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 Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Small Molecule Approaches for Immuno-Oncology
Discussion Leaders: Laura D'Agostino (Bristol Myers Squibb, United States) and Julia Haas (Pfizer Boulder R&D, United States)
7:40 pm - 8:10 pm
Eric Miller (Emory University School of Medicine, United States)
"A Medicinal Chemist’s Primer to Immuno-Oncology: Case Study on the Development of Small Molecule CXCR4 Antagonists"
8:10 pm - 8:15 pm
Discussion
8:15 pm - 8:45 pm
Louis Chupak (Bristol-Myers Squibb, United States)
"Phenotypic Discovery and Optimization of Potent T-Cell Modulators: Dual Inhibition of Diacylglycerol Kinases Alpha and Zeta"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Nigel Swain (Sosei Heptares, United Kingdom)
"Discovery of HTL0039732: A Potent and Selective EP4 Receptor Antagonist for Cancer Immunotherapy"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Emerging Technologies: From In Silico to Implementation
Discussion Leader: H. Rachel Lagiakos (Schrödinger, United States)
9:00 am - 9:30 am
David Hallett (Exscientia, United Kingdom)
"AI-Driven Drug Discovery Delivers A2AR Antagonist Clinical Candidate"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Falgun Shah (Merck & Co., Inc., United States)
"Case Studies Utilizing an In Silico ADMET Toolbox to Prioritize Chemical Series with a High Probability of Success"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Bryce Harrison (Morphic Therapeutic, United States)
"In Silico Driven Drug Discovery of a Zwitterionic Integrin αvβ6 Development Candidate for Fibrosis"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Heike Schoenherr (Relay Therapeutics, United States)
"Motion-Based Drug Design™ in Action: Discovery of RLY-4008, an Isoform Selective, Irreversible Small Molecule Inhibitor of FGFR2"
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: David Marcoux (Janssen Pharmaceuticals, United States) and Amy Hart (Aleksia Therapeutics, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Therapies Targeting Diseases of the CNS
Discussion Leader: Emily Peterson (Biogen, United States)
7:30 pm - 8:00 pm
Peter Fuller (Merck, United States)
"Discovery of MK-1468: An Exquisitely Selective, CNS Penetrant LRRK2 Inhibitor for the Treatment of Parkinson’s Disease"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Mark Healy (Novartis, United States)
"The Discovery and First Disclosure of MIJ821, a Novel, Rapidly Acting Antidepressant"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Kevin Guckian (Biogen, United States)
"Discovery of a Clinical Stage OGA Inhibitor and Companion PET tracer for the Treatment of Alzheimer’s Disease"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Synthetic Technologies to Enable Medicinal Chemistry
Discussion Leader: Amy Hart (Aleksia Therapeutics, United States)
9:00 am - 9:30 am
Jesus Alcazar (Janssen Pharmaceutical Companies of J&J, Spain)
"How Flow Chemistry Can Impact Drug Discovery: An Automated Tool to Access Novel Chemical Space with Improved Fsp3"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Ben Cons (Astex Pharmaceuticals, United Kingdom)
"Emerging Synthetic Technologies in Fragment-Based Drug Discovery"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
Alison Wendlandt (Massachusetts Institute of Technology, United States)
"Selective Catalytic Isomerization Reactions"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Michelle Hall (Eli Lilly, United States)
"Genetic Nanomedicine: State of the Art, Frontiers, and Current Research"
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
Recent Advances in Protein Degraders
Discussion Leader: Joachim Rudolph (Genentech, United States)
7:30 pm - 8:00 pm
Eric Fischer (Harvard Medical School / Dana Farber Cancer Institute, United States)
"Family-centric Screening Enables the Development of Selective HDAC Degraders"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
James Henderson (C4 Therapeutics, United States)
"Discovery of CFT7455: A Potent IKZF1/3 Degrader with Enhanced Catalytic and Pharmacological Properties"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Woody Sherman (Roivant Sciences, United States)
"Driving the Design of Induced Proximity Modulators via Ternary Structure Ensembles from MD+HDX"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Strategies for Overcoming Drug Safety Liabilities
Discussion Leader: Izzat Raheem (Merck & Co. Inc., United States)
9:00 am - 9:30 am
Iyassu Sebhat (Kallyope, United States)
"Gut-Targeted GPR40 Agonists to Engage the Gut-Brain Axis"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Michael Rudd (Merck & Co., Inc, United States)
"Overcoming an Ames-positive Lead to Enable the Discovery of mGluR2 Negative Allosteric Modulator MK-8768"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Grace Chuang (Cytokinetics, United States)
"Challenges with the Prediction of Fraction Metabolized by CYPs and Application of New Strategies to the Cardiac Myosin Inhibitor Aficamten "
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Patrizio Mattei (F. Hoffmann-La Roche Ltd., Switzerland)
"Abx MCP RG6006 - a Tethered Macrocyclic Peptide Targeting Acinetobacter"
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
New Directions in Beyond 500 Compounds: From PK to the Clinic
Discussion Leader: Andrew Scholte (Sanofi, United States)
7:30 pm - 8:00 pm
Matthew Mitcheltree (Merck & Co., Inc., United States)
"An Adaptable Toolkit for BRo5 Property Engineering Delivers Permeable KRAS-targeting Peptides"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
John O. Link (Gilead Sciences, United States)
"The Discovery and Development of Lenacapavir (GS-6207): a Twice-Yearly Injectable or Orally Dosed First-in-Class HIV Capsid Inhibitor"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Xiaozhang Zheng (Kymera Therapeutics, United States)
"Targeted Protein Degrader Pharmacokinetics: Optimizing towards Oral Bioavailability"
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; Discuss Future Dates and Venue; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
Discussion Leader: Meredeth McGowan (MOMA Therapeutics, United States)
9:00 am - 9:30 am
Michael Graupe (Gilead Sciences, United States)
"GS-4224: A Potent, Oral Small Molecule PD-L1 Inhibitor"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Scott Edmondson (Nimbus Therapeutics, United States)
"Discovery of NDI-034858, a Highly Potent and Selective TYK2-JH2 Inhibitor for the Treatment of Autoimmune Diseases, through Structure-based Drug Design"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Michelle Garnsey (Pfizer, Inc, United States)
"Discovery of the MC4R Antagonist PF-07258669 as a Potential Treatment for Appetite Loss"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Maksim Osipov (Denali Therapeutics, United States)
"Discovery of DNL343: a Potent Selective and Brain-penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases"
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: Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery
Discussion Leaders: Michael Ellis (Bristol Myers Squibb, United States)
7:30 pm - 8:30 pm
Rosana Kapeller (ROME Therapeutics, United States)
"Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery"
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