Aug 3rd, Sep 14 and Oct 19: "Utilizing Kinase Inhibition Data  from Journal Articles and Patents in your Research". 

Protein kinases are now one of the most intensely pursued classes of drug targets. Over 30 distinct kinase targets and over 200 kinase inhibitors are in clinical development. While currently most of the clinical kinase drug targets are being investigated for treatment of cancer, a growing number of other disorders including immunological, neurological, metabolic and infectious diseases, have been associated with dysregulation of protein phosphorylation. 

Most of the current kinase inhibitors target the ATP binding site of the kinase catalytic domain, despite the high degree of conservation of the ATP site across the kinome. In fact, the clinical efficacy of many of the current kinase inhibitor oncology drugs is now well understood in terms of their polypharmacology – their ability to inhibit multiple kinase at the same time. The development of novel efficacious and safe compounds thus requires a finely tuned balance of polypharmacology and selectivity. Although biochemical kinase profiling is now well established in discovery programs, experimental testing of many compounds across hundreds of kinases can be very expensive. With this Webinar series we want to introduce the Kinase Knowledge Base (KKB): an extensive set of high-quality small molecule kinase inhibitor data curated and standardized from scientific publications and patents as a valuable resource to guide the discovery and development of novel targeted kinase inhibitors as chemical probes and potential drug candidates.

AUG 3rd 2011: A RESOURCE OF HIGH-QUALITY SMALL MOLECULE KINASE INHIBITOR DATA FROM LITERATURE AND PATENTS: THE KINASE KNOWLEDGEBASE

This Webinar will provide an overview of the Kinase Knowledgebase(KKB). We will discuss what types of information the KKB contains; how data are annotated and standardized; how the information is organized, details captured and data constantly growing to support modern research.

 View Slides 

SEP 14^th 2011: HOW KINASE INHIBITION DATA CAN BE LEVERAGED IN PRACTICE. 

We will illustrate two scientific scenarios in which KKB can be used to inform a research or development project to support decision making about how to move a project forward or how to find entry points into a novel project.  In on example we will focus on identifying compounds of interest using the KKB based on chemotypes and kinase activity.  In another illustration we will use KKB to charaterize compounds of interest by systematically annotating them based on data available in the KKB, i.e. generating a KKB profile based on reported activity / inhibition data.  This can be a useful first step to prioritize the most promising compounds before committing significant resources to profile compounds of interest experimentally.

Watch the recording using Adobe Flash (requires Adobe Flash plugin)

Watch the recording using QuickTime (requires Apple QuickTime plugin)

Download a sample data set of KKB mapped onto commercial libraries as discussed during the webinar (MS Excel format).

OCT 19^th 2011: DEVELOPMENT OF PREDICTIVE MODELS AND VIRTUAL KINASE PROFILING UTILIZING KINASE KNOWLEDGEBASE DATA

In this Webinar we will illustrate how KKB data an be used to develop predictive models using machine learning and applying these models to virtually profile a set of compounds of interest.  By developing predictive kinase models, we can essentially amplify the content of the KKB (within a reasonable applicability domain) and thus extend the KKB profile presented in Webinar 2 towards a virtual / predicted profile, to prioritize compounds of interest. In addition we will illustrate the development of highly predictive kinase classifiers and their potential for application to virtual prioritization of compounds for kinase screening.  With such an approach it may be possible to avoid very large HTS campaigns and instead screen only 0.1 to 1 % of compounds that were selected on a kinase predictor.

Watch the recording using Adobe Flash (requires Adobe Flash plugin)

Watch the recording using QuickTime (requires Apple QuickTime plugin)