Kinase Assay Substrates
&
Kinome Profiling Services
PRODUCTS
We offer Kinase Substrates for direct, real-time(kinetic) Fluoroscent Microplate Assays that yield better, more reliable data than other methods, enabling better decisions regarding target biology and generation of lead candidates to empower faster movement through the drug discovery process.
SERVICES
Our Kinome Profiling & Compound Testing services come with the flexibility that can meet your HTS needs, including a variety of compound potency measurements and the option for preincubations, comparison of ATP at the Km or 1 mM, and analysis with recombinant enzyme or crude cell lysates. Our profiling services portfolio include Kinases,LIPID (DGK) Kinases & Phosphatases !
Our services enable complex determinations to provide critical understanding of enzyme inhibitor properties to improve drug performance, including:
Kinome Profiling – Multiple ATP concentrations & 400+ wild-type kinases (mutants as per customer request)
IC50 or Ki – 12 pts, BSA or DTT; low or high ATP, protein complexes & crude lysates
kinact/KI – 24 pts for time-dependent inhibition with covalent compounds
Residence Time – Uses Jump Dilution method with a range of detection from 30 seconds to 2 days
Mechanism of Action (MOA) – ATP Competitive, Un-competitive or Non-competitive
EC50 – Assess potency of compounds for target activation
PhosphoSens® Technology forms the basis of its extensive portfolio of more than 400 unique Kinases and Phosphatase assays. We offer two assay formats: Continuous and End-Point/Red-Shift, compatible with 96, 384 and 1536-well plates and produce signals that are directly proportional to the amount of phosphorylated product present in the reaction mixture at the time of the measurement. In both cases, potency results have been shown to align with those obtained from cell-based assays, accelerating, and improving lead identification, characterization, profiling, and optimization studies, leading to the potential for developing drugs faster and with better efficacy.
Both assay formats are fully compatible with a wide range of ATP concentrations (including low to physiological [mM] levels) and use physiological Mg++, Mn++, Ca++ ion concentrations and peptide sequences derived from known substrates. With our selective PhosphoSens substrates, assays can be performed using crude cell or tissue lysates providing a more physiological context, including measuring activity of kinases in functional complexes that are formed in living cells.
Services available:
Kinome Profiling Services
Phosphatome Profiling Services
IC50 Services
TDI- Time Dependent Inhibition Services
Kinase Assay Validation ( ATP Km | Sensor Km | Enzyme Titration | DMSO Tolerance | Inhibitor Titration
HTS Kinase Profiling Assay Workflow with PhosphoSens Technology