Understanding Kinase and Phosphatase Function Using Continuous Enzyme Activity Assays to Develop the Most Effective Drugs
Using direct, real-time, kinetic enzyme activity assays, rapidly rank covalent, reversible and irreversible inhibitors for small molecules and fragment candidates by inhibition mechanism, selectivity profiling and multiple measures of potency.
To help accelerate your drug development, we have combined chelation-enhanced fluorescence with high-throughput peptide synthesis to create optimized physiological substrate sensors so you can continuously monitor the activity of protein kinases and phosphatases. Our novel, PhosphoSens® continuous enzyme activity assays use fluorogenic kinase substrates, tailored to and optimized for use with individual protein kinases, which allow detailed analysis inhibition kinetics, providing rich insight into the mechanism of action (MOA) and mechanism of inhibition (MOI).
Whether used in high, moderate or low throughput modes, the resulting richer information from quantitative data allows you to rapidly rank candidates by inhibition mechanism, selectivity profiling and multiple measures of potency, with covalent, reversible and irreversible inhibitors and fragments.
Sophisticated Measurements in a Simple Mix & Read Format
PhosphoSens® continuous assays utilize a simple add-and-read protocol, providing the capability for real-time, kinetic measurements, with a straight-forward, fluorescence intensity measurement. These assays are compatible with essentially any commercially available fluorescence microplate reader and associated laboratory automation equipment. No stop solution or quench/develop step is needed, minimizing time while maximizing throughput.
This simple add & read method for continuous, quantitative and direct detection of activity using recombinant enzymes or crude lysates enables better decisions regarding target biology and generation of lead candidates to empower faster movement through the drug discovery process.
Erik Schaefer, Ph.D., President, CEO, CSO
Erik has over 25 years of experience leading innovative life science tool companies, including Promega, BioSource, Invitrogen/Life Technologies, Thermo Fisher Scientific and now AssayQuant Technologies, Inc. He has commercialized more than 750 new products with a focus on workflow solutions and novel assay formats to improve understanding of signal transduction pathways and phosphoregulation in normal and disease states and to enable drug development leading to more effective treatments of human disease.