GPCR Modulators and Screening Optimization for New Chemotypes Using DNA-Encoded Libraries

Life Sciences, Drug Discovery & Development, Laboratory Technology, Fundamental Research,
  • Tuesday, February 13, 2024

Discover a groundbreaking webinar delving into the dynamic world of G-protein coupled receptors (GPCRs) modulator optimization in drug discovery. Small molecule modulators of GPCRs continue to be a highly productive area of research in drug discovery. Orthosteric and allosteric modalities provide a diverse and complex array of possible cellular responses, each requiring its optimization method.

In this webinar, the featured speakers will discuss components of GPCR modulator optimization including affinity, efficacy, signal bias and kinetics. As understanding of GPCR pharmacology has increased, so have methods to screen for them. The featured speakers will also describe robust methods that have been developed using DNA-encoded library (DEL) technology to screen libraries of >100 billion compounds to identify high-quality, drug-like hits that are completely structurally novel even among hits for GPCR targets that have undergone extensive screening through other technologies.

Join this webinar to gain insights into optimizing GPCR modulators and screening through DEL to better identify high-quality and drug-like hits.


Anthony Keefe, X-Chem

Anthony Keefe, PhD, Senior Vice President, Alliance Management and Innovation, X-Chem

Dr. Anthony (Tony) Keefe has over 20 years of experience with the use of encoded libraries and affinity-mediated discovery methods. He joined X-Chem in 2010 as Senior Director of Lead Discovery. From 2001 to 2009, he worked at Archemix Corp., where he developed the first-ever fully modified aptamers, thus improving the therapeutic potential of such candidate antagonists by making them highly resistant to biologically mediated degradation. From 1997 to 2001, he was a Postdoctoral Fellow in the laboratory of Nobel Laureate Jack Szostak at Harvard Medical School/Massachusetts General Hospital, developing mRNA display technology.

Tony’s achievements in the Szostak lab include the discovery of the first novel functional protein fold to have been discovered independent of biology and the introduction of a novel protein affinity tag. He is an Author of over 50 publications and is listed as an inventor on 13 granted US patents and 30 patent applications. He is also a member of the editorial board of the journal Nucleic Acid Therapeutics. Tony received his BSc in Chemistry from Exeter University in UK, in 1985, and his PhD in Chemistry from the University of Birmingham in UK, in 1989.

Message Presenter
Johan Bartholomeus, X-Chem

Johan Bartholomeus, PhD, Senior Principal Scientist, X-Chem

Dr. Johan Bartholomeus is a Senior Principal Scientist at X-Chem, Inc. specializing in Medicinal Chemistry. He earned his Ph.D in Synthetic Organic Chemistry from the University of Montreal in 2016, researching new methodologies of amination of C-H bonds.  Since joining X-Chem in 2016, Johan worked on and led several projects involving all the different classes of targets. Having mainly worked on CNS programs, he is dedicated to developing new molecules to improve the condition of people suffering from neurodegenerative diseases. He is an author of 4 publications and is listed as an inventor of 5 patent applications

Message Presenter

Who Should Attend?

This webinar will be relevant to Scientists involved in medicinal chemistry, in vitro pharmacology, screening and others involved in target nomination, validation and assessment.

What You Will Learn

Attendees will gain insights into:

  • The key principles involved in the discovery and optimization of GPCR modulators
  • The use of DEL screening methods to find high-quality and structurally diverse novel hits as starting points in the development of new GPCR modulators

Xtalks Partner


X-Chem is a leader in small molecule drug discovery services for pharmaceutical and biotech companies. As pioneers of DNA-encoded chemical library (DEL) technology, the company leverages its market-leading DEL platform to discover novel small molecule leads against challenging, high-value therapeutic targets. As experts in medicinal chemistry, X-Chem can take those leads and progress them to clinical candidates with unmatched speed. Throughout the process, X-Chem’s advanced proprietary artificial intelligence (AI) technology accelerates all steps in the process. X-Chem also provides libraries, reagents and informatic tools to allow DEL operators to get the most of their DEL platform. X-Chem empowers its partners to effectively build drug pipelines from target to clinical candidate, enhanced with AI. For further information, please visit

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