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Medicinal Chemistry

Gordon Research Conference

Emerging Science to Enable Drug Discovery

August 6 - 11, 2023

Chair

Vice Chair

Colby-Sawyer College

541 Main Street

New London, New Hampshire, United States

Venue and Travel Information

Conference Description

The Medicinal Chemistry GRC is a premier, international scientific conference focused on advancing the frontiers of science through the presentation of cutting-edge and unpublished research, prioritizing time for discussion after each talk and fostering informal interactions among scientists of all career stages. The conference program includes a diverse range of speakers and discussion leaders from institutions and organizations worldwide, concentrating on the latest developments in the field. The conference is five days long and held in a remote location to increase the sense of camaraderie and create scientific communities, with lasting collaborations and friendships. In addition to premier talks, the conference has designated time for poster sessions from individuals of all career stages, and afternoon free time and communal meals allow for informal networking opportunities with leaders in the field.

The 2023 Medicinal Chemistry Gordon Research Conference will feature talks on the cutting edge of the discipline that include new innovations, technologies, and compounds that advance the science. Erin DiMauro of Merck is responsible for the scientific program; please see the planned topics and contact the Chairs if you would like to submit a talk proposal. A preliminary program of speakers will be posted in November 2022.

In addition to the various scientific sessions, the conference will culminate with a “Late-Breaking Topics” session organized by H. Rachel Lagiakos of Schrodinger. This session comprises late-breaking results on prioritized clinical candidates across therapeutic areas. Finally, the conference program will conclude on Thursday evening with the Keynote address organized by the Chair.

We strongly encourage attendees to submit poster presentations on any aspect of Medicinal Chemistry as the poster sessions are an essential outlet for thoughtful discussion and interaction among the conferees. This year, the poster sessions will be organized by Izzat Raheem of Merck.

The 2023 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed atmosphere offering a variety of social activities. Vice Chair-Elect Matt Volgraf of Septerna will organize social events for the week, including hikes of Mt. Kearsarge and Mt. Cardigan, cycling, frisbee golf, cruising Lake Sunapee, volleyball, softball, soccer, a golf scramble, and a charity fundraiser.

As we look forward to another amazing conference in 2023, on behalf of myself, the Vice Chair, and the Vice Chair-Elect, we welcome your application. This conference is typically full by early May. We encourage applications by April 1, 2023 and the submission of any poster abstracts by April 15, 2023 to facilitate the admissions process. We particularly encourage applications from those of diverse backgrounds and scientific perspectives.

Thank you for your interest in the Medicinal Chemistry GRC!

Mike Ellis

Bristol Myers Squibb

Chair, 2023 Medicinal Chemistry GRC

Related Meeting

This GRC will be held in conjunction with the "Medicinal Chemistry" Gordon Research Seminar (GRS). Those interested in attending both meetings must submit an application for the GRS in addition to an application for the GRC. Refer to the associated GRS program page for more information.

Conference Program

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:
7:40 pm - 8:10 pm	"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	"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	"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: and
9:00 am - 9:30 am	"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	"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	"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	"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: and
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:
7:30 pm - 8:00 pm	"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	"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	"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:
9:00 am - 9:30 am	"Rapid Identification of HPGD Inhibitors Using Physics-based Machine Learning Methods"
9:30 am - 9:45 am	Discussion
9:45 am - 10:15 am	"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	"Targeting KRASG12C and Beyond"
11:30 am - 11:45 am	Discussion
11:45 am - 12:15 pm	"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:
7:30 pm - 8:00 pm	"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	"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	"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:
9:00 am - 9:25 am	"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	"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	"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	"Using Systematic Chemical Diversity for Biological Interrogation"
11:10 am - 11:15 am	Discussion
11:15 am - 11:40 am	"Application of a Chaperone Mediated Protein Degradation Platform to KRAS Therapeutics"
11:40 am - 11:55 am	Discussion
11:55 am - 12:20 pm	"Leveraging a New PK Metric – Low Dose Na_V1.8 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:
7:30 pm - 8:00 pm	"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	"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	"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:
9:00 am - 9:30 am	"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	"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	"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	"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:
7:30 pm - 8:30 pm	"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

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