March 4, 2016

 

 As fragment screening continues to grow in popularity and establish itself as an integral part of discovery research, the emergence of more and more compounds added to fragment library collections seems to grow exponentially. What once was an efficient means of effectively screening a target to provide information about its drugability or identify the unique building blocks of a clinical candidate, has now become diluted in a pool of tens or hundreds of thousands of compounds to endlessly screen.

 

Designing efficiency into any application should be one of the primary principles and only be modified when expanded scope adds additional information. When this simple required element is ignored or modified to adapt to an ever changing landscape of discovery research, the other primary principle that appears to be compromised is value. Value is the true measurement of success. The simplicity of design directly relates to the elegance of its footprint, regardless of its true complexity, an...

January 27, 2016

Zenobia Therapeutics was founded in 2008 by Drs Vicki Nienaber and Robert Meadows. Zenobia’s founders are pioneers in the field of fragment-based lead discovery (FBLD) contributing to the model NMR screening paradigm, SARbyNMR (1,2) and inventing the first crystallographic screening method, CrystaLead (3).

Recognizing that diseases of the CNS are a significant unmet medical need, Zenobia Therapeutics quickly adapted the strengths of FBLD to address one of the biggest challenges of CNS drug discovery: finding leads that cross the blood-brain-barrier (BBB).  The leading chemical properties for brain penetration include low molecular weight and clogP.  So starting with small simple fragments and growing them systematically into small efficient leads seemed a strategic advantage in discovery of a CNS-directed therapeutic (4).  Furthermore, data mining of historic clinical data showed that small simple compounds have a better chance of success in the clinic. This coined the phrase: “Start sm...

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