Peakdale introduces arrays for kinase studies
collection of drug-like molecules targeted towards specific
receptor families achieving drug selectivity to modulate
therapeutically relevant signalling pathways.
The latest Peakdale array will be targeted toward protein kinases, a highly regulated family of enzymes that are implicated in many diseases, such as cancer, diabetes, cardiovascular disease, and neurological disorders.
It is estimated that kinase malfunction contributes to more than 400 diseases and that greater than 20 per cent of the drug discovery efforts are focused on protein kinase inhibitors.
The Peakfinder Chemogenetic arrays are designed to enhance receptor-ligand interactions within different but closely related families of targets, as previously demonstrated by the Peakdale GPCR array.
"The addition of peakfinder chemogenetic arrays, through development of our in-house capabilities, signifies a big step forward in supporting our customers' drug discovery challenges," said Ray Fisher, Peakdale commercial director.
"It draws upon our core strength in organic synthesis, complemented with CADD and medicinal chemistry expertise."
Peakfinder arrays are designed using peakradar, a computer-aided drug design tool which incorporates information from ADMET profiles, hERG-free solubilising groups and 3D-QSAR models to direct the synthesis of focused arrays with a high-level of compound diversity.
"The introduction of peakfinder chemogenetic arrays will help place us at the forefront as a provider of medicinal chemistry products and services," said Terry Hart, Medicinal Chemistry Services director.
"They offer a significant advantage to our customers as they have critical ADMET functionality built-in and are therefore expected to produce better leads for medicinal chemists to work on allowing more rapid development and a substantially reduced failure rate."
