Gordon Research Conferences
Meeting Details

Medicinal Chemistry (GRS)
Gordon Research Seminar

Lead Optimization Strategies for Medicinal Chemists


August 5-6, 2017


Colby-Sawyer College
New London, NH


Benjamin A. Pratt

Meeting Description

The Gordon Research Seminar on Medicinal Chemistry is a unique forum for graduate students, post-docs, and other early career scientists with comparable levels of experience and education to learn from experienced medicinal chemists, present and exchange new data and cutting edge ideas.

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.


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 pmThe Role of the Medicinal Chemist in Drug Discovery
Discussion Leader: Amy Dounay (Colorado College, USA)
3:45 pm - 3:55 pmIntroduction by Discussion Leader
3:55 pm - 4:25 pmChristopher Smith (COI Pharmaceuticals, USA)
"Introduction to Medicinal Chemistry"
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 pmOptimizing for ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity)
Discussion Leader: Mark Mitton-Fry (Ohio State University, USA)
7:30 pm - 7:40 pmIntroduction by Discussion Leader
7:40 pm - 8:10 pmDeidre Johns (Oregon State University, USA)
"Principles of ADMET - Part 1"
8:10 pm - 8:25 pmDiscussion
8:25 pm - 8:55 pmGraeme Freestone (Dart NeuroScience, USA)
"Principles of ADMET - Part 2"
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 amAnimal Models for Safety and Efficacy
Discussion Leader: Dustin Mergott (Eli Lilly, USA)
9:00 am - 9:10 amIntroduction by Discussion Leader
9:10 am - 9:40 amMichael Ellis (Merck Research Laboratories, USA)
9:40 am - 9:55 amDiscussion
9:55 am - 10:25 amTom Simpson (West Chester University, USA)
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 Drug Discovery
Discussion Leader: Amy Ripka (WuXi AppTec, USA)
1:30 pm - 1:55 pmKatherine Lee (Pfizer, USA)
"Lead Generation Strategies for IRAK4"
1:55 pm - 2:00 pmDiscussion
2:00 pm - 2:25 pmErin DiMauro (Merck & Co., USA)
"Discovery of High Quality TNKS Inhibitors via Multidimensional Lead Generation and Optimization"
2:25 pm - 2:30 pmDiscussion
2:30 pm - 3:00 pmEvaluation Period
Fill in GRS Evaluation Forms
3:00 pmSeminar Concludes
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