Leaders in Pharmaceutical Business Intelligence (LPBI) Group

AbbVie

» Important Aspects of Fragment Screening Collection Design

Ashley Adams, Ph.D., Senior Scientist, Discovery Chemistry and Technology

» Comparison of Methods for Determination of Drug-Target Engagement in Live Cells

Aleksandra Baranczak, Ph.D., Senior Scientist, Discovery Chemistry and Technology

» Bruton’s Tyrosine Kinase (BTK) – Considerations for the Design and Profiling of Irreversible Covalent Inhibitors

Michael Friedman, Ph.D., Principal Scientist

» Targeting the PRC2 Complex through a Novel Protein-Protein Interaction Inhibitor of EED

Chaohong Sun, Ph.D., Senior Principal Research Scientist; Head, Fragment Based Drug Discovery, and Global Protein Sciences-Small Molecule

» Fragment-Based, Structure-Enabled Approach to the Discovery of Novel Inhibitors of the BET Family of Proteins: ABBV-075 and Others

Le Wang, Ph.D., Principal Research Scientist, Oncology Discovery, Chemistry

» Kinetic and Thermodynamic Profiling in Drug Discovery: Are We There Yet?

Ying Wang, Ph.D., Principal Research Scientist, Department of Chemistry and Technology

AstraZeneca

» Clinical Candidate AZD5153 Is a Novel Bivalent Inhibitor of BET Bromodomains

Huawei (Ray) Chen, Ph.D., Principal Scientist II, Oncology iMed

» Targeting Inducible Nitric Oxide Synthase (iNOS)

Fredrik Edfeldt, Ph.D., Associate Principal Scientist, Biophysics, Discovery Sciences

Biogen

» Germinal-Center Kinase-Like Kinase Co-Crystal Structure Reveals a Swapped Activation Loop and C-Terminal Extension

Laura Silvian, Ph.D., Principal Scientist and Head, Physical Biochemistry

Boehringer Ingelheim

» Discovery of Novel Spiro[3H-Indole-3,2′-Pyrrolidin]-2(1H)-One Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2–p53 Interaction

Andreas Gollner, Ph.D., Laboratory Head, Medicinal Chemistry

» Small Molecule Modulators of RORγ

Robert Hughes, Ph.D., Senior Associate Director, Small Molecule Discovery Research

» LTA4H Case Study: Parallel Core and Substituent FBDD to Clinical Compounds

Matthew R. Netherton, Ph.D., Senior Principal Scientist, Small Molecule Discovery Research, Medicinal Chemistry

Bristol-Myers Squibb

» Applications of the Thermal Shift Assay: More than Melts the Eye

Mary Harner, Ph.D., Research Investigator II, Leads Discovery & Optimization

» Compound Mechanism of Action: “The Known Unknown” and How That Affects Lead Optimization

Brian J. Murphy, Ph.D., Senior Principal Scientist, Fibrosis Drug Discovery, Disease Sciences and Biologics, R&D

» A Twisted Road to the Discovery of BMS-986142: Using Locked Atropisomers to Drive Potency in a Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK)

Joseph Tino, Ph.D., Senior Principal Scientist, Immunoscience Discovery Chemistry

» A First-in-Class Allosteric Inhibitor of TYK2 as a Potential Treatment for Inflammatory Autoimmune Diseases

Stephen Wrobleski, Principal Investigator, Immunoscience Chemistry

Celgene

» Ligand-directed Degradation of GSPT1 by a Novel Cereblon Modulator

Philip Chamberlain, Ph.D., Principal Scientist, Biochemistry and Structural Biology

» Targeting Inducible Nitric Oxide Synthase (iNOS)

Fredrik Edfeldt, Ph.D., Associate Principal Scientist, Biophysics, Discovery Sciences

» Ozanimod: An S1P1,5R Modulator that Targets Lymphocyte Trafficking in Autoimmune and Inflammatory Disease

Kristin Taylor Meadows, Ph.D., Scientist III, Biology

Eli Lilly & Co

» Inhibiting Interaction of IL17A and Its Receptor

Sepideh Afshar, Ph.D., Principal Research Scientist, Department of Protein Engineering

EMD Serono

» Structure-Based Optimization of a Potent, Selective and CNS penetrable p70S6K/AKT Inhibitor M2698 for the Treatment of Tumors with PAM Pathway Genomic Alterations

Igor Mochalkin, Ph.D., Associate Director, Medicinal Chemistry & Lead Optimization

Genentech

» The Development of Orally Bioavailable Antagonists of Inhibitor of Apoptosis Proteins (IAPs) for the Treatment of Cancer

Lewis Gazzard Ph.D., Senior Scientist, Discovery Chemistry

» Small Molecule Kinase Inhibitors for Brain Cancer: Limitations, Challenges and Opportunities

Timothy P. Heffron, Ph.D., Senior Scientist, Discovery Chemistry

GlaxoSmithKline

» Affinity Selection Mass Spectrometry for Target Validation and Hit Triage

Jeff Messer, Director, NCE Molecular Discovery

» Using Encoded Library Technologies to Discover Small Molecule Inhibitors of RSV Protein Complexes

Christopher Phelps, Ph.D., Manager, Drug Design & Selection Boston, RD Platform Technology & Science

Janssen

» Determination of a Focused Mini-Kinase Panel for Early Identification of Selective Kinase Inhibitors

Scott Bembenek, Ph.D., Principal Scientist, Computer-Aided Drug Discovery

» Discovery of a Series of Thiazole RORγt Inverse Agonists

Steven Goldberg, Ph.D., Associate Scientific Director, Immunology

» Combining Biophysical Techniques for Difficult Targets: Case Vignettes

Kevin Lumb, Ph.D., Scientific Director, Discovery Sciences

Merck & Co

» GPCR Structural Biology for Drug Discovery: Through the Protein Science Lens

Sujata Sharma, Ph.D., Director, Screening and Protein Science

Novartis

» Design of Technology-Compatible Cyclic Peptide Scaffolds with Oral Bioavailability

Lauren Monovich, Ph.D., Senior Investigator, Global Discovery Chemistry

» Natural Products: Promising Starting Points for Fragment-Based Screening

Tim Schuhmann, Ph.D., Investigator III, Natural Products Unit

» Leniolisib (CDZ173) – The Discovery of a New Generation of Selective PI3Kδ Inhibitors

Nicolas Soldermann, Ph.D., Senior Investigator and Group Leader, Global Discovery Chemistry

Pfizer

» Inhibition of Autoimmune Pathways with Dual Inhibition of JAK1 and TYK2

Brian Gerstenberger, Ph.D., Principal Scientist, Medicinal Chemistry

» Advancing a Clinical Candidate Targeting IRAK4 from a Fragment Lead

Seungil Han, Ph.D., Associate Research Fellow, Structural Biology & Biophysics, WorldWide Research & Development

» Allosteric Activators of AMP-Activated Protein Kinase for the Treatment of Diabetic Nephropathy

Ravi G. Kurumbail, Ph.D., Research Fellow and Structural Biology Laboratory Head

» Macrocyclic Secondary Structure: Permeability and Chemical Biology

Spiros Liras, Ph.D., Vice President, Head, Cardiovascular Metabolism, RDRU and Discovery Network

» Discovery and Synthesis of the Macrocyclic EML4-ALK Inhibitor, Lorlatinib (PF-06463922)

Paul Richardson, Ph.D., Director, Process and Analytical Technologies, Oncology Medicinal Chemistry

» CASE STUDY: Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype Distinct Screening Hits

Mark E. Schnute, Ph.D., Medicine Design

Takeda

» FBDD: Part of an Integrated Drug Discovery Platform

Derek Cole, Ph.D., Director, Medicinal Chemistry

» Discovery of NF-kappa-B-Inducing Kinase (NIK) Inhibitors

Walter Keung, Ph.D., Senior Scientist, Medicinal Chemistry

» Biophysical Characterization of GPCRs: SPR and Other Techniques

Phillip Schwartz, Ph.D., Senior Scientist, Biophysical Chemistry

» Fragments and SPR for GPCRs

Shuo Wang, Ph.D., Principal Scientist, Biophysical Chemistry

» Structure-Based Design, Synthesis, and Dermal Application of Novel Tyrosine Kinase 2 (TYK2) Inhibitors

Takatoshi Yogo, Ph.D., Principal Scientist, Research, Immunology Unit

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Event-At-A-Glance

April 24-25

April 25-26

April 27

Inflammation Inhibitors

Kinase Inhibitor Chemistry

Biophysical Approaches

Protein-Protein Interactions, Part 1

Protein-Protein Interactions, Part 2

Small Molecules for Cancer Immunotherapy

GPCR-Targeted Drug Design

Fragment-Based Drug Discovery

Blood-Brain Penetrant Inhibitors

Macrocyclics & Constrained Peptides