Twenty Years of the Rule of Five

 

Wednesday, 20th November 2019

 

Sygnature Discovery, BioCity, Nottingham, UK

 

 

Registration is now closed - fully booked

 

Twitter hashtag - #RuleofFive2019

 

Downloads and Links
 

Third announcement

Second announcement

First announcement

 

Directions to the venue

Site plan (showing car park)

RSC website

 

Synopsis
It has been over twenty years since Lipinski published his work determining the properties of drug molecules associated with good solubility and permeability. Since then, there have been a number of additions and expansions to these “rules”. There has also been keen interest in the application of these guidelines in the drug discovery process and how these apply to new emerging chemical structures such as macrocycles.

This symposium will bring together researchers from a number of different areas of drug discovery and will provide a historical overview of the use of Lipinski’s rules, as well as looking to the future and how we use these rules in the changing drug compound landscape.

 

Features of the Meeting

  • Historical look at the use of the Rule of Five

  • New parameters used in drug discovery

  • Look forward to the next 20 years

  • Panel discussion in each session

  • Poster session

Who should attend

This meeting is of interest to scientists of any level of experience from academia and industry.
 

Call for Poster Abstracts

Applications for poster presentations were invited within the theme of historical use of the Rule of Five or looking forward and beyond the Rule of Five.  Posters will be displayed throughout the day. The closing dates for submissions were:

  6th October - poster

  30th June - oral.

 

Programme

09:30Registration and refreshments
 

 

Session 1:  History to Present Day

Session chair:  Mary Wheldon, University of Dundee

10:00

The rule of five and the pursuit of compound quality

Paul Leeson, Paul Leeson Consulting, UK

10:30

Do we need to change the definition of drug-like properties?

Michael Shultz, Novartis, USA

11:00Refreshments and posters
11:30

Molecule properties: how relevant are aromatic and aliphatic descriptors?

Tim Ritchie, Zerlavanz Consulting UK, UK

12:00

BET PROTACs: investigating the effects of linker functionality on physicochemical properties

John Priestner, GlaxoSmithKline, UK

12:30

Discussion panel, facilitated by Chris Swain, Cambridge MedChem Consulting

13:00

Lunch and posters

 

 

Session 2:  Beyond the Rule of Five and the Future

Session chair:  Jonathan Goodman, University of Cambridge

14:00

Structure property relationships in the Ro5 space and beyond

Elisabetta Chiarparin, AstraZeneca, UK

14:30

Investigating the chameleonic properties of αVβ6 integrin antagonists for the treatment of IPF

James Thompson, GlaxoSmithKline, UK

15:00

Chemical space adventures below and beyond Lipinski

Jean-Louis Reymond, University of Bern, Switzerland

15:30

Refreshments and posters

16:00

Defining known drug space using DFT

Jóhannes Reynisson, Keele University, UK

16.30  Property-based drug design Beyond Ro5- lessons learned  from AbbVie’s drugs and compound collection
Phil Cox, AbbVie, USA
17:00Panel discussion, facilitated by Mihiro Sunose, Sygnature Discovery
17:30Drinks reception
18:30

Close (latest)

 

Registration and Bursaries

Registration is now closed - fully booked

If you wish to add your name to a waiting list in case of additional spaces becoming available, please send an e-mail to Maggi via this link.


£120 RSC member
£165 Non-member
  £50 RSC student* member
  £80 Student* non-member
* Student is undergraduate or post-graduate, not post-doc
Member is a paid-up member of the RSC. A late fee of £30 will apply to payments received from 19th October onwards.

A number of RSC-BMCS and RSC-CICAG student bursaries were available up to a value of £250, to support registration, travel and accommodation costs for PhD and post-doctoral applicants studying at academic institutions. The closing date for bursary applications was 4th October.

 

Delegate Pack Inserts

Delegate pack inserts may be booked at £150, comprising no more than two pages of A4 fixed together.

 

Cancellation Policy
In the event of cancellation before 6th November, 80% of the fee paid will be refunded. Cancellations must be received in writing. Refunds will not be possible from that date although substitutions are possible at any time.

In the unlikely event of cancellation of the meeting, fees paid will be refunded in full.  Registration acknowledgements will be sent within two weeks.
 

Venue and Travel
Address:  Innovation Building, Sygnature Discovery, BioCity, Pennyfoot Street, Nottingham NG1 1GF.   Please download a site plan (showing car park) here.
 

Travel: 

 

By train

East Midlands airport is just 20 minutes away, and regular trains run direct from London (journey time two hours).  Sygnature Discovery is just over half-a-mile from the railway station. 

 

Leave the railway station following signage for trams. After passing through the barriers, turn right onto Station Street, turn left at Jury's onto London Road. At the roundabout, bear right onto Lower Parliament Street (A6008) towards MachineMart, turn right at MachineMart onto Pennyfoot Street. Enter second building on the right (white with green stripes) with black Innovation Building sign outside (postcode NG1 1GF) - about 12 minutes' walk.

 

By car

There is no car parking for visitors at the venue, BioCity.

 

Instead the nearest car park (run by the city council) is immediately behind the Innovation Centre, Motorpoint Arena.  Further information about charges may be found here, and you should buy your ticket from the machine.  Here is a site plan showing the car park location.  

 

By Taxi

Cloud Cars offers an eco-friendly car service.  The entire fleet is of environmentally-friendly hybrid cars, which run on a combination of electricity and petrol, significantly reducing emissions.  Book via this weblink or by telephone on 01158 244244.   Card only, fixed-price fares.

 

DG Cars are open 24 hours a day.  Book via this weblink or by telephone on 01159 500500 and 01159 607607.  

 

By Air
You may take a bus from East Midlands airport to Nottingham railway station, or you may take a train from East Midlands Parkway railway station to Nottingham.

 

DG Cars offer airport transfers which may be booked online via this weblink or by telephone on 01159 500500 and 01159 607607.  

 

Sponsors
This symposium is organised by the RSC BMCS (Biological and Medicinal Chemistry Sector) and the RSC CICAG (Chemical Information and Computer Applications Group). 

    

 

We are grateful to Sygnature Discovery for their generous sponsorship of this event.

 

 

Organising Committee
Chris Swain (chair), Cambridge MedChem Consulting
Jonathan Goodman, University of Cambridge
Mihiro Sunose, Sygnature Discovery
Mary Wheldon, University of Dundee

 

Secretariat Contact
Maggi Churchouse, 3 East Barn, Market Weston Road, Thelnetham, Diss IP22 1JJ, UK
Telephone: +44 (0)1359 221004
E-mail:  maggi@maggichurchouseevents.co.uk

 

To contact the secretariat, please send an e-mail.

 

Registration is now closed - fully booked

 


 

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