Human Kinase Chemical Probe Program

Protein kinases constitute a family of more than 500 proteins in human with central functions in most aspects of life. Due to their key roles in cellular signalling, deregulation of kinases is frequently associated with disease and inhibitors have been developed for a considerable number of them. Although kinases are well established drug targets many of the developed kinase inhibitors lack selectivity over related kinases making them less useful tools for biological experiments to explore the activity of a specific kinase. In addition there is a large number of kinases ‘the untargeted kinome’ for which no potent, specific and cell active inhibitors ‘probes’ are available.

Goals

  • to develop chemical probes for protein kinases
  • to share chemical probes with the research community
  • to create a comprehensive chemogenomics set

susanne.muller-knapp[at]sgc.ox.ac.uk (Susanne Muller-Knapp) coordinates the Kinase Chemical Probe Program.

 

SGC Site Lead Investigator Primary Capabilities Primary Focus
Campinas jon.elkins[at]sgc.ox.ac.uk (Jon Elkins) Protein expression
X-ray crystallography
Medicinal chemistry
Cell assays

 

RNA splicing
In-house kinase profiling

 

UNC

tim.willson[at]unc.edu (Tim Willson) Medicinal chemistry
Compound sets
Chemical probes
Chemogenomics
Oxford alex.bullock[at]sgc.ox.ac.uk (Alex Bullock) Protein expression
X-ray crystallography
Screening
Cell assays
Chemical biology
Frankfurt stefan.knapp[at]sgc.ox.ac.uk (Stefan Knapp) Screening
X-ray crystallography
Medicinal chemistry
Cell assays
Chemical biology
Chemical probes
Name Structure Protein Family Specific Targets Control In vivo parameters tested* Addedsort ascending
FM-381 Kinase JAK3 FM-476 02/17
NVS-PAK1-1 Kinase PAK1 NVS-PAK1-C no 06/16
glqxz9283 sfy39587stf02 mnesdcuix8
sfy39587stf03