Sunday
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2:00 pm - 9:00 pm |
Arrival and Check-in
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6:00 pm - 7:00 pm |
Dinner
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7:30 pm - 7:40 pm |
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
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7:40 pm - 9:30 pm |
Small Molecule Approaches for Immuno-Oncology
Discussion Leaders: Laura D'Agostino (Bristol Myers Squibb, USA) and Julia Haas (Pfizer Boulder R&D, USA)
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7:40 pm - 8:10 pm |
Eric Miller (Emory University School of Medicine, USA)
"A Medicinal Chemist’s Primer to Immuno-Oncology: Case Study on the Development of Small Molecule CXCR4 Antagonists"
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8:10 pm - 8:15 pm |
Discussion
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8:15 pm - 8:45 pm |
Louis Chupak (Bristol Myers Squibb, USA)
"Phenotypic Discovery and Optimization of Potent T-Cell Modulators: Dual Inhibition of Diacylglycerol Kinases Alpha and Zeta"
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8:45 pm - 8:50 pm |
Discussion
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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"
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9:20 pm - 9:30 pm |
Discussion
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Monday
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7:30 am - 8:30 am |
Breakfast
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9:00 am - 12:30 pm |
Emerging Technologies: From In Silico to Implementation
Discussion Leader: H. Rachel Lagiakos (Schrödinger, USA)
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9:00 am - 9:30 am |
Steve Swann (Exscientia, USA)
"Discovery of the First AI-Designed A2A Antagonist to Enter Clinical Trials for Immuno-Oncology"
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9:30 am - 9:45 am |
Discussion
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9:45 am - 10:15 am |
Falgun Shah (Merck & Co., Inc., USA)
"AI In Toxicology: Case Studies Utilizing an In Silico Toxicology Toolbox to Prioritize Chemical Series with a High Probability of Success"
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10:15 am - 10:30 am |
Discussion
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10:30 am - 11:00 am |
Coffee Break
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11:00 am - 11:30 am |
Bryce Harrison (Morphic Therapeutic, USA)
"In Silico Driven Drug Discovery of a Zwitterionic Integrin αvβ6 Development Candidate for Fibrosis"
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11:30 am - 11:45 am |
Discussion
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11:45 am - 12:15 pm |
Heike Schoenherr (Relay Therapeutics, USA)
"Motion-Based Drug Design™ in Action: Discovery of RLY-4008, an Isoform Selective, Irreversible Small Molecule Inhibitor of FGFR2"
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12:15 pm - 12:30 pm |
Discussion
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12:30 pm - 1:30 pm |
Lunch
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1:30 pm - 4:00 pm |
Free Time
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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: Jennifer Riggs (Bristol Myers Squibb, USA) and David Marcoux (Janssen Pharmaceuticals, USA)
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4:00 pm - 6:00 pm |
Poster Session
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6:00 pm - 7:00 pm |
Dinner
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7:30 pm - 9:30 pm |
Therapies Targeting Diseases of the CNS
Discussion Leader: Emily Peterson (Biogen, USA)
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7:30 pm - 8:00 pm |
Peter Fuller (Merck & Co., Inc., USA)
"Discovery of MK-1468: An Exquisitely Selective, CNS Penetrant LRRK2 Inhibitor for the Treatment of Parkinson’s Disease"
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8:00 pm - 8:10 pm |
Discussion
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8:10 pm - 8:40 pm |
Duane Burnett (Arkuda Therapeutics, USA)
"Progranulin Enhancers for the Treatment of FTD-GRN"
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8:40 pm - 8:50 pm |
Discussion
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8:50 pm - 9:20 pm |
Kevin Guckian (Biogen, USA)
"Discovery of a Clinical Stage OGA Inhibitor and Companion PET tracer for the Treatment of Alzheimer’s Disease"
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9:20 pm - 9:30 pm |
Discussion
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Tuesday
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7:30 am - 8:30 am |
Breakfast
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9:00 am - 12:30 pm |
Synthetic Technologies to Enable Medicinal Chemistry
Discussion Leader: Amy Hart (Aleksia Therapeutics, USA)
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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"
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9:30 am - 9:45 am |
Discussion
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9:45 am - 10:15 am |
Rachel Grainger (Astex Pharmaceuticals, United Kingdom)
"Emerging Synthetic Technologies in Fragment-Based Drug Discovery"
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10:15 am - 10:30 am |
Discussion
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10:30 am - 11:00 am |
Group Photo / Coffee Break
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11:00 am - 11:30 am |
Alison Wendlandt (Massachusetts Institute of Technology, USA)
"Selective Catalytic Isomerization Reactions"
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11:30 am - 11:45 am |
Discussion
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11:45 am - 12:15 pm |
Michelle Hall (Eli Lilly, USA)
"Genetic Nanomedicine: State of the Art, Frontiers, and Current Research"
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12:15 pm - 12:30 pm |
Discussion
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12:30 pm - 1:30 pm |
Lunch
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1:30 pm - 4:00 pm |
Free Time
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4:00 pm - 6:00 pm |
Poster Session
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6:00 pm - 7:00 pm |
Dinner
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7:30 pm - 9:30 pm |
Recent Advances in Modulators of Protein-Protein Interactions
Discussion Leader: Alex Cortez (Bristol Myers Squibb, USA)
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7:30 pm - 8:00 pm |
Eric Fischer (Harvard Medical School / Dana Farber Cancer Institute, USA)
"Family-centric Screening Enables the Development of Selective HDAC Degraders"
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8:00 pm - 8:10 pm |
Discussion
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8:10 pm - 8:40 pm |
James Henderson (C4 Therapeutics, USA)
"Discovery of CFT7455: A Potent IKZF1/3 Degrader with Enhanced Catalytic and Pharmacological Properties"
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8:40 pm - 8:50 pm |
Discussion
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8:50 pm - 9:20 pm |
Woody Sherman (Roivant Sciences, USA)
"Driving the Design of Induced Proximity Modulators via Ternary Structure Ensembles from MD+HDX"
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9:20 pm - 9:30 pm |
Discussion
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Wednesday
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7:30 am - 8:30 am |
Breakfast
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9:00 am - 12:30 pm |
Strategies for Overcoming Drug Safety Liabilities
Discussion Leader: Izzat Raheem (Merck & Co. Inc., USA)
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9:00 am - 9:30 am |
Iyassu Sebhat (Kallyope, USA)
"Gut-Targeted GPR40 Agonists to Engage the Gut-Brain Axis"
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9:30 am - 9:45 am |
Discussion
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9:45 am - 10:15 am |
Michael Rudd (Merck Research Laboratories, USA)
"Overcoming an Ames-positive Lead to Enable the Discovery of mGluR2 Negative Allosteric Modulator MK-8768"
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10:15 am - 10:30 am |
Discussion
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10:30 am - 11:00 am |
Coffee Break
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11:00 am - 11:30 am |
Grace Chuang (Cytokinetics, USA)
"Challenges with the Prediction of Fraction Metabolized by CYPs and Application of New Strategies to the Cardiac Myosin Inhibitor Aficamten"
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11:30 am - 11:45 am |
Discussion
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11:45 am - 12:15 pm |
Patrizio Mattei (F. Hoffmann-La Roche Ltd., Switzerland)
"Abx MCP RG6006, a Tethered Macrocyclic Peptide Targeting Acinetobacter: Identifying the Drug-like Property Space for a New Class of Antibiotics"
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12:15 pm - 12:30 pm |
Discussion
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12:30 pm - 1:30 pm |
Lunch
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1:30 pm - 4:00 pm |
Free Time
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4:00 pm - 6:00 pm |
Poster Session
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6:00 pm - 7:00 pm |
Dinner
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7:30 pm - 9:30 pm |
New Directions in Beyond 500 Compounds: From PK to the Clinic
Discussion Leader: Andrew Scholte (Sanofi, USA)
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7:30 pm - 8:00 pm |
Matthew Mitcheltree (Merck & Co., Inc., USA)
"An Adaptable Toolkit for BRo5 Property Engineering Delivers Permeable KRAS-targeting Peptides"
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8:00 pm - 8:10 pm |
Discussion
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8:10 pm - 8:40 pm |
John O. Link (Gilead Sciences, USA)
"The Discovery and Development of Lenacapavir (GS-6207): a Twice-Yearly Injectable or Orally Dosed First-in-Class HIV Capsid Inhibitor"
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8:40 pm - 8:50 pm |
Discussion
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8:50 pm - 9:20 pm |
Xiaozhang Zheng (Kymera Therapeutics, USA)
"Targeted Protein Degrader Pharmacokinetics: Optimizing towards Oral Bioavailability"
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9:20 pm - 9:30 pm |
Discussion
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Thursday
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7:30 am - 8:30 am |
Breakfast
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8:30 am - 9:00 am |
Business Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
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9:00 am - 12:30 pm |
Late-Breaking Topics: First Disclosures of Clinical Candidates
Discussion Leader: Meredeth McGowan (MOMA Therapeutics, USA)
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9:00 am - 9:30 am |
Michael Graupe (Gilead Sciences Inc., USA)
"GS-4224: A Potent, Oral Small Molecule PD-L1 Inhibitor"
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9:30 am - 9:45 am |
Discussion
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9:45 am - 10:15 am |
Scott Edmondson (Nimbus Therapeutics, USA)
"Discovery of NDI-034858, a Highly Potent and Selective TYK2-JH2 Inhibitor for the Treatment of Autoimmune Diseases, through Structure-based Drug Design"
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10:15 am - 10:30 am |
Discussion
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10:30 am - 11:00 am |
Coffee Break
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11:00 am - 11:30 am |
Michelle Garnsey (Pfizer, Inc, USA)
"Discovery of the MC4R Antagonist PF-07258669 as a Potential Treatment for Appetite Loss"
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11:30 am - 11:45 am |
Discussion
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11:45 am - 12:15 pm |
Maksim Osipov (Denali Therapeutics, USA)
"Discovery of DNL343: a Potent Selective and Brain-penetrant eIF2B Activator Designed for the Treatment of Neurodegenerative Diseases"
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12:15 pm - 12:30 pm |
Discussion
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12:30 pm - 1:30 pm |
Lunch
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1:30 pm - 4:00 pm |
Free Time
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4:00 pm - 6:00 pm |
Poster Session
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6:00 pm - 7:00 pm |
Dinner
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7:30 pm - 9:30 pm |
Keynote Session: Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery
Discussion Leader: Michael Ellis (Bristol-Myers Squibb, USA)
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7:30 pm - 8:30 pm |
Rosana Kapeller (ROME Therapeutics, USA)
"Unlocking the Dark Genome and Other Uncharted Territories in Drug Discovery"
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8:30 pm - 8:55 pm |
Discussion
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8:55 pm - 9:15 pm |
General Discussion
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9:15 pm - 9:30 pm |
Closing Remarks
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Friday
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7:30 am - 8:30 am |
Breakfast
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9:00 am |
Departure
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