EFMC-ISMC 2022

XXVII EFMC International Symposium on Medicinal Chemistry

 Nice, France    September 4-8, 2022

Programme


13:30

Registration

AGORA HALL

16:00

Opening Ceremony

Dr Luc VAN HIJFTE
SYMERES, Nijmegen, The Netherlands
Prof. Rebecca DEPREZ-POULAIN
UNIVERSITY OF LILLE / INSTITUT PASTEUR OF LILLE, Lille, France
Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal

ATHENA AUDITORIUM

16:20

EFMC Fellows Ceremony

Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal
16:35

Opening Lecture - Patient Testimonial

Chair

Dr Tatjana ROSS
MERCK HEALTHCARE KGAA, Darmstadt, Germany
16:50

Musical Interlude

17:00

EFMC Awards Ceremony

Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal
17:20

NAUTA PHARMACOCHEMISTRY AWARD FOR MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY
AL001 - Pseudo Natural Products – Chemical Evolution of Natural Product Structure

Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany

Chairs

Prof. Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands
Dr Andele NAUTA
PROF. DR. W. TH NAUTA STICHTING, The Netherlands
18:05

GDCh - Klaus Grohe Prize Ceremony

Laudatio

Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany

Prize Ceremony

Dr Rolf ALBACH
GDCH & COVESTRO, Cologne, Germany
18:15

KLAUS GROHE PRIZE
PR001 - Discovery of a Druggable Copper-signaling Pathway that Drives Cell Plasticity and Inflammation

Dr Raphaël RODRIGUEZ
INSTITUT CURIE, Paris, France
19:00

Welcome Reception sponsored by WuXi AppTec

RHODES HALL

20:00

End of the Day

08:00

Registration

AGORA HALL

08:30

UCB EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
AL002 - Small Molecule Drugs and where to find them - Approaches to Hit Generation and Lead Optimisation

Prof. Mike WARING
NEWCASTLE UNIVERSITY, Newcastle upon Tyne, United Kingdom

ATHENA AUDITORIUM

Chair

Dr Adrian HALL
UCB BIOPHARMA SRL, Braine-l'Alleud, Belgium
09:15

PL001 - Boosting « Chance and Necessity » with Experience and Molecular Creativity

Prof. Benoit DEPREZ
INSTITUT PASTEUR DE LILLE, Lille, France

Chair

Dr Luc VAN HIJFTE
SYMERES, Nijmegen, The Netherlands
10:00

Exhibition & Coffee

RHODES HALL

10:30

Start of sessions

Session 1 'Chemical Biology'

Beyond PROTACS, Monovalent and Glues Degraders
Session 2 'Drug Discovery'

Renaissance of Natural-Product Inspired Drug Discovery in the 21st Century
Session 3 'Technologies'

Methods for Late-Stage Functionalization

Session 1 'Chemical Biology'

Beyond PROTACS, Monovalent and Glues Degraders
10:30
Session Chair
Dr Laura M. LUH
BAYER, Wuppertal, Germany
10:35
LE001 - Strategies to Discover Molecular Glue Degraders at Scale
Dr Cristina MAYOR-RUIZ
IRB BARCELONA, Barcelona, Spain
11:15
LE002 - Haven't Got a Glue: Protein Surface Variation for the Design of Molecular Glue Degraders
Dr Nicolas THOMÄ
FRIEDRICH MIESCHER INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland
11:35
LE003 - Antibody-Protac Conjugates: an Approach for Targeted Selective BRD4 Degradation in HER2+ Phenotypes
Dr Maria MANEIRO
UNIVERSIDADE DE SANTIAGO DE COMPOSTELA, Santiago de Compostela, Spain
11:55
LE004 - Discovery And Profiling of AZ'6421: an Oral ERa-Protac with an in vitro-in vivo Disconnect
Dr Thomas HAYHOW
ASTRAZENECA, Cambridge, United Kingdom
RHODES12 AUDITORIUM
Session 2 'Drug Discovery'

Renaissance of Natural-Product Inspired Drug Discovery in the 21st Century
10:30
Session Chair
Dr Boris VAUZEILLES
INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES, Gif-sur-Yvette, France
10:35
LE005 - Big Data Analyses for the Discovery of Lead Structures from Nature
Prof. Judith ROLLINGER
UNIVERSITY OF VIENNA, Vienna, Austria
11:15
LE006 - Design of Naturally Inspired Anti-Cancer Compounds that Modulate Cholesterol Homeostasis
Dr Fanny ROUSSI
ICSN - CNRS, Gif sur Yvette, France
11:35
LE007 - Reduce to the Max: Functionally Optimized Natural Products via Chemical Synthesis
Prof. Karl GADEMANN
UNIVERSITY OF ZÜRICH, Zürich, Switzerland
11:55
LE008 - Tuning the Reactivity of the Natural Product Andrographolide: Towards Targeted Covalent Inhibitors for the Treatment of Inflammation
Prof. Christina CHAI
NATIONAL UNIVERSITY OF SINGAPORE, Singapore, Singapore
ATHENA AUDITORIUM
Session 3 'Technologies'

Methods for Late-Stage Functionalization

10:30
Prof. Tobias RITTER
MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany
10:35
LE009 - New Synthetic Chemistry to Probe the Biology of Modified Nucleic Acids
Prof. Matthew GAUNT
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
11:15
LE010 - Tritiation of Pharmaceuticals Via Late Stage C-H Functionalization
Dr Dieter MURI
ROCHE · PHARMA RESEARCH AND EARLY DEVELOPMENT (PRED), Basel, Switzerland
11:35
LE011 - Late-Stage Functionalizations
Prof. Tobias RITTER
MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany
11:55
LE012 - Chemical Modification of Wild-type Proteins
Dr Bauke ALBADA
WUR, Wageningen, The Netherlands
HERMES AUDITORIUM
12:15

Exhibition & Lunch

RHODES HALL

12:15

Schrödinger workshop
Digital Chemistry in Action: Combining physics-based modelling, AI/ML and experimental data in collaborative decision making

ROOM RISSO 8

12:15

Mestrelab Research workshop
Automate your analytical workflows with Mnova Gears: Relieve your teams from long and tedious tasks!

ROOM RISSO 6

13:15

Start of sessions

Flash Poster Session 1
FP01 to FP10
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

RHODES12 AUDITORIUM
Flash Poster Session 2
FP11 to FP20
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

ATHENA AUDITORIUM
Flash Poster Session 3
FP21 to FP30
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

HERMES AUDITORIUM
Flash Poster Session 1
FP01 to FP10
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

RHODES12 AUDITORIUM
RHODES12 AUDITORIUM
Flash Poster Session 2
FP11 to FP20
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

ATHENA AUDITORIUM
ATHENA AUDITORIUM
Flash Poster Session 3
FP21 to FP30
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

HERMES AUDITORIUM
HERMES AUDITORIUM
13:45

Start of sessions

Session 4 'Chemical Biology'

Targeting Epigenetic Modifications in Cancer Therapy / ICBS Session
Session 5 'Drug Discovery'

Drugging the Undruggable : Targeting Transcription Factors / ACSMEDI Session
Session 6 'Technologies'

Hit Discovery with DNA-Encoded Libraries

Session 4 'Chemical Biology'

Targeting Epigenetic Modifications in Cancer Therapy / ICBS Session
13:45
Session Chair
Prof. Zaneta NIKOLOVSKA-COLESKA
UNIVERSITY OF MICHIGAN, Ann Arbor, United States
13:50
LE013 - Disrupting hDot1L and MLL Oncofusion Protein Interactions as a Novel Therapeutic Strategy
Prof. Zaneta NIKOLOVSKA-COLESKA
UNIVERSITY OF MICHIGAN, Ann Arbor, United States
14:30
LE014 - New Opportunities for Studying the Function of the Nucleosome Remodeling Factor, NURF, Through Inhibition and Degradation
Prof. William POMERANTZ
UNIVERSITY OF MINNESOTA, Minneapolis, United States
14:50
LE015 - New Generation of EZH2 Inhibitors for Cancer Therapy: A Computer-Aided Drug Design Approach in Epigenetics
Dr Filipa RAMILO-GOMES
UNIVERSITY OF LISBON, Lisboa, Portugal
15:10
EFMC-YMCS Prize 2021
LE016 - A Mating Mechanism to Generate Diversity for the Darwinian Selection of DNA-encoded Synthetic Molecules
Mr Lluc FARRERA SOLER
UNIVERSITY OF GENEVA, Geneva, Switzerland
RHODES12 AUDITORIUM
Session 5 'Drug Discovery'

Drugging the Undruggable : Targeting Transcription Factors / ACSMEDI Session
13:45
Session Chair
Dr Anthony ROMERO
ORIC PHARMACEUTICALS, South San Francisco, United States
13:50
LE017 - Chemical Probe Discovery for Recalcitrant Targets Virtual Presentation
Prof. Angela KOEHLER
MIT KOCH INSTITUTE FOR INTEGRATIVE CANCER RESEARCH, Cambridge, United States
14:30
LE018 - Transcription Factors as Drug-Discovery Targets
Prof. Fraydoon RASTINEJAD
UNIVERSITY OF OXFORD, Oxford, United Kingdom
14:50
LE019 - Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9/Cyclin T1 for MYC-Dependent Cancers
Dr David FREEMAN
KRONOS BIO, INC. , Massachussetts, United States
15:10
LE020 - Inhibiting the MYC Oncogene through Cell Active Max-E47 (ME-47)
Dr Amy BITTNER MCCRACKEN
MSD, New Jersey, United States
ATHENA AUDITORIUM
Session 6 'Technologies'

Hit Discovery with DNA-Encoded Libraries

13:45
Session Chair
Dr Andreas BRUNSCHWEIGER
TU DORTMUND, Dortmund, Germany
13:50
LE021 - Innovating DNA-encoded Chemical Library Technology for Better Ligand Discovery
Dr Jörg SCHEUERMANN
ETH ZURICH, Zürich, Switzerland
14:30
LE022 - A DNA Barcode with Enhanced Chemical Stability for DNA-encoded Library Design
Dr Andreas BRUNSCHWEIGER
TU DORTMUND, Dortmund, Germany
14:50
LE023 - Exploiting DNA-encoded Library Technology for the Discovery of Novel Antibody Recruiting Molecules Against LOX-1
Ms Katherine MACFARLANE
UNIVERSITY OF STRATHCLYDE, London, United Kingdom
15:10
LE024 - Photoactivated Covalent Capture of DNA-encoded Fragments to Identify Ligands for Challenging Targets
Prof. Roderick HUBBARD
VERNALIS, Cambridge, United Kingdom
HERMES AUDITORIUM
15:30

Exhibition & Coffee

RHODES HALL

16:00

Start of sessions

SCT (Société de Chimie thérapeutique) Prize Session
SCT (Société de Chimie thérapeutique) Prize Session
16:00
Ceremony for the 2022 Galapagos Award for Drug Discovery Chemistry (in partnership with Société de Chimie thérapeutique)
Chairs
Prof. Rebecca DEPREZ-POULAIN
UNIVERSITY OF LILLE / INSTITUT PASTEUR OF LILLE, Lille, France
Dr Alexis DENIS
GALAPAGOS, Ile de France, France
16:10
GALAPAGOS AWARD LECTURE (Award-winning Team: Bioversys/University of Lille/GSK)
LE025 - Rejuvenating Ethionamide for Treatment of Tuberculosis - TRICky, but Possible
Dr Modesto REMUINAN
GSK, Tres Cantos (Madrid), Spain
ATHENA AUDITORIUM
16:30

Start of sessions

Session 7
First Time Disclosures - Part 1
Session 7
First Time Disclosures - Part 1
16:30
Session Chair
Dr Pilar MANZANO-CHINCHON
GLAXOSMITHKLINE, Tres Cantos (Madrid), Spain
16:35
LE026 - First-time Disclosure of M1069, a Highly Selective Dual Inhibitor of Adenosine A2a/A2b Receptors With Improved Therapeutic Activity Compared to A2a Receptor Selective Antagonists
Dr Kai SCHIEMANN
MERCK HEALTHCARE KGAA, Darmstadt, Germany
17:05
LE027 - Discovery of BI 456906, a Novel Long-acting GCG/GLP-1 Receptor Dual Agonist for the Treatment of Patients With Obesity
Dr Peter HAEBEL
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach Riss, Germany
17:35
LE028 - Discovery of AZD5462, an Oral Agonist of the Relaxin Family Peptide Receptor 1 (RXFP1) for the Treatment of Cardiorenal Disease
Dr Kenneth GRANBERG
ASTRAZENECA, Mölndal, Sweden
ATHENA AUDITORIUM
18:05

Poster Session 1 & Networking

AGORA HALL

19:35

End of the Day

08:30

PROUS INSTITUTE - OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
AL003 - How PROTACs Work: Molecular Recognition and Design Principles

Prof. Alessio CIULLI
UNIVERSITY OF DUNDEE, Dundee, United Kingdom

ATHENA AUDITORIUM

08:30

Chair

Dr Josep Jr. PROUS
PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain
09:15

PL002 - The Shape and Modification of RNA in Health and Disease

Prof. Eric MISKA
UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom
09:15

Chair

Dr Maria DUCA
UNIVERSITY OF CÔTE D'AZUR, Nice, France
10:00

Exhibition & Coffee

RHODES HALL

10:30

Start of sessions

Session 8 'Chemical Biology'

Addressing Cooperative Ligand Binding in Drug Discovery / EUCHEMS Session
Session 9 'Drug Discovery'

Time to Act Against Antimicrobial Resistance

Session 10 'Technologies'

New Screening Technologies : Affinity Selection - Mass Spectrometry
Session 8 'Chemical Biology'

Addressing Cooperative Ligand Binding in Drug Discovery / EUCHEMS Session
10:30
Session Chair
Prof. Luc BRUNSVELD
EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands
10:35
LE029 - Fragment-Based Approaches to Stabilize Protein-Protein Interactions
Prof. Michelle ARKIN
UNIVERSITY OF CALIFORNIA, San Francisco, United States
11:15
LE030 - Development of Bisubstrate Inhibitors to Tackle Epigenetics
Dr Paola B. ARIMONDO
INSTITUT PASTEUR - CNRS, Paris, France
11:35
LE031 - Identification and Structure-activity Relationship Profiling of Positive Allosteric Modulators Targeting Muscarinic Acetylcholine Receptors
Dr Manuela JORG
MONASH UNIVERSITY, Parkville, Australia
11:55
LE032 - Molecular Glues for the 14-3-3 Interactome
Dr Richard DOVESTON
UNIVERSITY OF LEICESTER, Leicester, United Kingdom
RHODES12 AUDITORIUM
Session 9 'Drug Discovery'

Time to Act Against Antimicrobial Resistance

10:30
Session Chair
Prof. Maria-Jesus PÉREZ-PÉREZ
INSTITUTO DE QUÍMICA MÉDICA, Madrid, Spain
10:35
LE033 - The Global Antibiotic R&D Partnership: Helping to Advance the Discovery & Development of New Treatments for Bacterial Infections
Dr Benjamin BLASCO
THE GLOBAL ANTIBIOTIC RESEARCH & DEVELOPMENT PARTNERSHIP (GARDP) , Geneva, Switzerland
11:15
LE034 - Novel Tetrazole Inhibitor of Mycobacterium Tuberculosis Tryptophan Synthase
Dr Lourdes ENCINAS
GLAXOSMITHKLINE, Madrid, Spain
11:35
LE035 - Discovery and Preclinical Development of ANT3310, a Broad-Spectrum β-Lactamase Inhibitor which Potentiates Meropenem Against Carbapenem-Resistant Bacteria
Dr David DAVIES
ANTABIO SAS, Labège, France
11:55
LE036 - Discovery of Pseudomonas Aeruginosa Elastase LasB Inhibitors by in Situ Click Chemistry
Dr Virgyl CAMBERLEIN
HIPS - HELMHOLTZ-INSTITUT FÜR PHARMAZEUTISCHE FORSCHUNG SAARLAND, Saarbrücken, Germany
ATHENA AUDITORIUM
Session 10 'Technologies'

New Screening Technologies : Affinity Selection - Mass Spectrometry
10:30
Session Chair
Dr Didier ROCHE
EDELRIS, Lyon, France
10:35
LE037 - Adapting the Affinity MS Technology to GPCR Ligand Discovery Virtual Presentation
Prof. Wenqing SHUI
SHANGHAITECH UNIVERSITY, Shanghai, China
11:15
LE038 - EDELRIS Keymical Space™ and GPCR : Identification of Allosteric Binders by AS-MS
Dr Renaud PRUDENT
EDELRIS, Lyon, France
11:35
LE039 - High Throughput Affinity Screening for Rapid Hit Discovery and Prosecuting Intractable Targets
Dr Jarrod WALSH
ASTRAZENECA, Macclesfield, United Kingdom
11:55
LE040 - Accelerating Drug Discovery with the Integration of Affinity Selection Mass Spectrometry (ALIS)
Dr Bryan CHOI
RELAY THERAPEUTICS, Cambridge, United States
HERMES AUDITORIUM
12:15

Exhibition & Lunch

RHODES HALL

12:15

WuXi AppTec workshop
Introduction to Self-Service DNA-Encoded libraries (DELs)

ROOM RISSO 6

12:15

Chemical Computing Group workshop
De Novo Design of Novel Compounds to Meet Multiple Property Constraints

ROOM RISSO 8

13:15

Start of sessions

Flash Poster Session 4
FP31 to FP40
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

RHODES12 AUDITORIUM
Flash Poster Session 5
FP41 to FP50
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

ATHENA AUDITORIUM
Flash Poster Session 6
FP51 to FP60
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

HERMES AUDITORIUM
Flash Poster Session 4
FP31 to FP40
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

RHODES12 AUDITORIUM
RHODES12 AUDITORIUM
Flash Poster Session 5
FP41 to FP50
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

ATHENA AUDITORIUM
ATHENA AUDITORIUM
Flash Poster Session 6
FP51 to FP60
Opportunity for 10 young scientists to present a summary of their poster

Discover the presenters here

HERMES AUDITORIUM
HERMES AUDITORIUM
13:45

Start of sessions

Session 11 'Chemical Biology'

Targeting Self-Associating Proteins & Biomolecular Condensates in Drug Discovery
Session 12 'Drug Discovery'

Covalent Drugs

Session 13 'Technologies'

Next Generation Medicinal Chemistry - an EFMC² Session
Session 11 'Chemical Biology'

Targeting Self-Associating Proteins & Biomolecular Condensates in Drug Discovery
13:45
Session Chair
Prof. Raphaël FREDERICK
UCLOUVAIN, Brussels-Woluwe, Belgium
13:50
LE041 - Targeting Protein-Protein Interactions of Receptor Complexes
Prof. Kristian STROMGAARD
UNIVERSITY OF COPENHAGEN, Copenhagen, Denmark
14:30
LE042 - Leveraging Biomolecular Condensates for Drug Discovery
Dr Marta FRIGOLE-VIVAS
DEWPOINT THERAPEUTICS GMBH, Dresden, Germany
14:50
LE043 - Polarity-sensitive Fluorescent Probes for Cellular Organelles: from Chemical to Genetically Encoded Targeting
Dr Andrey KLYMCHENKO
UNIVERSITÉ DE STRASBOURG, Illkirch, France
15:10
LE044 - Interrogating Lactate Dehydrogenases Oligomeric Interfaces Using (Stapled) Peptides And Small Molecules
Dr Léopold THABAULT
INSTITUTE OF CANCER RESEARCH, London, United Kingdom
RHODES12 AUDITORIUM
Session 12 'Drug Discovery'

Covalent Drugs

13:45
Session Chair
Dr Samir JEGHAM
SANOFI R&D, Montpellier, France
13:50
LE045 - Inhibiting KRAS: Strategies, Structures, and Lessons Learned in the Invention of Sotorasib
Dr Brian LANMAN
AMGEN, Thousand Oaks, CA, United States
14:30
LE046 - Covalent Fragment Approaches in Drug Discovery
Prof. György KESERU
HUNGARIAN ACADEMY OF SCIENCES, Budapest, Hungary
14:50
LE047 - Discovery of Covalent Protein Kinase Inhibitors Targeting Cysteines in the Hinge Region
Prof. Matthias GEHRINGER
UNIVERSITY OF TUEBINGEN, Tuebingen, Germany
15:10
LE048 - Discovery of Novel Covalent, EGFR WT Sparing, HER2 Selective Inhibitors for the Treatment of Her2 Exon 20 Insertion Driven Tumours
Dr Birgit WILDING
BOEHRINGER INGELHEIM, Vienna, Austria
ATHENA AUDITORIUM
Session 13 'Technologies'

Next Generation Medicinal Chemistry - an EFMC² Session
13:45
Session Chair
Dr Clara CHRIST
BAYER, Berlin, Germany
13:50
Introduction to EFMC²
Dr Richard LEWIS
NOVARTIS PHARMACEUTICALS, Basel, Switzerland
Dr Franz VON NUSSBAUM
NUVISAN, Berlin, Germany
14:00
LE049 - Driving Lead Optimization with BRADSHAW
Dr Darren GREEN
GSK, Stevenage, United Kingdom
14:30
LE050 - A Perspective on AI and Automation for the Medicinal Chemistry Lab Virtual Presentation
Prof. Connor COLEY
MIT, Cambridge, United States
14:50
LE051 - The Power and Pitfalls of Machine Learning in Early Stage Drug Discovery
Prof. Charlotte DEANE
UNIVERSITY OF OXFORD, Oxford, United Kingdom
15:10
LE052 - Using AI to Derive Valuable Insights from Drug Discovery Data
Dr Matthew SEGALL
OPTIBRIUM, Cambridge, United Kingdom
HERMES AUDITORIUM
15:30

Exhibition & Coffee

RHODES HALL

16:00

Start of sessions

Session 14

First Time Disclosures -Part 2
Session 14

First Time Disclosures -Part 2
16:00
Session Chair
Dr Leena OTSOMAA
ORION PHARMA, Espoo, Finland
16:05
LE053 - mPGES1 Inhibitors: First Time Disclosure of Clinical Candidate BI01029539 / GS-248
Dr Roland PFAU
BOEHRINGER INGELHEIM PHARMA GMBH&CO. KG, Ingelheim am Rhein, Germany
16:35
LE054 - First Disclosure of Cannabinoid Receptor Type 2 Agonist Rg7774 – An Innovative Oral Treatment for Diabetic Retinopathy
Dr Uwe GRETHER
F. HOFFMANN-LA ROCHE, Basel, Switzerland
17:05
LE055 - Discovery and Optimisation of Potent, Slow-dissociating Inhaled PI4KB Inhibitors
Dr Sophie BERTRAND
GSK, Stevenage, United Kingdom
17:35
LE103 - Discovery of a Selective Oral CCR4 Antagonist RPT193 for Treatment of Atopic Dermatitis and other Allergic Disorders
Dr Mikhail ZIBINSKY
RAPT THERAPEUTICS, INC., South San Francisco, United States
ATHENA AUDITORIUM
18:05

Poster Session 2 & Networking

AGORA HALL

19:35

End of the Day

08:30

PL003 - Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire

Prof. Sarah E. REISMAN
CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States

ATHENA AUDITORIUM

Chair

Prof. Karl-Heinz ALTMANN
ETH ZÜRICH, Zürich, Switzerland
09:15

EFMC Prizes for Young Medicinal Chemist or Chemical Biologist in Academia and in Industry
Ceremony & Lectures

Chair

Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal
09:20

EFMC PRIZE FOR A YOUNG MEDICINAL CHEMIST OR CHEMICAL BIOLOGIST IN INDUSTRY
PR002 - Chemical Biology Strategies Applied to Phenotypic Screening and Targeted Protein Degradation Discovery Programs

Dr Marie-Helene LARRAUFIE
ALMIRALL, Barcelona, Spain
09:40

EFMC PRIZE FOR A YOUNG MEDICINAL CHEMIST OR CHEMICAL BIOLOGIST IN ACADEMIA
PR003 - Chemical Biology Tools for Enlightening Drug Discovery

Prof. Olalla VÁZQUEZ
PHILIPPS-UNIVERSITÄT MARBURG, Marburg, Germany
10:00

Exhibition & Coffee

RHODES HALL

10:30

Start of sessions

Session 15 'Chemical Biology'

In vivo Chemistry to Study Biological Mechanisms and to Develop Innovative Tools for Therapy and Diagnosis
Session 16 'Drug Discovery'

Rising Horizons of Small Molecule Immunotherapies and Beyond

Session 17 'Technologies'

Innovative Synthetic Technologies for Drug Discovery

Session 15 'Chemical Biology'

In vivo Chemistry to Study Biological Mechanisms and to Develop Innovative Tools for Therapy and Diagnosis
10:30
Session Chair
Dr Frédéric TARAN
CEA/SACLAY, Gif-sur-Yvette, France
10:35
LE056 - Chemically-Triggered Payload Release in-vivo
Dr Marc ROBILLARD
TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands
11:15
LE057 - Tumor Activated Therapy
Prof. Sebastien PAPOT
SCT & UNIVERSITY OF POITIERS, Poitiers, France
11:35
LE058 - Investigating and Controlling mRNAs Via Chemo-enzymatic Modification
Prof. Andrea RENTMEISTER
UNIVERSITY OF MÜNSTER, Münster, Germany
11:55
LE059 - Fast Detection and Imaging of Hydrogen Peroxide with New Borinic Probes
Dr Boris VAUZEILLES
INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES, Gif-sur-Yvette, France
RHODES12 AUDITORIUM
Session 16 'Drug Discovery'

Rising Horizons of Small Molecule Immunotherapies and Beyond

10:30
Session Chair
Prof. Antonio MACCHIARULO
UNIVERSITY OF PERUGIA, Perugia, Italy
10:35
LE060 - Tipping the Balance: MALT1 Inhibitors with Paradoxical Effects on the Immune System
Dr Jean QUANCARD
NOVARTIS, Basel, Switzerland
11:15
LE061 - The discovery of the Clinical Candidate AZD0284, a Orally Bioavailable Inverse Agonist of RORG for the Treatment of Psoriasis
Dr Frank NARJES
ASTRAZENECA, Gothenburg, Sweden
11:35
LE062 - Macrolide Inspired Macrocycles as Effective Disruptors of the IL-17A/IL-17RA Interaction
Dr Dijana PESIC
SELVITA, Zagreb, Croatia
11:55
LE063 - NR2F6 Antagonists: in Vitro Pharmacology and Preclinical Data of a Potential Next Generation Immuno-oncology Therapy
Dr Francesco GRECO
TES PHARMA SRL, Perugia, Italy
ATHENA AUDITORIUM
Session 17 'Technologies'

Innovative Synthetic Technologies for Drug Discovery

10:30
Session Chair
Dr Cara BROCKLEHURST
NOVARTIS, Basel, Switzerland
10:35
LE064 - Molecular Vending Machines for the On-Demand Synthesis of Drug-Like Molecules
Prof. Jeffrey BODE
ETH ZURICH, Zürich, Switzerland
11:15
LE065 - Photocatalysis in Drug Discovery
Dr Lisa CANDISH
BAYER, Wuppertal, Germany
11:35
LE066 - Visible-light Photocatalysis: a Powerful Tool in the Pursuit of New Pharmaceuticals
Dr Giulia BERGONZINI
ASTRAZENECA, Gothenburg, Sweden
11:55
LE067 - Iridium-catalyzed C-H Activation Methods for Late-stage Functionalization of Pharmaceuticals
Dr Erik WEIS
ASTRAZENECA, Mölndal, Sweden
HERMES AUDITORIUM
12:15

Exhibition & Lunch

RHODES HALL

13:15

Start of sessions

Session 18

Highlights in Medicinal Chemistry
Part 1
Session 19 'Drug Discovery'

Targeting RNA by Small Molecules
Session Sponsored by Sanofi
Session 20 'Technologies'

AI in Drug Discovery / CPA Session

Session 18

Highlights in Medicinal Chemistry
Part 1
13:15
Session Chair
Dr Jan Willem THURING
JANSSEN PHARMACEUTICA NV, Beerse, Belgium
13:20
LE068 - Formulation Strategies for Compounds with Challenging Physicochemical Properties
Prof. Guy VAN DEN MOOTER
KULEUVEN, Leuven, Belgium
14:00
LE069 - Dual Inhibition of P53-MDM2/4 Interactions With Spiropyrazoline Oxindoles
Ms Elizabeth A. LOPES
UNIVERSITY OF LISBON, Lisboa, Portugal
14:20
LE070 - Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106
Dr Timo HEINRICH
MERCK, DARMSTADT, Germany
14:40
LE071 - A New Dual Mode of Action to Treat Pain - From Scratch to Pre-Clinical Candidate
Dr Anita WEGERT
SYMERES, Nijmegen, The Netherlands
RHODES12 AUDITORIUM
Session 19 'Drug Discovery'

Targeting RNA by Small Molecules
Session Sponsored by Sanofi
13:15
Session Chair
Dr Hasane RATNI
SKYHAWK THERAPEUTICS, Basel , Switzerland
13:20
LE072 - Enabling Technologies for Revealing Druggable Paths in RNA Biology
Dr Amanda GARNER
UNIVERSITY OF MICHIGAN, Ann Arbor, United States
14:00
LE073 - Targeting RNA with Small Molecules, A New Therapeutic Strategy
Dr Yann FORICHER
SANOFI, Vitry-sur-Seine, France
14:20
LE074 - Fundamental Basis for SMN2 Specific Splicing Correction by Small Molecules and Bulge Repair Mechanism
Dr Sébastien CAMPAGNE
INSERM BORDEAUX, BORDEAUX, France
14:40
LE075 - Bis-3-chloropiperidines Targeting TAR RNA as a Novel Strategy to Impair the HIV-1 Nucleocapsid Protein
Dr Alice SOSIC
UNIVERSITY OF PADOVA, Padova, Italy
ATHENA AUDITORIUM
Session 20 'Technologies'

AI in Drug Discovery / CPA Session

13:15
Session Chair
Prof. Mingyue ZHENG
SHANGHAI INSTITUTE OF MATERIA MEDICA, Shanghai, China
13:20
LE076 - Uncertainty Quantification: Considering the Reliability of Artificial Intelligence in Drug Design Virtual Presentation
Dr Dingyan WANG
SHANGHAI INSTITUTE OF MATERIA MEDICA, Shanghai, China
14:00
LE077 - Innovative Therapeutic Target Discovery based on OMIC Technology and Machine Learning Virtual Presentation
Prof. Feng ZHU
ZHEJIANG UNIVERSITY, Hangzhou, China
14:20
LE078 - Opportunity and Challenge of Artificial Intelligence (AI) in Drug Delivery Virtual Presentation
Prof. Defang OUYANG
MACAU UNIVERSITY, Macau, China
14:40
LE079 - In Silico Prediction of Brain Penetration - High Accuracy Achieved
Dr Herve GENESTE
ABBVIE, Ludwigshafen, Germany
HERMES AUDITORIUM
15:00

End of the Day

15:45

Excursions

20:00

Banquet

08:30

Start of sessions

Session 21 'Chemical Biology'

Mining the Phosphosignaling Networks

Session 22 'Drug Discovery'

New Treatments for Current and Future Pandemics
Session 23

Highlights in Medicinal Chemistry
Part 2
Session 21 'Chemical Biology'

Mining the Phosphosignaling Networks

08:30
Session Chair
Dr Nadia AHMAD
CHARLES RIVER LABORATORIES, Harlow, United Kingdom
08:35
LE080 - The Phosphatase Family: a Widely Neglected Target Space for Small-Molecule Drug Discovery
Dr Gerhard MÜLLER
ANAVO THERAPEUTICS, Leiden, The Netherlands
09:15
LE081 - A Novel Fragment-Based Ligand Design Tool : Application to Kinase Research
Prof. Pascal BONNET
UNIVERSITY OF ORLÉANS, Orléans, France
09:35
LE082 - Protein Phosphatase 2A, a Druggable Tumor Suppressor for Cancer Therapy
Prof. Jukka WESTERMARCK
UNIVERSITY OF TURKU, Turku, Finland
09:55
LE083 - Mining the Leishmania Kinome
Dr Exequiel PORTA
DURHAM UNIVERSITY, Durham, United Kingdom
RHODES12 AUDITORIUM
Session 22 'Drug Discovery'

New Treatments for Current and Future Pandemics
08:30
Session Chair
Prof. Ana MARTINEZ
CSIC, Madrid, Spain
08:35
LE084 - Searching for Drugs against Pandemic Viruses
Dr Carmen GIL
CENTRO DE INVESTIGACIONES BIOLÓGICAS (CSIC), Madrid, Spain
09:15
LE085 - Addressing Current Challenges in Antiviral Therapies Against Emerging RNA Viruses
Dr Karine ALVAREZ
AIX-MARSEILLE UNIVERSITY, Marseille, France
09:35
LE086 - Embrace Complexity: in Silico Polypharmacological Profiling to Repurpose Medicines and Design New Drugs
Dr Andrea BECCARI
DOMPÉ PHARMA, L'Aquila, Italy
09:55
LE087 - Human Dihydroorotate Dehydrogenase Inhibitor MEDS443: a Magic Bullet Against Coronaviruses
Dr Stefano SAINAS
UNIVERSITY OF TORINO, Torino, Italy
ATHENA AUDITORIUM
Session 23

Highlights in Medicinal Chemistry
Part 2
08:30
Session Chair
Prof. Roberto DI SANTO
SAPIENZA UNIVERSITY OF ROME, Rome, Italy
08:35
IUPAC-RICHTER PRIZE 2022
PR004 - Drug Discovery in Academia: A Drug For Glioblastoma Multiforme
Prof. Michael E. JUNG
UCLA CHEMISTRY & BIOCHEMISTRY, Los Angeles, United States
09:15
LE088 - Discovery of Clinical Candidate CHF-6366: a Super-soft Heterobifunctional Muscarinic Antagonist and β2-adrenoceptor Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases
Dr Laura CARZANIGA
CHIESI FARMACEUTICI SPA, PARMA, Italy
09:35
LE089 - Discovery of JNJ-1245, a Novel and Potent Fluoroallylamide Mcl-1 Inhibitor for the Treatment of Hematologic Malignancies
Dr Soufyan JERHAOUI
JANSSEN PHARMACEUTICA NV, Beerse, Belgium
09:55
LE090 - Structure-Guided Design of Foldamer-Based Inhibitors of Protein-Protein Interactions
Dr Gilles GUICHARD
UNIVERSITY OF BORDEAUX, Pessac, France
HERMES AUDITORIUM
10:15

Exhibition & Coffee

RHODES HALL

10:45

Start of sessions

Session 24 'Chemical Biology'

Chemical Probes for Target Identification & Validation / EUFEPS Session
Session 25 'Drug Discovery'

Drug Discovery in Targeting Neurodegenerative Disorders / ACSMEDI Session
Session 26 'Technologies'

Radiochemistry / AFMC Session

Session 24 'Chemical Biology'

Chemical Probes for Target Identification & Validation / EUFEPS Session
10:45
Session Chair
Dr Joanna REDMOND
FRANCIS CRICK INSTITUTE, London, United Kingdom
10:50
LE091 - Chemical Probes and How to Find Them
Dr Alex PAUTSCH
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach, Germany
11:30
LE092 - De Novo Cyclic Peptides as Chemical Tools to Explore Epigenetic Regulation

Dr Louise WALPORT
THE FRANCIS CRICK INSTITUTE, London, United Kingdom
11:50
LE093 - Chemical Probes for Targets in Lipid Signalling
Prof. Eugen PROSCHAK
GOETHE UNIVERSITY OF FRANKFURT, Frankfurt/Main, Germany
12:10
LE094 - First Selective Nanomolar Inhibitors of ERAP2 for Modulation of the Antigen Presentation
Prof. Rebecca DEPREZ-POULAIN
UNIVERSITY OF LILLE / INSTITUT PASTEUR OF LILLE, Lille, France
RHODES12 AUDITORIUM
Session 25 'Drug Discovery'

Drug Discovery in Targeting Neurodegenerative Disorders / ACSMEDI Session
10:45
Session Chair
Prof. Rong HUANG
PURDUE UNIVERSITY, West Lafayette, IN, United States
10:50
LE095 - Beyond Amyloid and Tau: Exploring Alternative Therapeutic Targets Using an Integrative Approach
Prof. Daniel WATTERSON
NORTHWESTERN UNIVERSITY, Chicago, United States
11:30
LE096 - Discovery of Selective NKCC1 Inhibitors for the Treatment of Core Symptoms in Autism, Down Syndrome, and Brain Disorders with Defective NKCC1/KCC2 Ratio
Dr Marco BORGOGNO
IAMA THERAPEUTICS SRL, Genoa, Italy
11:50
LE097 - Selective Butyrylcholinesterase Inhibitors for Alleviating Symptoms of Dementia
Dr Urban KOSAK
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia
12:10
LE098 - Modulation of TDP-43-pathy by Brain Penetrant Protein Kinase Inhibitors, a New Hope for ALS and Related Disorders
Prof. Ana MARTINEZ
CENTRO DE INVESTIGACIONES BIOLÓGICAS-CSIC, Madrid, Spain
ATHENA AUDITORIUM
Session 26 'Technologies'

Radiochemistry / AFMC Session

10:45
Session Chair
Prof. Sun CHOI
EWHA WOMANS UNIVERSITY, Seoul, Korea, South
10:50
LE099 - Radiotheragnostics from Bench-to-Bedside Virtual Presentation
Prof. Roger SCHIBLI
ETH ZURICH, Zürich, Switzerland
11:30
LE100 - Evaluation of Cancer Immunity and Development of Novel Radiolabeling Method with Astatin-211 Virtual Presentation
Dr Mikako OGAWA
HOKKAIDO UNIVERSITY, Sapporo, Japan
11:50
LE101 - Medicinal Chemistry in the Development of Molecular Imaging Probes Targeting Prostate-Specific Membrane Antigen
Prof. Youngjoo BYUN
KOREA UNIVERSITY, Sejong, Korea, South
12:10
LE102 - Development of First PET Tracers for the Imaging of CD73 Expression in Triple-negative Breast Cancer
Dr Anna JUNKER
EUROPEAN INSTITUTE FOR MOLECULAR IMAGING, Muenster, Germany
HERMES AUDITORIUM
12:30

Closing Lecture

ATHENA AUDITORIUM

PL004 - Drivers of Innovation in Drug Discovery

Prof. Outi VAARALA
ORION CORPORATION, Espoo, Finland

Chair

Prof. Gianluca SBARDELLA
UNIVERSITY OF SALERNO, Fisciano, Italy
13:15

Closing Remarks, EFMC-YSN PhD Prizes, Poster Prizes & Welcome to EFMC-ISMC 2024

Dr Maria DUCA
UNIVERSITY OF CÔTE D'AZUR, Nice, France
Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal
Prof. Roberto DI SANTO
SAPIENZA UNIVERSITY OF ROME, Rome, Italy

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