Recorded Webinar

Overcoming Challenges in Small Molecule Kinase Drug Discovery – Expert Panel Discussion


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The last decade has seen a dramatic increase in the
understanding of kinase biology and significant
investments in kinase related drug discovery. Advances
in screening technologies and kinase assay panels have
enabled researchers to make broader assessments of
compound/kinase selectivity earlier in the discovery and
development process. However, the identification and
optimization of selective inhibitors having minimal
off-target activity across the highly conserved kinome
continues to hamper kinase inhibitor drug discovery and
development. Additionally, in vitro assays, a mainstay
of the kinase inhibitor discovery market, can limit the
predictive power of these assays for cellular activity,
as they do not account for inhibitor permeability,
physiological ATP concentration, and other important
features of the cellular milieu. These challenges
necessitate a two-pronged strategy where in vitro and
cell-based assay formats are used in conjunction to
provide the maximum level of information about inhibitor
function, potency and selectivity.

During this webinar, you will learn about the extensive
solutions portfolio afforded by the KINOMEscan
biochemical and PathHunter® cell-based technology
platforms, and how these complementary platforms
may together be employed to reveal new target
opportunities, guide structure based drug design,
enable robust SAR analysis, and deconvolute cellular
SAR.

 

What is covered

• Description of the KINOMEscan™ & PathHunter®
   technology platforms for small molecules in kinase
   drug discovery
• Applications of technologies to identify novel scaffolds
   & data deconvolution
• Employing biochemical and cell-based assays to
   accelerate drug discovery

 

Who should listen

• Scientist involved in kinase drug discovery including
   assay development, HTS screening, lead optimization
   and pre-clinical
• Anyone engaged in target profiling or target fishing
• Medicinal chemists and biologists engaged in lead
   optimization
• Pharmacologists, cell biologists, researchers from
   biotech and academic sectors

 

LISTEN NOW!