Archived: 14th Winter Conference
on Medicinal & Bioorganic Chemistry

January 27th - 31st 2019

Steamboat Springs Resort, Colorado


Sunday, January 27th 2019

Drug Hunting

Program Chair: Dr Daniel Flynn, Deciphera Pharmaceuticals

Dr Petr Vachal Merck

The Invention of MK-8262, a CETP Inhibitor Backup to Anacetrapib (with best in class properties)

Dr Kevin Freeman-Cook Pfizer

Cell Cycle Intervention Beyond Palbociclib; Preclinical Discovery of a CDK2/4/6 Inhibitor

Dr Josh Bilenker LOXO (Drug Hunter Award)

TRK Inhibitor LOXO-101 and back up LOXO-195

Networking Session

Welcome Reception

Monday, January 28th 2019


Program Chair: Dr Wes Trotter, Merck

Dr Jared Cumming Merck

Novel STING Agonists for Immuno-oncology

Dr Ashvin Gavai BMS

Discovery of BMS-986158, an Oral BET Inhibitor

Dr Cynthia Parrish GlaxoSmithKline

Targeting the Adenosine Pathway with Non-Nucleoside Inhibitors of CD73

Dr Brendan Parr Genentech

Design of Selective, Heme-binding Inhibitors of Tryptophan-2,3-dioxygenase (TDO)

Structural and in-Silico Chemistry

Program Chair: Dr Georgia McGaughey, Vertex

Dr Georgia McGaughey Vertex

Giving Med Chemists the Comp Chem Tools for What They Want and What They Need

Dr Yuan Wang Novartis

Computational Methods Help Find Chemical Matter to Uncover Novel Biology

Dr Meihua Tu Pfizer

The Role of Water Molecule in Ketohexokinase Inhibitor Design

Dr Ed Sherer Merck

Impact of Computational Chemistry Post Candidate Selection and Translating Lessons Learned back into Discovery

Tuesday, January 29th 2019

Chemical Biology for Drug Discovery

Program Chair: Dr Paola Castaldi, AstraZeneca

Professor Daniel Nomura Berkeley

Reimagining Druggability using Chemoproteomic Platforms

Professor Christina Woo Harvard

Mapping Binding Site Hotspots in the Global Proteome by Photo-affinity Labeling Mass Spectrometry

Dr Paola Castaldi AstraZeneca

Chemical Biology to provide insight into Small Molecule Targeting of BCL6

Dr Andy Phillips C4 Therapeutics

Targeted Protein Degradation

Potential New Therapies for the Treatment of Chronic Pain

Program Chair: Dr Sarah Skerratt, Vertex

Dr Sarah Skerratt Vertex

Overview of Current Therapies for the Treatment of Pain

Dr Mark Layton Merck

Breathe Easy: Mechanistic Insights Enable a Path Forward for Highly Selective Nav1.7 Inhibitors

Professor Laura Bohn Scripps

Harnessing Opioid Receptor Signaling to Improve Pain Therapeutics

Dr Brendan Crowley Merck

Discovery And Optimization Of A Novel CGRP Receptor Antagonist Chemotype For The Treatment of Migraine

Dr Emilia Väisänen Orion

TRPA1: A Pain Target or a Painful Target?

Dr Steven McKerrall Genentech

Structure-Based Drug Discovery in the Search for Nav1.7 Inhibitors

Wednesday, January 30th 2019

Recent Advances in Targeting Autophagy

Program Chair: Professor Jay Debnath (UCSF)

Professor Jay Debnath UCSF

Complexities of Targeting Autophagy to Treat Human Disease

Professor Kevan Shokat UCSF

Targeting the Autophagy-Initiating Kinase ULK1

Professor Martin McMahon University of Utah

Combined Targeting of MAP Kinase Signalling and Autophagy for the Future Therapy of Cancers Driven by the RAS Pathway

Professors Ravi Amaravadi & Jeffrey Winkler University of Pennsylvania

Advances in Targeting Lysosomotrophic Agents

Advances in Synthesis and Medicinal Chemistry

Program Chair: Professor Darren Dixon, University of Oxford

Professor James Barrow Lieber Institute for Brain Development

Discovery and Evaluation of Non-Nitrocatechol COMT Inhibitors for Treatment of Psychiatric Conditions

Mr Scott Savage Bristol-Myer Squibb

Intrinsic Aminomethyl Pyridine Enables Regioselective C-H Arylation in the Synthesis of IKur Inhibitor, BMS-919373

Dr Vishal Verma Genentech

Development of Inhibitors of MsbA: From HTS to Gram-negative Wild-type Activity

Professor Michael Pollastri Northeastern University

Hit-to-lead Medicinal Chemistry Targeting Neglected Tropical Diseases

Dr Eva Prchalova John Hopkins University

Targeting of the Glutamine Antagonist DON (6-Diazo-5-oxo-L-norleucine) via Prodrug Approach

Dr Andrew Woodhead Astex Pharmaceuticals

The Role of Solution Conformation in Structure-Guided Fragment Optimization

Dr John Butler Amgen

Pyridyl Urea Sulfonamide Inhibitors of NaV1.7: Intramolecular Hydrogen Bonding Leads to Improved Properties and Exposure

Professor Darren Dixon University of Oxford

New Broad Scope Strategies for Amine Synthesis

Thursday, January 31st 2019

Photoredox Catalysis

Program Chair: Dr Dan DiRocco, Merck

Dr Dani Schultz Merck

Recent Advances in the Remote Functionalization of Aliphatic C-H Bonds via Decatungstate Photocatalysis

Dr Thomas Knauber Pfizer

Enablement of Photoredox Csp2-Csp3 Cross Coupling Reactions

Dr Kaid Harper Abbvie

Scaling Catalytic Photochemistry with Lasers

Professor Corey Stephenson University of Michigan

Photoredox Catalysis – An Enabling Platform for Discovery and Development

Professor Tomislav Rovis University of Columbia

Controlling Catalysis with Visible Light


Program Chair: Professor Michael Vannieuwenhze, Indiana University

5.00 - 6.00pm
Professor Phil S. Baran The Scripps Research Institute

Translational Chemistry

Networking Session

Poster Session & Pre-Dinner Drinks

Networking Session

Conference Dinner

Short course

Medicinal Chemistry Approaches to De-risking Toxicology Issues in Drug Discovery

Tuesday 29th January 2019: 12.00 – 4.00 pm
& Wednesday 30th January 2019: 12.00 – 4.00 pm

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