Alternatives to HTS – Hit-finding Approaches in the Medicinal Chemist’s Arsenal

While high-throughput screening (HTS) remains a powerful weapon for hit identification, it is important to be aware of the many alternative tools available to the medicinal chemist for initiating a drug discovery program. No hit identification method is always fruitful; they all have their strengths and weaknesses, and only by judicious integration of hit identification approaches can the chances of success be maximized.

In this webinar, Charles River’s scientists take a look at some of the complementary approaches to HTS from a chemist’s perspective and how these strategies have been successfully applied to real drug discovery programs at Charles River for Charles River’s partners.

Examples of such approaches include:

• Knowledge-based design: using chemistry expertise to make inventive modifications to known bioactive molecules
• In silico screening: using structure and ligand-based approaches to virtually screen large collections of compounds
• Fragment screening via low-throughput biophysical techniques such as SPR and NMR

Learning objectives:

• Better understand the range of alternative hit-finding approaches to HTS
• Understand how these approaches can be complementary to each other
• View case study examples of how each has been successfully applied to real drug discovery programs

Speaker

Sam Mann, MChem, PhD, Principal Scientist, Medicinal Chemistry, Charles River Laboratories

Sam Mann graduated from the University of York with a Master of Chemistry degree, having spent a year on exchange at the Université Joseph Fourier in Grenoble, France. He then moved to London to study for a PhD under the supervision of Dr. Tom Sheppard at University College London. His doctoral research focused on the development of new synthetic methodologies involving cyclic oxygen, nitrogen and sulfur acetal derivatives and their applications in palladium (II)-catalysed oxidations, multicomponent reactions and medium ring synthesis.

He later joined Argenta, which became part of Charles River in 2014. Having worked on a variety of drug discovery programs for high profile clients, he quickly progressed to his current position as a principal scientist, leading the medicinal chemistry effort on an early stage oncology project. Dr. Mann has approximately six years’ experience in oncology drug discovery, working primarily on kinase targets.

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