GPCRs in Medicinal Chemistry

8th RSC / SCI symposium on GPCRs in Medicinal Chemistry

Wednesday-Friday, 5th-7th October 2022

Evotec Campus Levi-Montalcini, Verona, Italy

Downloads and Links
Registration is open – follow the link to pay by card or to receive an invoice for settlement by bank transfer
Second announcement
First announcement
Abstract template  – closing dates are 31st March (oral, extended date) and 11th August (poster)
Bursary application form – closing date is 23rd August
Venue travel
Coach pick-up/drop-off location
Accommodation booking agency
Twitter hashtag – #GPCRs22

The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to be holding this 8th meeting in the series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.

The meeting will consist of:
• Case studies in GPCR drug discovery and development
• Structural biology advances and impact on drug design
• Showcasing multiple modalities and drug discovery approaches to modulating GPCRs

Also: poster session – trade exhibition opportunities – two evening dinners and vineyard visit – accommodation agency booking service.

Call for Abstracts
Applications for poster presentation are welcome. Posters will be displayed throughout the meeting and applicants should indicate whether they wish to be considered for a short flash oral presentation when submitting an abstract. Please use this abstract template and note the closing date of 11th August.  The closing date for oral abstract submissions was 31st March (extended date).

Confirmed Speakers
Discovery of VU6028418: a highly selective and orally bioavailable M4 muscarinic acetylcholine receptor antagonist
Aaron Bender, Vanderbilt University, US

Discovery of the clinical candidate ACT-777991, a potent CXCR3 antagonist with therapeutic potential in autoimmune diseases
Eva Caroff
, Idorsia, CH

Impact of GPCR structure-based drug discovery on identification and optimisation of allosteric modulators that bind at the receptor-membrane interface
Anna Cooper, Sosei Heptares, UK

The discovery of CFTX-1554 as an inhibitor of the angiotensin II type 2 receptor, a clinically validated target for the treatment of neuropathic pain
Ann De Blieck, Confo Therapeutics, BE

Structure-based drug discovery across the medicinal chemical GPCRome
Chris de Graaf, Sosei Heptares, UK

The resolution revolution:  GPCR structure-based drug design in 20:20 vision (in 2022)
James Errey, Evotec, UK

Identification of H4R antagonist HTL0032547 as a potential therapy for atopic dermatitis
Charlotte Fieldhouse, Sosei Heptares, UK

Roadmap and resource for GPCR biased signalling
KeynoteDavid Gloriam, University of Copenhagen, DK (virtual)

Discovery of AZD5462, an oral agonist of the Relaxin family peptide receptor 1 (RXFP1) for the treatment of cardiorenal disease
Kenneth Granberg, AstraZeneca, SE

Discovery of potent and selective S1P2 receptor antagonists for treatment of idiopathic pulmonary fibrosis
Bertrand Heckmann, Galapagos, FR

GPCR-based drug design with fragment molecular orbital method
Alexander Heifetz, Evotec, UK

Discovery of MK-4710: a potent, selective, and bioavailable M4 positive allosteric modulator
Michael Lo, MSD, US (virtual)

Salipro DirectMX® enables discovery of novel therapeutics against GPCRs
Robin Löving, Salipro, SE

Structure-guided GPCR drug discovery
Keynote: Bryan Roth, Eshelman School of Pharmacy, University of North Carolina, USA

Discovery of Pecavaptan: a novel dual acting vasopressin V1a/V2 receptor antagonist for the treatment of worsening chronic heart failure
Carsten Schmeck, Bayer, DE

How to leverage new AI technologies alongside traditional HTS to better validate hit compounds for GPCRs
Carleton Sage, Eurofins Discovery, US

Discovery of FPR2 agonists for treatment of heart failure
Nicholas Wurtz, Bristol-Myers Squibb, US

Programme Timings
To assist you with your travel plans, expected start and finish times are
Day 1  08.30 Registration opens
Day 1  09.20 Technical programme starts
Day 3  15.00 Close of symposium

Registration and the Pandemic
This event will be held at the Evotec Campus Levi-Montalcini in Verona, Italy, with a small number of virtual speakers. Should the COVID situation impair a face-to-face meeting, it would be re-organised as a virtual event (timing and details to be determined). Those who did not wish to attend the meeting in a virtual format would be refunded in full; and those registered delegates who did wish to attend the rearranged virtual meeting would be given partial refunds.

Registration Fees
Registration is open, and you may register via this link.  There is an option for Exhibitor and Sponsor registrations at the foot of the registration page, and you may pay by card or request an invoice for settlement by bank transfer.  Registration fee are:

Early rate, for payment by 4th July:
£500  Member* of the RSC or SCI
£700  Non-member
£200  Student** member, unemployed member, retired member
£300  Student** non-member, unemployed non-member, retired non-member

Standard rate, for payment between 5th July and 5th September:
£600  Member* of the RSC or SCI
£800  Non-member
£250  Student** member, unemployed member, retired member
£350  Student** non-member, unemployed non-member, retired non-member

Late rate, for payment from 6th September (due prior to event):
£675  Member* of the RSC or SCI
£875  Non-member
£325  Student** member, unemployed member, retired member
£425  Student** non-member, unemployed non-member, retired non-member

Registration closing dates:
Online registration (card payments): Friday, 30th September 2022 at 17:00 (BST)
Registration against invoice (bank transfers): Tuesday, 6th September 2022

* Member is a paid-up member of the RSC or SCI
** Student rates apply to undergraduate and post-graduate students only, but not post-doctoral students or students in full-time employment.

Registration fees include:
– coach transport between Verona city centre and the Evotec campus at the start and end of each day
– dinner on Wednesday evening at the Ristorante Scaligero
– vineyard visit and dinner on Thursday evening at Rocca Sveva.

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 and the SCI is offering some student bursaries to cover the registration fee and to contribute towards accommodation and/or travel.  Applications are invited from PhD and post-doctoral students studying at an academic institution, preferably members of the RSC, SCI or EFMC.

The closing date for bursary application will be 23rd August, and an application form may be downloaded here.

Networking Social Activities and Accommodation
The informal evening dinner on the first evening will be a great time to come together to enjoy a traditional three-course meal. The dinner will take place on Wednesday, 5th October at Ristorante Scaligero, Via Guglielmo Marconi 7.

A vineyard visit and informal dinner will be held on Thursday, 6th October. The visit will consist of a guided tour of the underground cellars of Cantina Soave  an aperitivo either in the botanical garden or outside the restaurant (location dependent on harvest-time), an opportunity to use the wine shop, and a fantastic dinner with wine-sampling in the Locanda del Borgo. (Coach transport will be provided.)

For all accommodation requests (including last-minute bookings), we suggest using the 24-hour service provided by Verona Booking, using this weblink.

Venue and Travel 
Detailed travel information may be found in this Venue Guide.

Coaches provided by Conference
A gratis coach service will be provided by the conference between Verona city centre (Giardini Pradaval location map) and Evotec at the beginning and end of each day, and on a daily basis.   On Thursday afternoon, the gratis coach service will travel to the vineyard and later back to Verona city centre.

Exhibitor Opportunity
The exhibition space is now fully booked – sorry!

The Exhibitor Package comprises:
– stand space measuring 3 metres wide x 2 metres deep
– table measuring 240 cm wide x 80 cm deep and chair
– electrical and wi-fi access
– your logo and full promotional page in the delegate handbook
– your web-linked company name on this page
– your logo in the rolling slides, shown during the breaks
– full attendance at the technical programme, poster sessions, Wednesday evening dinner, and Thursday evening vineyard visit and dinner.

Exhibitor Packages include full participation in the social activities and charges are below.
£1,600 including one full delegate
£2,000 including two full delegates

Delegate pack inserts, comprising no more than two pages of A4 fixed together, may be booked at a charge of £200 – sponsor provides the inserts.

Confirmed Exhibitors
Activate Scientific
BioAscent Discovery
Design Pharmaceuticals
Eurofins Discovery
SB Drug Discovery

Sponsorship Opportunities
We are  grateful to Evotec for their generous support, as well as Vertex and Sosei Heptares.   Additional sponsors are sought to support this event.



We are grateful to our supporters:

Organising Committee
Daniele Andreotti, Evotec, IT
Adrian Hall (co-chairman), UCB, BE
Duncan Hay (treasurer), Vertex, UK
Caroline Low (co-chairman), Isomorphic Laboratories, UK
Nigel Swain, Sosei Heptares, UK

Secretariat Contact and Further Information
Maggi Churchouse (Mrs), UK