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
Balancing Selectivity and Pharmacokinetics Delivers Clinical Candidates for Challenging Targets
Discussion Leader: Callie Bryan (Janssen R&D, United States)
7:40 pm - 8:10 pm
Jack Terrett (Genentech, Inc., United States)
"Discovery of Clinical TRPA1 Antagonist GDC-6599: How Mechanistic Investigation of Pre-Clinical Toxicity led to Potential First-In-Class Therapy for Respiratory Disease"
8:10 pm - 8:20 pm
Discussion
8:20 pm - 8:50 pm
Benjamin Milgram (Scorpion Therapeutics, United States)
"Discovery of STX-721, a Potent and Mutant-Selective EGFR Exon 20 Inhibitor with a Potential Best-in-Class Profile"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
Nicolas Soldermann (Novartis, Switzerland)
"Disrupting the YAP-TEAD Protein-Protein Interaction with Small Molecules – Discovery of Drug Candidate NVP-IAG933"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Lessons from the Development Frontier: Preclinical Leads and Winning Back-Ups
Discussion Leaders: Yue-Mei Zhang (Eli Lilly & Company, United States) and David Weinstein (Vividion Therapeutics, United States)
9:00 am - 9:30 am
Emily Peterson (Biogen, United States)
"The Discovery of Potent, Selective, and CNS-Penetrant IRAK4 Inhibitors for the Treatment of Neuroinflammatory Disease"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Ana Gonzalez (Gilead Sciences, United States)
"Structure-based Discovery of GS-9770: The Road to a Once-Daily, Unboosted, HIV Protease Inhibitor"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
David Wustrow (RAPT Therapeutics, United States)
"Discovery of Potent, Selective and Orally Bioavailable CCR4 Antagonists that Target Key Drivers of the Immune System"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Xueqing Wang (Abbvie Inc., United States)
"Identification of ABBV-2851, a CFTR Corrector, as a Backup to ABBV-2222"
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: Emily Peterson (Biogen, United States) and David Marcoux (TRIANA Biomedicines, United States)
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
First in Class Mechanisms: From Bench to Clinic
Discussion Leader: Amy Hart (Aleksia Therapeutics, United States)
7:30 pm - 8:00 pm
Roland Burli (Cerevance, United Kingdom)
"Discovery of CVN293, a Blocker of Potassium Two Pore Domain Channel Subfamily K Member 13 (KCNK13 aka THIK1), a Novel Microglial Target for Neurodegenerative Diseases"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Jim Ding (Chinook Therapeutics, Canada)
"Discovery of CHK-336: A First-in-Class, Liver-Targeted, Small Molecule Inhibitor of Lactate Dehydrogenase for The Treatment of Primary Hyperoxalurias"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Tim Jonckers (Janssen Pharmaceutica, Belgium)
"Acyl-Indole Derivatives as Potent Pan-Serotype Dengue Virus NS3-NS4B Interaction Inhibitors. Discovery of JNJ-1802"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Platform- and Technology-Based Approaches to Empower Drug Discovery
Discussion Leader: Julia Haas (Pfizer Boulder R&D, United States)
9:00 am - 9:30 am
Leela Dodda (Nimbus Therapeutics, United States)
"Rapid Identification of HPGD Inhibitors Using Physics-based Machine Learning Methods"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Bryce Allen (Differentiated Therapeutics, United States)
"Prospective Design of a Selective CDK2/CCNE1 Dual Degrader"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
Elena Koltun (Revolution Medicines, United States)
"Targeting KRASG12C and Beyond"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Brandon Turunen (GlaxoSmithKline, United States)
"Cytotoxicity Targeting Chimeras (CyTaCs) to Drug the Undruggable"
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
Covalent Approaches to Challenging Targets
Discussion Leader: Joachim Rudolph (Genentech, United States)
7:30 pm - 8:00 pm
Jonathan Wilson (Flare Therapeutics, United States)
"Discovery and Development of FX-909, a Covalent Inverse Agonist of PPARG"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Birgit Wilding (Boehringer Ingelheim, Austria)
"The Discovery of BI 1810631, a Selective HER2 Inhibitor for the Treatment of HER2 Exon 20 Insertion Driven Tumors"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Jason Green (Vividion Therapeutics, United States)
"Chemoproteomic Identification and Optimization of Covalent KEAP1 Inhibitors"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Breakthroughs
Discussion Leader: Meredeth McGowan (MOMA Therapeutics, United States)
9:00 am - 9:25 am
Joseph Young (Novartis, United States)
"Discovery of EDI048, a First-in-Class Oral Soft-Drug Cp PI(4)Ki for the Treatment of Pediatric Cryptosporidiosis"
9:25 am - 9:40 am
Discussion
9:40 am - 10:05 am
Norbert Schmees (Nuvisan ICB GmbH, Germany)
"Discovery of BAY 2965501, a Highly Selective DGK-zeta Inhibitor for Cancer Immuno-Therapy with First-In-Class Potential"
10:05 am - 10:20 am
Discussion
10:20 am - 10:45 am
Coffee Break
10:45 am - 10:55 am
Dalia Soueid (University of Michigan, United States)
"Cell-Based Assay Development Strategies for the Detection and Validation of Aberrant mRNA-Protein Interactions"
10:55 am - 11:00 am
Discussion
11:00 am - 11:10 am
Damian Young (Baylor College of Medicine, United States)
"Using Systematic Chemical Diversity for Biological Interrogation"
11:10 am - 11:15 am
Discussion
11:15 am - 11:40 am
Weiwen Ying (Ranok Therapeutics, United States)
"Application of a Chaperone Mediated Protein Degradation Platform to KRAS Therapeutics"
11:40 am - 11:55 am
Discussion
11:55 am - 12:20 pm
Christopher Bungard (Merck and Co.; Inc, United States)
"Leveraging a New PK Metric – Low Dose NaV 1.8 Channel Blockers for the Treatment of Pain"
12:20 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 Screening and Lead Generation
Discussion Leader: Thomas Durand-Reville (Dewpoint Therapeutics, United States)
7:30 pm - 8:00 pm
Katherine Partridge (Recursion Pharmaceuticals, United States)
"A Phenomics-Based Approach to Phenotypic Drug Discovery: The Discovery of REC-0163964 and an Introduction to Map-Based Inferential Search"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Zhe Nie (Schrodinger Inc, United States)
"In Silico Enabled Discovery of Potent, Selective and Brain-Penetrant DLK Inhibitors for the Treatment of Neurodegenerative Diseases"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Yuhua Huang (Merck, United States)
"A PCSK9 Vignette: from mRNA Display to Passively Permeable Macrocycles"
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: H. Rachel Lagiakos (Schrödinger, United States)
9:00 am - 9:30 am
Beth Thomas (Storm Therapeutics, United Kingdom)
"Discovery of STC15, the First Molecule Specifically Targeting an RNA Methyltransferase Enzyme to Enter Clinical Development"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Brendan Crowley (Merck, United States)
"Positive Allosteric Modulators of the alpha7 nAChR for the Treatment of Cognitive Disorders: Invention of MK-4334"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
Barbara Czako (Nurix, United States)
"First Disclosure of NX-5948, an Oral Targeted Degrader of Bruton's Tyrosine Kinase (BTK) for the Treatment of B-Cell Malignancies and Autoimmune Disease"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Dean Brown (Jnana Therapeutics, United States)
"Discovery and Characterization of JNT-517, an Inhibitor of SLC6A19 for the Treatment of Phenylketonuria"
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: Activity-based Proteomics – Protein and Ligand Discovery on a Global Scale
Discussion Leader: Michael Ellis (Bristol Myers Squibb, United States)
7:30 pm - 8:30 pm
Benjamin Cravatt (The Scripps Research Institute, United States)
"Activity-Based Proteomics – Protein and Ligand Discovery on a Global Scale"
8:30 pm - 9:00 pm
Discussion
9:00 pm - 9:20 pm
General Discussion
9:20 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure