We support every step of your kinase drug development
Evaluate Kinase Activity
Uncover the inhibitory effect of your compound on its target kinase with precision
Leverage our high-throughput screening capabilities and diverse detection methods (radiometric, fluorescent, luminescent) to identify promising leads. Interested in testing smaller size libraries, such as a fragment library, a focused library, or an FDA drug collection library instead? Ask us about our SPR screening services.
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HotSpot™ Kinase Screen
Our best-in-class radiometric activity assay is now available at physiological ATP concentrations (1mM) to help you get a true-to-life insight into kinase activity.
Decipher Your Compund’s Mechanism of Action
Investigate binding kinetics of your selected inhibitor(s)
Our service utilizes structure-activity relationship (SAR) analysis with IC50 potency assays to elucidate the mechanism of action (MoA) of your shortlisted kinase inhibitors. This approach systematically evaluates the impact of structural modifications on inhibitor potency (IC50) against:
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- Wild-type target kinase: The unmodified form of the target kinase
- Kinase variants harboring mutations: These variants contain targeted modifications in key kinase domains
By meticulously comparing IC50 values across these variants, you gain invaluable insights into the critical binding interactions between the inhibitor and the kinase. We help identify three key interaction types:
- Covalent inhibitor: Forms a direct chemical bond with the kinase.
- ATP-competitive: Competes with ATP for binding to the ATP-binding pocket.
- Substrate-competitive: Competes with the substrate for binding to the substrate-binding pocket.
This refined approach not only confirms your initial kinase activity profiling findings but also provides a deeper mechanistic understanding, paving the way for targeted optimization strategies.
Kinase Selectivity Profiling
Explore selectivity and off-target effects of your compounds across the human kinome
We offer the industry’s largest collection of the human kinome with more than 700+ kinases. Our flexible approach allows you to preselect a subfamily of kinases or the entire human kinome.
Benefits of Kinase Selectivity Profiling:
- Early Detection of Off-Target Effects: Proactive identification of drug selectivity and potential liabilities minimizes risk and saves resources during development.
- Unveiling New Kinase Opportunities: This analysis can reveal unexpected sensitivities towards other kinases within your target pathway, potentially leading to the discovery of novel therapeutic targets.
Target Engagement and Functionality inside Living Cells
Evaluate the selectivity of your kinase inhibitor with advanced functional assays
Traditional in vitro assays only tell part of the story. Our target engagement and phosphorylation assay portfolio provides fundamental insights into how your drug interacts with its target and affects signalling pathways inside a living cell
NanoBRET Assay
Measure the apparent affinity of your test compound(s) for its target within intact living cells
Cellular Phosphorylation Assay
Evaluate the impact of your test compound on on downstream phosphorylation targets
Preclinical Testing
Test the in vitro and in vivo efficacy and safety of your compound
Our diverse cell lines (2D & 3D) and advanced in vivo models offer an in-depth view of your kinase inhibitor’s efficacy, safety, and potential on specific indications or a broader cancer panel. Navigate development with confidence.
ProLiFiler™
Fast-track your lead identification with a powerful efficacy screen across 160 cancer cell lines. Pinpoint optimal targets, predict drug response, and select the best candidates for development.
In Vitro Toxicology
Leverage our InVest functional and biochemical assays to assess the safety of your lead compound(s)
In Vivo Efficacy Screen
De-risk your kinase inhibitor with robust in vivo efficacy testing across hollow fiber model, xenografts, and syngeneic models for a translatable path to clinical success.
Get Started Today
Unlock the full potential of your kinase drug development program with Reaction Biology
Contact us to learn more about our services and how we can help accelerate your path to success.