8th Fragment-based Drug Discovery Meeting

8th RSC-BMCS Fragment-based Drug Discovery Meeting

Sunday – Tuesday, 27th-29th March 2022

Churchill College, Cambridge plus Virtual

Churchill College




Churchill College

Important links and downloads
Twitter hashtag – #Fragments22
To view Covid-19 RSC policy, click here

The aim of the 8th RSC-BMCS Fragment-based Drug Discovery meeting will be to continue the focus on case studies in Fragment-based Drug Discovery that have delivered compounds to late stage medicinal chemistry, preclinical or clinical programmes. The Fragment series was started in 2007 and continues with this theme in having over three-quarters of the presentations focused on case studies. This will be complemented by technology progress in high concentration, NMR, SPR and X-ray screening.

Who should attend
This conference is suitable for scientists including chemists, biophysicists, structural biologists, etc., with either existing experience of fragments or wanting to learn about this exciting approach to drug discovery. This international meeting attracts delegates from the UK, several mainland European counties, as well as from the USA, Japan, China and South Korea.

Call for Posters / Abstracts
Abstract submission is now closed.


Sunday, 27th March

18.00 Delegate Registration
Buffet supper in Churchill College

Monday, 28th March

07.30Registration and refreshments
10.20Opening remarks
Gordon Saxty, Fidelta
10.30Session 1: Case Histories
Session chair: Mike Hann, GSK

S01: FBLD-Enabled Discovery of cGAS Inhibitors
Fabio Casagrande and Katrin Groebke Zbinden
11.00S02: The Discovery and optimisation of small molecule Inhibitors of TNF - Using Fragments to Inhibit a Protein: Protein Interaction
James O’Connell, UCB
11.30Session 2: Flash poster presentations
Chair: Samantha Hughes, AstraZeneca

FO01: Reactivity Profiling of Sulfur(VI) Fluorides as ‘Beyond Cysteine’ Reactive Electrophiles
Katherine Gilbert, GSK
11.32FO02: Development of Chemical Tools Targeting the Non-Catalytic Functions of Tankyrase
Iona Black, The Institute of Cancer Research
11.34FO03: Exploring the bromodomain of SMARCA4 (BRG1) by Weak Affinity Chromatography (WAC™)
People's Poster Prize Winner
Kirill Popov, Red Glead Discovery
11.36FO04: Successful Fragment library screening by Grating Coupling Interferometry (GCI) against E3 Ligase Target
Nick Martin, Domainex
11.38FO05: Identification of fragments for the development of protein-protein-interaction inhibitors targeting the N-domain of p97
Student Poster Prize Winner
Sebastian Bothe, Julius-Maximilians-University Wuerzburg
11.40FO06: Synthesis and biological evaluation of small fragment inhibitors of Tumor
Necrosis Factor Receptor 1 (TNFR1)
Sara Pannilunghi, University of Geneva
11.42FO07: The synergy of fragment-based drug discovery and high throughput approaches – application to the discovery of inhibitors of the KEAP1:NRF2 protein-protein interaction
Charlotte Griffiths-Jones, Astex Pharmaceuticals
11.44FO08: Title Fragment-based discovery of a novel, brain penetrant, orally active HDAC2 inhibitor
Yuji Ochi, Astex Pharmaceuticals
11.46FO09: 4-pi-photocyclisation as an enabling tool for the synthesis of highly functionalised small-ring carbocyclic and heterocyclic fragments
Susannah Coote, Lancaster University
11.48FO10: Using fragment-based drug discovery to synthesise novel inhibitors of Mycobacterium tuberculosis dihydrofolate reductase
Tim Kirkman, University of Warwick
11.50FO11: Inhibitor or degrader? A drug discovery campaign against B-Cell lymphoma 6 protein
Roxanne Smith, Institute of Cancer Research
11.52FO12: Fragment based design of mycobacterial thioredoxin reductase inhibitors: from a fragment screening to novel inhibitors
Friederike Theresa Fusser, Westfälische Wilhelms-Universität
11.54FO13: Specific inhibition of CK2α from an anchor outside the active site
Paul Brear, University of Cambridge
11.56FO15: Harnessing the Biophysical Fragment Screening Sweet Spot to Discover New Chemotypes for BRPF1 Inhibition
Industry Poster Prize Winner
Thomas Pesnot, Concept Life Sciences
12.30Exhibition, poster session (odd numbers) and networking
13.30Session 3:
Session chair: Samantha Hughes, AstraZeneca

S03 Electrophile Fragment Screening as an Efficient Tool for Covalent Inhibitor Discovery
Nir London, Weizmann Institute of Science
14.00S04 Reactive fragment profiling against the DUBome by MS-proteomics
Rosa Cookson, GSK
14.30S05 Reimagining Druggability using Chemoproteomic Platforms
Daniel Nomura, University of California
15.00Refreshments, exhibition, networking
15:30Session 4: Panel discussion
Session chair: Mary Wheldon, University of Dundee

S06Thoughts on the future for FBDD
Gianni Chessari, Astex Pharmaceuticals

S06: Fragments: Impact, Lessons and What's Next?
Roderick Hubbard, Vernalis
16:30Refreshments, exhibition and networking
18.20Walk to conference dinner
19.00Reception and conference dinner at St Johns College

Tuesday, 29th March

9.30Session 5:
Session chair: Alison Woolford, Astex Pharmaceuticals

S07: SpotXplorer fragments for maximal coverage of pharmacophore space
György M Keserű, Research Centre for Natural Sciences (RCNS)
10.00S08: Enabling CryoEM for SBDD and FBDD
Pamela Williams, Astex Pharmaceuticals
10.30Refreshments, exhibition, networking
11.00S09: Rapid optimisation of fragments and hits to lead compounds from screening of crude reaction mixtures
Lisa Baker, Vernalis
11.30S10: GPCR Fragment-Based Drug Discovery
Ijen Chen, Sosei Heptares
Chris de Graaf, Sosei Heptares
12.30Exhibition, poster session (even numbers) and networking
13.30Session 6:
Session chair: Gordon Saxty, Fidelta

S11: Crystallographic fragment screening identifies sixty diverse inhibitors of carboxylesterase Notum. An example of hit selection, validation and optimisation to ARUK3001185.
Paul Fish, ARUK UCL Drug Discovery Institute
14.00S12: Late Breaking Talk
CAM833 - a small-molecule inhibitor of the BRCA2-RAD51 protein-protein interaction
Marko Hyvonen, Department of Biochemistry, Cambridge

14.15Refreshments, exhibition and networking
15.00S13: Fragment-based design of methionine adenosyl transferase (MAT2a) inhibitors with anti-tumour effect
Marianne Schimpl and Ulf Börjesson, AstraZeneca
15.30S14: Discovery of the first VHL-recruiting, orally bioavailable PROTAC preferentially degrading SMARCA2 over SMARCA4
Christiane Kofink, Boehringer-Ingelheim RCV GmbH & Co KG, Vienna
16.00S15: Fragment based discovery of MRTX1719, a selective inhibitor of the PRMT5.MTA complex for the treatment of MTAP deleted tumours
Christopher Smith, Mirati Therapeutics
16.30Closing remarks
Mike Hann, GSK

Close and depart

Conference dinner
The conference dinner will take place on Monday 28th March at St John’s College and is included within the delegate registration fee.  The Hall at St John’s College is viewed by some as the most magnificent Hall within the Colleges of Cambridge, this splendid room is housed in a 16th century building with an impressive hammerbeam roof and fine old linen fold panelling.  It is a semi-formal evening and is a great time to come together to enjoy a three-course meal.

St Johns College

St Johns College Dining Room

Want to become a member?
To join the RSC in order to qualify for discounted registration fees at all RSC, please follow this RSC link.

Student Bursaries
The RSC BMCS are offering some student bursaries to attend this meeting in person. Applications are open to PhD and post-doctoral applicants studying at academic institutions. Preference will be given to members of the RSC, a National Adhering Organisation of the EFMC, and any co-sponsoring organisation.
Bursary application is now closed.

We are grateful to our confirmed sponsors for their valued support.

AstraZeneca logo

We are grateful to our confirmed exhibitors for their valued support.


Organising Committee
Mike Hann, GSK
Samantha Hughes, AstraZeneca
Darryl McConnell, Boehringer Ingelheim
Gordon Saxty, Fidelta d.o.o. (Chair)
Mary Wheldon, University of Dundee (Treasurer)
Alison Woolford, Astex Pharmaceuticals

Secretariat Contact
Hg3 Conferences Ltd
+44 (0)1423 529333