Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
Target Engagement Case Studies: Covalent and Non-Covalent Mechanisms
Discussion Leader: Meredeth McGowan (MOMA Therapeutics, United States)
7:40 pm - 8:05 pm
Ivar McDonald (Bristol Myers Squibb, United States)
"Covalent Inhibitors of MK2 Utilizing Non-Traditional Warheads"
8:05 pm - 8:15 pm
Discussion
8:15 pm - 8:40 pm
Derun Li (Nimbus Therapeutics, United States)
"Thinking Covalently to Tackle a Challenging Target: Designing Selective WRN Covalent Inhibitors from Non-Covalent Binders"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Mike Ameriks (Johnson & Johnson, United States)
"Discovery and Characterization of Non-Covalent Monoacyclglycerol Lipase (MAGL) Inhibitors that Exhibit Target-Mediated Drug Disposition"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Topics in Global Health
Discussion Leaders: Anil Gupta (Calibr-Skaggs Institute for Innovative Medicines, United States) and Julia Haas (Think Bioscience, United States)
9:00 am - 9:30 am
Julien Papillon (TB Alliance, United States)
"Targeting the Mycolic Acid Pathway for Tuberculosis Treatment: Optimization of Indolecarboxamide Inhibitors of MmpL3"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Stephen Brand (Medicines for Malaria Venture, Switzerland)
"Discovery of Long-Acting Antimalarials"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Margaret Phillips (University of Texas Southwestern Medical Center, United States)
"Structure-Based Discovery and Development of Highly Potent Dihydroorotate Dehydrogenase Inhibitors for Malaria Chemoprevention"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Thomas Kirrane (Novartis Biomedical Research, United States)
"Identification of IWY357, a Promising Pyrazine-2-Carboxamide Compound, as a Highly Effective and Prolonged Suppressor of Plasmodium Falciparum Blood Stage, Showing Potential for Single-Dose Cure in Uncomplicated Malaria"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
3:00 pm - 4:00 pm
The GRC Power Hour™
The GRC Power Hour™ is designed to address diversity and inclusion in the scientific workplace by providing a safe environment for informal and meaningful conversations amongst colleagues of all career stages. The program supports the professional growth of all members of our communities, including ethnicity, race and/or gender identity by providing an open forum for discussion and mentoring.
Organizers: Dustin Mergott (Eli Lilly and Company, United States) and Ludivine Moine (Blueprint Medicines, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Synthetic Breakthroughs Enabling Innovations in Medicinal Chemistry
Discussion Leader: Izzat Raheem (Merck & Co. Inc., United States)
7:30 pm - 8:00 pm
Scott Shaw (Bristol Myers Squibb, United States)
"Charting a Course out of Flatland: Discovery of RXFP1 Agonists by Embracing Underutilized Synthetic Techniques"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Chandrasekar Venkataramani (Gilead Sciences, United States)
"Application of Acyl Sulfonimidamides in the Discovery of GS-9716, a Potent Orally Active MCL1 Inhibitor"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Libby Hennessy (Merck, United States)
"Discovery and Clinical Evaluation of a Potent and Selective A2A/2B Dual Receptor Antagonist: How Innovative Chemistry Accelerated Med Chem and Process Efforts"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Challenging Medicinal Chemistry Dogma
Discussion Leader: David Marcoux (TRIANA Biomedicines, United States)
9:00 am - 9:30 am
Randy Miller (Merck, United States)
"Optimizing Drug Potency Can Accomplish Far More than We Have Traditionally Thought"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Stéphane Ciblat (Ventus Therapeutics, Canada)
"Drug Discovery Driven by Dynamic Solvation: The Discovery and Optimization of an Aminothiadiazole Series of cGAS Inhibitors"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
Jennifer Petter (Arrakis Therapeutics, United States)
"Drugging MYC mRNA with Small Molecules: Every Dogma Has Its Day"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
David Weinstein (Vividion Therapeutics, United States)
"Discovery of VVD-130037: A First-in-Class Covalent Allosteric Molecular Glue of the KEAP1-CUL3 Ligase Complex"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Advances in Protein Conjugate Therapeutics
Discussion Leader: Dustin Mergott (Eli Lilly and Company, United States)
7:30 pm - 8:00 pm
Christopher Marvin (AbbVie, Inc., United States)
"Optimization of Glucocorticoid Linker-Payloads for Antibody-Drug Conjugates"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Marc-André Kasper (Tubulis GmbH, Germany)
"Delivering Primary, Secondary, Tertiary and Phenolic Alcohols: Linker Systems for Antibody-Drug-Conjugates that Enable Stable Conjugation and Tunable Traceless Release of Hydroxy-Containing Payloads"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Steve Staben (Lycia Therapeutics, United States)
"Lysosome Targeting Protein Small Molecule Conjugates for the Degradation of Immunoglobulins"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
ADME and Safety Problem-Solving
Discussion Leader: Silvana Leit (Nimbus Therapeutics, United States)
9:00 am - 9:30 am
Rebecca Gallego (Pfizer, United States)
"Navigation of Plasma Instability, CYP2D6 Metabolism and Active Metabolites to Deliver a Small Molecule Inhibitor of HPK1"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Subharekha Raghavan (Merck & Co. Inc., United States)
"Balancing Adenosine Transporter Liability with Soluble Guanylate Cyclase (sGC) Stimulator Activity for the Treatment of PAH"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Jullien Rey (Novartis, Switzerland)
"Reducing Lipophilicity While Filling Highly Lipophilic Pockets : Leveraging the Power of Fluorine"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Jeffrey Axten (GSK, United States)
"Discovery and Optimization of Orally Available Small Molecule Furin Inhibitors"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Molecular Glues and Monovalent Degrading Technologies
Discussion Leader: Justin Ernst (Belharra Therapeutics, United States)
7:30 pm - 8:00 pm
Yongxin Han (Nested Therapeutics, Inc., United States)
"Discovery of NST-628, a Fully Brain-Penetrant Non-Degrading MEK-Pan-RAF Molecular Glue for Treating RAS and RAF Driven Cancers"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Laura McAllister (Monte Rosa Therapeutics, Switzerland)
"Molecular Glue Degraders of VAV1 for Autoimmune Diseases: A New Degron and Glue Chemotype for an Undruggable Target"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Kevin Freeman-Cook (Plexium, United States)
"Discovery of PLX-4545, a Molecular Glue Degrader of IKZF2"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Business Meeting
Nominations for the Next Vice Chair(s); Complete the GRC Evaluation Forms; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
Discussion Leader: Alex Cortez (Bristol Myers Squibb, United States)
9:00 am - 9:30 am
Michael G. Hahn (Bayer AG Pharmaceuticals, Germany)
"The Journey to the Alpha-2C Adrenergic Receptor Antagonist BAY 2925976 for the Treatment of Obstructive Sleep Apnea (OSA)"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Deborah Mortensen (Bristol Myers Squibb, United States)
"Discovery of the Casein Kinase 1α (CK1α) Degrader BMS-986397 for the Treatment of Acute Myeloid Leukemia (AML)"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Darryl Kato (Gilead Sciences, United States)
"Discovery of Elunonavir (GS-1156): A Non-Boosted HIV Protease Inhibitor that Achieves a Half-Life of More than Two Weeks in Humans"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Neelu Kaila (Nimbus Therapeutics, United States)
"Discovery of NDI-101150, A Highly Potent and Selective HPK1 Inhibitor for the Treatment of Cancer, through Structure-Based Drug Design"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: New Directions in Drug Discovery: Expanding Exploration of Chemical Space
Discussion Leader: Erin DiMauro (Merck & Co., Inc., United States)
7:30 pm - 8:30 pm
Emma Parmee (Johnson & Johnson, United States)
"New Directions in Drug Discovery: Expanding Exploration of Chemical Space"
8:30 pm - 8:55 pm
Discussion
8:55 pm - 9:15 pm
General Discussion
9:15 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure