TR-FRET based Kinase Target Screening Service
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Illuminating Kinase Drug Discovery: The Power of TR-FRET-Based Target Screening
Kinases, a vast family of enzymes orchestrating virtually all cellular signaling pathways, have emerged as prime therapeutic targets for a multitude of human diseases, including cancer, inflammatory disorders, and metabolic conditions. Their pivotal role in cell proliferation, differentiation, and survival makes them attractive candidates for pharmacological intervention. However, the high degree of structural similarity across the kinome presents a formidable challenge: developing selective inhibitors that minimize off-target effects and associated toxicities. Addressing this requires sophisticated, robust, and high-throughput screening methodologies. At Creative Biolabs, we leverage cutting-edge technologies, and among the most powerful in our arsenal is Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET)-based kinase target screening, a platform that offers unparalleled sensitivity and specificity for modern drug discovery.
TR-FRET-based Kinase Target Screening Service at Creative Biolabs
At Creative Biolabs, we harness the full potential of TR-FRET technology to provide comprehensive kinase target screening solutions tailored to your specific research objectives. Our service portfolio includes:
Extensive Kinase Panel Screening
We offer screening against large, diverse panels of kinases, covering various families (tyrosine kinases, serine/threonine kinases, lipid kinases) using validated TR-FRET activity and binding assays. This allows for early assessment of compound selectivity and potential off-target effects.
Custom TR-FRET Assay Development
For novel kinase targets or specific research needs not covered by off-the-shelf assays, our expert team can develop and optimize bespoke TR-FRET assays. This includes substrate identification, antibody selection/conjugation, and assay validation.
In-depth Compound Profiling
Beyond primary screening, we provide detailed characterization of hit compounds, including IC50/EC50 determination, affinity measurements (Ki/Kd), and kinetic studies to understand inhibitor potency and mechanism of action.
Diverse Inhibitor Modality Characterization
Our TR-FRET platforms are adept at identifying and characterizing various types of kinase inhibitors, including ATP-competitive inhibitors, allosteric modulators, and conformational state-specific binders like Type II inhibitors.
Support for Challenging Targets
Leveraging the sensitivity of TR-FRET binding assays, we can effectively screen compounds against traditionally difficult targets such as low-activity kinases or pseudokinases.
Integrated Drug Discovery Support
Our services extend beyond screening, offering hit-to-lead optimization consultation, mechanism of action elucidation, and integration with other biophysical or cell-based assay platforms.
Our Advantages
Choosing Creative Biolabs as your partner for TR-FRET-based kinase screening offers distinct advantages rooted in our decades of experience and commitment to scientific rigor:
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Unparalleled Expertise
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State-of-the-Art Technology
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Comprehensive Kinase Coverage
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Flexible and Customized Solutions
FAQs
Q1: What types of kinases can Creative Biolabs screen using TR-FRET?
A1: Creative Biolabs can screen a vast array of kinases using TR-FRET technology. This includes various members of the tyrosine kinase and serine/threonine kinase families, lipid kinases, as well as both active and inactive kinase conformations. Our TR-FRET binding assays are particularly well-suited for interrogating pseudokinases or kinases with inherently low catalytic activity.
Q2: How sensitive are the TR-FRET kinase assays offered by Creative Biolabs?
A2: TR-FRET assays are inherently highly sensitive due to the time-resolved detection mechanism that effectively minimizes background fluorescence. This allows for the reliable detection of kinase activity or binding events even with low enzyme concentrations or weak inhibitor affinities, often enabling determination of potencies in the picomolar to nanomolar range.
Q3: Can Creative Biolabs assist with mechanism of action studies or other follow-up investigations after the initial TR-FRET screen?
A3: Absolutely. Beyond primary screening and IC50 determination, Creative Biolabs offers a suite of services to support hit validation and lead optimization. This includes detailed mechanism of action (MOA) studies, selectivity profiling against broader kinase panels, and integration with orthogonal biophysical or cell-based assays to confirm target engagement and functional effects.
Q4: What information or materials does Creative Biolabs require to initiate a TR-FRET kinase screening project?
A4: To get started, we typically require information about your specific kinase target(s) of interest, details of your compound library (if you are providing compounds, including concentration and solvent), and a clear outline of your research objectives and screening goals. Our team will guide you through the necessary information during our initial consultation.
Contact Us
Advance your kinase drug discovery program with the precision and power of TR-FRET technology. The expert team at Creative Biolabs is ready to discuss your specific needs and design a screening strategy that propels your research forward.
To explore how our TR-FRET-based kinase target screening services can benefit your project, please contact us today.
For Research Use Only | Not For Clinical Use
