Small Molecule Discovery Technologies
Innovations in Fragment-Based Drug Discovery and Emerging Lead-Generation Tools
4/20/2027 - April 21, 2027 ALL TIMES PDT
CHI’s Small-Molecule Discovery Technologies conference covers lead-generation approaches ranging from well-established fragment-based ligand design to newer medicinal chemistry advances such as covalent chemistry and direct-to-biology (D2B) applications. A focus will be on the technological innovations of the biophysical-based tools enabling small-molecule drug discovery against difficult-to-drug targets such as protein-protein interactions (PPIs). But classic small molecule enzyme-inhibitor discovery stories, reflecting the event’s medicinal chemistry roots, will also be included. The more detailed discovery stories of small molecules advancing against PPI targets will be covered in our companion Targeting Protein-Protein Interactions conference in the second half of Drug Discovery Chemistry. The back-to-back conferences keep you apprised of new biophysical approaches, innovative applications of well-established tools, and small-molecules showing medical promise. All while providing the chance to interact with leaders in the fields of medicinal and biophysical chemistry.
Preliminary Agenda

COVALENT APPROACHES FOR DRUG DISCOVERY

FEATURED PRESENTATION: Ligand and Target Discovery in Cells

Photo of Christopher G. Parker, PhD, Professor, Chemistry, Scripps Research Institute , Professor , Chemistry , The Scripps Research Institute
Christopher G. Parker, PhD, Professor, Chemistry, Scripps Research Institute , Professor , Chemistry , The Scripps Research Institute

Cyclic Imine Mannich Electrophiles for Covalent Inhibitor Discovery

Photo of Casey J. Krusemark, PhD, Associate Professor, Medicinal Chemistry & Molecular Pharmacology, Purdue University , Associate Professor , Medicinal Chemistry & Molecular Pharmacology , Purdue University
Casey J. Krusemark, PhD, Associate Professor, Medicinal Chemistry & Molecular Pharmacology, Purdue University , Associate Professor , Medicinal Chemistry & Molecular Pharmacology , Purdue University

FRAGMENT-BASED DRUG DESIGN (FBDD)

SHP2 and Covalent Fragment Approaches: Targeting Tractable Lysines on Challenging Drug Targets

Photo of Gyorgy Keseru, PhD, Professor, Medicinal Chemistry, Research Center for Natural Sciences (RCNS), Hungary , Professor , Medicinal Chemistry , Research Centre for Natural Sciences (RCNS), Hungary
Gyorgy Keseru, PhD, Professor, Medicinal Chemistry, Research Center for Natural Sciences (RCNS), Hungary , Professor , Medicinal Chemistry , Research Centre for Natural Sciences (RCNS), Hungary

Electrophile-first strategies represent a powerful approach developing covalent ligands. To map the reactivity and accessibility of tractable lysine residues we compiled a covalent fragment library covering a wide range of aminophilic warheads. Screening the library against a phosphatase SHP2, a glycan binding lectin receptor DC-SIGN and an E3 ligase FBXW7 revealed that lysine targeting covalent fragments provide viable starting points to identify functionally active allosteric covalent compounds against challenging protein targets.

Fragment Hit to Clinical Candidate—A Novel and Selective AMPKgamma3 Activator

Photo of Parag Sahasrabudhe, PhD, Senior Principal Scientist, Pfizer Inc. , Sr Principal Scientist , Pfizer Inc
Parag Sahasrabudhe, PhD, Senior Principal Scientist, Pfizer Inc. , Sr Principal Scientist , Pfizer Inc

Fragment-Based Approaches for Challenging Targets: Insights and Learnings

Photo of Chiara R. Valenzano, PhD, Associate Director, Molecular Science, Astex Pharmaceuticals , Associate Director , Molecular Science , Astex Pharmaceuticals
Chiara R. Valenzano, PhD, Associate Director, Molecular Science, Astex Pharmaceuticals , Associate Director , Molecular Science , Astex Pharmaceuticals

Targeting mTOR with Fragment-Based Methods

Photo of Stephen W. Fesik, PhD, Professor of Biochemistry, Pharmacology & Chemistry; Orrin H. Ingram II Chair in Cancer Research, Vanderbilt University , Professor & Orrin H Ingram II Chair , Biochemistry & Pharmacology & Chemistry , Vanderbilt University
Stephen W. Fesik, PhD, Professor of Biochemistry, Pharmacology & Chemistry; Orrin H. Ingram II Chair in Cancer Research, Vanderbilt University , Professor & Orrin H Ingram II Chair , Biochemistry & Pharmacology & Chemistry , Vanderbilt University

DIRECT-TO-BIOLOGY METHODS

Unlocking the Intractable: An Integrated High-Throughput Platform for Small-Molecule Drug Discovery

Photo of Terry Lou, PhD, Scientist, Octant , Scientist , Octant
Terry Lou, PhD, Scientist, Octant , Scientist , Octant

INNOVATIVE MEDICINAL CHEMISTRY

The Scope Concept: Earlier Identification of Tractable Hits by Combining FBDD and HTS Principles

Photo of Charles Wartchow, PhD, Formerly Associate Director, Discovery Sciences, Novartis Institutes for BioMedical Research , Associate Director , Discovery Sciences
Charles Wartchow, PhD, Formerly Associate Director, Discovery Sciences, Novartis Institutes for BioMedical Research , Associate Director , Discovery Sciences

Discovery of GS-1701, a Non-Boosted Pan-Beta-Coronavirus Mpro Inhibitor

Kevin X. Rodriguez, Senior Scientist, Medicinal Chemistry, Gilead Sciences Inc. , Senior Scientist , Medicinal Chemistry , Gilead Sciences Inc

Design of Novel Antimalarial Chemotypes: Thiophene-Linked "Nucleoside" Phosphonates

Photo of Zlatko Janeba, PhD, Senior Researcher & Group Head, Medicinal Chemistry, Academy of Sciences of the Czech Republic , Senior Researcher & Group Head , Medicinal Chemistry , Academy of Sciences of the Czech Republic
Zlatko Janeba, PhD, Senior Researcher & Group Head, Medicinal Chemistry, Academy of Sciences of the Czech Republic , Senior Researcher & Group Head , Medicinal Chemistry , Academy of Sciences of the Czech Republic

PLENARY

PLENARY KEYNOTE

The Druggable Transcriptome: From RNA Recognition to Precision Medicines

Matthew D. Disney, PhD, Institute Professor & Chair, UF Scripps Institute for Biomedical Innovation & Technology , Professor , Chemistry , Scripps Research Institute


For more details on the conference, please contact:
Anjani Shah, PhD
Senior Conference Director
Cambridge Healthtech Institute
(+1) 781-247-6252
Email: ashah@healthtech.com

For sponsorship information, please contact:
Kristin Skahan
Senior Business Development Manager
Cambridge Healthtech Institute
Phone: (+1) 781-972-5431
Email: kskahan@healthtech.com


Register Early for Maximum Savings

APRIL 19

Covalent & Induced Proximity-Based Therapies

RNA-Modulating Small Molecule Drugs

Generative AI for Drug Discovery

training seminars

View In-Person Short Courses

APRIL 20 - 21

Degraders & Molecular Glues - Part 1

Small Molecule Discovery Technologies

AI/ML for Early Drug Discovery - Part 1

Linker & Conjugation Chemistries

Peptides

APRIL 21 - 22

Degraders & Molecular Glues - Part 2

Protein-Protein Interactions / Difficult Targets

AI/ML for Early Drug Discovery - Part 2

DNA-Encoded Libraries

GLP1 & Oral Peptides


Drug Discovery Chemsitry Europe

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