Fragment-based Screening
Zenobia has access to most well-known fragment screening methods including thermal melt shift, NMR, SPR and biochemical screens. In addition to more typical biochemical screens which often have a limited sensitivity range, especially for weakly binding inhibitors, through our collaboration with Palo Alto Research Center, we can screen targets by the nanocalorimetry method which accurately yields Ki up to 2mM.
After a primary screen, a secondary screen using x-ray crystallography is conducted to identify compound binding mode and help to eliminate false positives. For our internal active drug discovery programs, we have used Tm shift, nanocalorimetry and more traditional biochemical assays as a primary screen. An example of a Tm shift screen followed by crystal structure for one of our internal programs is shown below.
After a primary screen, a secondary screen using x-ray crystallography is conducted to identify compound binding mode and help to eliminate false positives. For our internal active drug discovery programs, we have used Tm shift, nanocalorimetry and more traditional biochemical assays as a primary screen. An example of a Tm shift screen followed by crystal structure for one of our internal programs is shown below.
As a discovery service, Zenobia will work with its client to identify the best tool for screening that particular target class. Tm shift and nanocalorimetry are expected to provide adequate data for most programs although in some cases NMR or SPR screens may be warranted.
Zenobia has access to NMR through a relationship with the UCSD NMR facility and SPR through a collaboration with Biosensor tools. Tm shift and traditional biochemical assays are conducted at Zenobia and nanocalorimetry through our collaboration with PARC.
Crystallography data are collected at the Advanced Photon Source.
Zenobia has access to NMR through a relationship with the UCSD NMR facility and SPR through a collaboration with Biosensor tools. Tm shift and traditional biochemical assays are conducted at Zenobia and nanocalorimetry through our collaboration with PARC.
Crystallography data are collected at the Advanced Photon Source.
