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Medicinal Chemistry

Gordon Research Conference

Innovations in Drug Discovery and Enabling Technologies

August 7 - 12, 2022

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Chair Cynthia A. Parrish

Vice Chair Michael Ellis

Contact Chairs

Colby-Sawyer College

541 Main Street

New London, NH, United States

Venue and Travel Information

Application Information

Applications for this meeting must be submitted by July 10, 2022. Please apply early, as some meetings become oversubscribed (full) before this deadline. If the meeting is oversubscribed, it will be stated here. Note: Applications for oversubscribed meetings will only be considered by the conference chair if more seats become available due to cancellations.

Conference Description

The 2022 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. Mike Ellis of Bristol Myers Squibb 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 December 2021.

In addition to the various scientific sessions, the conference will culminate with a “Late-Breaking Topics” session organized by Meredeth McGowan of MOMA Therapeutics. This session comprises late-breaking results on important clinical candidates across therapeutic areas. Finally, the conference will wrap up 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 Matt Volgraf of Genentech.

The 2022 Medicinal Chemistry GRC will continue a tradition of outstanding science presented in a relaxed atmosphere offering a variety of social activities. Vice-Chair Elect Erin DiMauro of Merck will organize social events for the week, including hikes of Mt. Kearsarge and Mt. Cardigan, a Philbrick-Cricenti bog walk, frisbee golf, volleyball, softball, soccer, a golf scramble, and a charity poker tournament.

As we look forward to another fantastic conference in 2022, 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 and the submission of any poster abstracts by April 15 to facilitate the admissions process. In particular, we encourage applications from those of diverse backgrounds and scientific perspectives.

Thank you for your interest in the Medicinal Chemistry GRC!

Cindy Parrish

GlaxoSmithKline

Chair, 2022 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 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, USA) and Julia Haas (Pfizer Boulder R&D, USA)
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"
8:10 pm - 8:15 pm	Discussion
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"
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, USA)
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"
9:30 am - 9:45 am	Discussion
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"
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, USA) "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, USA) "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: Jennifer Riggs (Bristol Myers Squibb, USA) and David Marcoux (Janssen Pharmaceuticals, USA)
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, USA)
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"
8:00 pm - 8:10 pm	Discussion
8:10 pm - 8:40 pm	Duane Burnett (Arkuda Therapeutics, USA) "Progranulin Enhancers for the Treatment of FTD-GRN"
8:40 pm - 8:50 pm	Discussion
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"
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, USA)
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	Rachel Grainger (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, USA) "Selective Catalytic Isomerization Reactions"
11:30 am - 11:45 am	Discussion
11:45 am - 12:15 pm	Michelle Hall (Eli Lilly, USA) "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 Modulators of Protein-Protein Interactions Discussion Leader: Alex Cortez (Bristol Myers Squibb, USA)
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"
8:00 pm - 8:10 pm	Discussion
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"
8:40 pm - 8:50 pm	Discussion
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"
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., USA)
9:00 am - 9:30 am	Iyassu Sebhat (Kallyope, USA) "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 Research Laboratories, USA) "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, USA) "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: Identifying the Drug-like Property Space for a New Class of Antibiotics"
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, USA)
7:30 pm - 8:00 pm	Matthew Mitcheltree (Merck & Co., Inc., USA) "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, USA) "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, USA) "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; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
9:00 am - 12:30 pm	Late-Breaking Topics: First Disclosures of Clinical Candidates Discussion Leader: Meredeth McGowan (MOMA Therapeutics, USA)
9:00 am - 9:30 am	Michael Graupe (Gilead Sciences Inc., USA) "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, USA) "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, USA) "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, USA) "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 Leader: Michael Ellis (Bristol-Myers Squibb, USA)
7:30 pm - 8:30 pm	Rosana Kapeller (ROME Therapeutics, USA) "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

Contributors

Conference Links

Conference History Medicinal Chemistry (GRS) Contribute Financially to This Conference

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Poster Information

Poster sessions are an integral part of the our conferences, and offer all conferees an opportunity to discuss their research.

Preparing your GRC poster

Diversity Funding

Financial assistance is available for qualified applicants through the GRC Carl Storm Underrepresented Minority Fellowship Program. This program provides a grant to underrepresented minority graduate students, postdocs, faculty and scientists to help fund their attendance at their first GRC meeting. Learn more.

Registration Fees

Conferee Single Room:

$950.00

Conferee Shared Room:

$900.00

Conferee Off-Site:

$750.00

Guest Single Room:

$760.00

Guest Shared Room:

$710.00

Guest Off-Site:

$560.00

Child 4-12 yrs Shared Room:

$355.00

Child 4-12 yrs Off-Site:

$280.00

Child Under 4 yrs Shared Room:

Free

Child Under 4 yrs Off-Site:

Free

Bus Arriving:

$50.00

Bus Departing:

$50.00

Additional Fee Info

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Medicinal Chemistry

Innovations in Drug Discovery and Enabling Technologies

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