Gordon Research Conferences
Meeting Details

Medicinal Chemistry (GRS)
Gordon Research Seminar

Understanding Key Concepts for Lead Optimization


August 6-7, 2016


Colby-Sawyer College
New London, NH


Michael P. Pollastri

Meeting Description

The Gordon Research Seminar on Medicinal Chemistry is a unique forum for graduate students, post-docs, and other scientists with comparable levels of experience and education to present and exchange new data and cutting edge ideas in modern drug discovery projects.

Topics will include discussion of concepts of lead-likeness and also on the impact of chemical structure on physicochemical properties, pharmacology, pharmacokinetic and toxicology outcomes. The application of cutting edge technologies to drug discovery programs will also be discussed. The focus of this meeting is to explore fundamental principles of contemporary medicinal chemistry coupled with poster presentations representing the various therapeutic areas and target classes of current interest in the biotech and pharmaceutical industries. The principles will be presented in a workshop format, allowing for close interaction between practicing medicinal chemists and participating attendees. Case studies of drug discovery projects will highlight successful approaches taken to deliver clinical candidates. Registration support will be available for participants; please contact the chair for details.

Related Meeting

This GRS was held in conjunction with the "Medicinal Chemistry" Gordon Research Conference (GRC). Refer to the associated GRC program page for more information.


Final Meeting Program

2:00 pm - 5:00 pmArrival and Check-in
3:30 pm - 3:45 pmIntroductory Comments by GRC Site Staff / Welcome by the GRS Conference Chair
3:45 pm - 5:45 pmUnderstanding Drug-Likeness and Medicinal Chemistry Strategies
Discussion Leader: Amy Dounay (Colorado College, USA)
3:45 pm - 3:55 pmIntroduction by Discussion Leader
3:55 pm - 4:25 pmThomas Simpson (Boehringer Ingelheim Pharmaceuticals, USA)
"What Makes a Good Lead?"
4:25 pm - 4:40 pmDiscussion
4:40 pm - 5:10 pmMark Tichenor (Janssen Research & Development LLC, USA)
"Strategies for Lead Optimization"
5:10 pm - 5:25 pmDiscussion
5:25 pm - 5:45 pmGeneral Discussion
6:00 pmDinner
7:30 pm - 9:30 pmAbsorption, Distribution, Metabolism, Excretion, and Toxicity
Discussion Leader: Srinivasa Karra (EMD Serono Research & Development Institute, USA)
7:30 pm - 7:40 pmIntroduction by Discussion Leader
7:40 pm - 8:10 pmKimberly Cameron (Pfizer, USA)
"Medicinal Chemistry Lead Optimization: The Use of In Vitro Assays to Solve ADME and Safety Issues"
8:10 pm - 8:25 pmDiscussion
8:25 pm - 8:55 pmChristopher Smith (COI Pharmaceuticals, USA)
"Addressing Issues Identified by Second-Tier ADMET Assays"
8:55 pm - 9:10 pmDiscussion
9:10 pm - 9:30 pmGeneral Discussion
9:45 pm - 11:00 pmPoster Session
7:30 am - 8:30 amBreakfast
9:00 am - 11:00 amTranslation into Animal Models
Discussion Leader: David Kummer (Janssen, Johnson & Johnson, USA)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:40 amMargaret Chu-Moyer (Amgen, USA)
"A Medicinal Chemist's Primer on Pharmacokinetics"
9:40 am - 9:55 amDiscussion
9:55 am - 10:25 amDavid Price (Pfizer Inc., USA)
"In Vivo Models and PKPD, First Principles"
10:25 am - 10:40 amDiscussion
10:40 am - 11:00 amGeneral Discussion
11:00 am - 12:30 pmPoster Session

Coffee will be served in the poster area from 11:00 am - 11:30 am
12:30 pmLunch
1:30 pm - 2:30 pmCase Studies in Medicinal Chemistry
Discussion Leader: Christoph Boss (Actelion Pharmaceuticals Ltd., Switzerland)
1:30 pm - 1:50 pmKim Huard (Pfizer, USA)
"Sodium-Coupled Citrate Transporter (NaCT or SLC13A5) Inhibitors for the Treatment of Metabolic Diseases"
1:50 pm - 1:55 pmDiscussion
1:55 pm - 2:15 pmPatrick Stoy (GlaxoSmithKline, USA)
"TRPV4 Antagonists: A Case Study in Managing Lipophilicity"
2:15 pm - 2:20 pmDiscussion
2:20 pm - 2:30 pmClosing Remarks
2:30 pm - 3:00 pmEvaluation Period
Fill in GRS Evaluation Forms
3:00 pmSeminar Concludes
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