. Aiebchun T, Mahalapbutr P, Auepattanapong A, et al. Identification of vinyl sulfone derivatives as EGFR tyrosine kinase inhibitor: in vitro and in silico studies. Molecules. 2021;26(8):2211. doi:10.3390/molecules26082211
  2. Cavallini A, Brewerton S, Bell A, et al. An unbiased approach to identifying tau kinases that phosphorylate tau at sites associated with Alzheimer Disease. Journal of Biological Chemistry. 2013;288(32):23331-23347. doi:10.1074/jbc.M113.463984
  3. Němec V, Maier L, Berger BT, et al. Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. European Journal of Medicinal Chemistry. 2021;215:113299. doi:10.1016/j.ejmech.2021.113299
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