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Cambridge MedChem Consulting

Solutions for Drug-Resistant Infections Meeting

SDRI 2017 is a multi-disciplinary scientific conference for the Asia Pacific region focused on Solutions for Drug Resistant Infections. This inaugural conference theme is New Drugs for Drug-Resistant Infections. The conference will take place at the Brisbane Convention and Exhibition Centre in Australia from 3 - 5 April, 2017.

The program is expected to attract 400 international participants and will provide a fantastic forum for researchers and industry representatives working in the space of microbiology, virology, parasitology, genomics, pharmacology and medicinal chemistry, to network and discuss new ways to solve the global challenge of drug-resistant infections. Our goal for SDRI 2017 is to lead a concerted discussion to set three priorities and guide research efforts towards global solutions for drug resistance research.

Conference themes:

  • Antimicrobial drug discovery
  • Improvements to existing anti-infective agents and repurposing
  • New Drug Targets
  • Alternate therapies
  • Navigating the pipeline
  • International Models and Funding
  • Vector control and vaccines

International keynote speakers confirmed:

  • Professor Dame Sally Davies DBE FMedSci FRS, Chief Medical Officer for England
  • Professor Ramanan Laxminarayan, Director for Center for Disease Dynamics, Economics & Policy (CDDEP), Washington and Vice-President for Research & Policy at Public Health Foundation of India (PHFI)

More details and registration

Fragment based screening

I’ve just updated some of the fragment based screening pages, in particular I’ve updated the section on Published fragment Hits. The database now contains 1216 entries culled from over 240 publications directed at nearly 174 different molecular targets using 26 different detection technologies.

I also noticed that a fragment library I was helped design is now commercially available, The Selcia Fragment Library was designed to have broad applicability and chemical tractability. It is also one of the few libraries where solubility has been confirmed experimentally. The profile of the library is included in the fragment library profiles.

Why Most Clinical Research Is Not Useful

An interesting publication in PLOS Medicine titled “Why Most Clinical Research Is Not Useful” DOI.

John P. A. Ioannidis suggests that a series of features that make clinical research useful can be identified, including those relating to problem base, context placement, information gain, pragmatism, patient centeredness, value for money, feasibility, and transparency and concludes …

Overall, not only are (clinical) most research findings false, but, furthermore, most of the true findings are not useful. Medical interventions should and can result in huge human benefit. It makes no sense to perform clinical research without ensuring clinical utility. Reform and improvement are overdue.

Given the costs involved I suspect this final point may catch the eye.

Reform is needed. Altering our approach could easily produce more clinical research that is useful, at the same or even at a massively reduced cost

CO-ADD web portal

The CO-ADD web portal is now live You can now submit your free antimicrobial screening request, download all forms and access your primary screening, cytotoxicity, hit confirmation and hit validation reports online on the new secure CO-ADD user portal.

CO-ADD (Community for Open Antimicrobial Drug Discovery) is a not-for-profit initiative led by academics at The University of Queensland. Our goal is to screen compounds for antimicrobial activity for academic research groups for free. We aim to help researchers worldwide to find new, diverse compounds to combat drug-resistant infections.

Chemical Probes Portal Updated

The Chemical Probes Portal has been updated, the new site includes a lot more data about the existing probes, reviewer ratings and their comments.

A chemical probe is simply a reagent—a selective small-molecule modulator of a protein’s function—that allows the user to ask mechanistic and phenotypic questions about its molecular target in cell-based and/or animal studies. These are tools not drugs, they allow scientists to investigate the relationship between a molecular target and the broader biological consequences of modulating that target in cells or organisms. In general the focus is on specificity for the target rather than pharmacokinetics.

BIO Releases Clinical Development Success Rates 2006-2015

Biotechnology Innovation Organisation (BIO) have released the results of a huge study on clinical development success rates.

The study included 9,985 clinical trails and covered a wide number of therapeutic ares including Allergy, Autoimmune, Cardiovascular, Chronic High Prevalence Diseases, Endocrine, Gastroenterology, Hematology, Infectious Disease, Metabolic, Neurology, Oncology, Ophthalmology, Psychiatry, Rare Diseases, Respirator, and Urology.

Key findings from the study include:

  • Clinical trial programs that used selection biomarkers saw an overall likelihood of approval (LOA) from Phase I of 25.9%, compared to 8.4% when no selection biomarkers were used.
  • The overall LOA from Phase I for all developmental candidates was 9.6%, and 11.9% for all indications outside of Oncology.
  • Of the 14 major disease areas studied, Hematology had the highest LOA from Phase I (26.1%) and Oncology had the lowest (5.1%).
  • Oncology drugs were approved the fastest of all 14 disease areas.
  • Rare disease programs had higher success rates at each phase of development vs. the overall dataset.
  • Chronic diseases with high populations had lower LOA from Phase I vs. the overall dataset.
  • Phase II clinical programs continue to experience the lowest success rate of the four development phases, with only 30.7% of developmental candidates advancing to Phase III

Open Source Malaria Webinar recording


A webinar describing the work undertaken by the Open Source Malaria Consortium was held on 24th May and a recording of the meeting is now available.

The meeting lasted around 1 hour and be viewed online here

Open Source Malaria (OSM) is aimed at finding new medicines for malaria using open source principles, embodied in the 6 Laws of Open Research. At the moment the majority of work involves the synthesis of analogs of compounds identified by big pharma, with the aim of improving their potency while making the molecules more "druggable", what is known as a "hit-to-lead" campaign.

The questions raised in the webinar are highlighted as “Meeting Discussion Points” on the github page. Please feel free to join in the discussions.

RSC symposium on Late Stage Functionalization for Synthesis and Medicines

RSC symposium on Late Stage Functionalization for Synthesis and Medicines

Date Monday, 5th December 2016 Place Mathematical Institute, Andrew Wiles Building, Oxford, U Organisers RSC-BMCS (Royal Society of Chemistry – Biological and Medicinal Chemistry Sector)

Late Stage Functionalization (LSF) holds the potential to revolutionise the logic of chemical synthesis and open new ways to prepare novel natural products and medicines. The introduction of important chemical groups for medicinal chemistry in the very last steps of the synthesis through LSF could also dramatically speed up the preparation of NCEs and have a major impact on drug discovery. The availability of new powerful catalytic chemistries showing a high degree of functional group tolerance and that can be performed under mild conditions offer tremendous opportunities for chemists to access new molecules that cannot be made easily by conventional approaches.

Cheminformatics for Drug Design: Data, Models & Tools

A joint meeting Organised by SCI's Fine Chemicals Group and RSC's Chemical Information and Computer Applications Group

A4 Cheminfo flyer

Community for Open Antimicrobial Drug Discovery

A little while ago I mentioned The Community for Open Antimicrobial Drug Discovery effort to provide free compound screening against a variety of infective agents. .

Primary Screening of a 1mg sample Test against key ESKAPE pathogens, E. coli, K. pneumoniae, A. baumannii, P. aeruginosa, S. aureus (MRSA), as well as the fungi C. neoformans and C. albicans, at a single concentration.
Hit Confirmation:- Confirm activity with minimum inhibitory concentration and counterscreen for cytotoxicity and membrane interaction.
Hit Validation:- Test the positive hit against a broader panel of microbes and evaluate the basic drug qualities of actives. CO-ADD will screen your compounds for free and make no claim to IP. The linked flyer gives full details

You can also read more details in this Nature article DOI

It looks like they have achieved an important milestone!

Thanks to our research community we have received 100,000 compounds from 30 countries in 15 months! Make a difference: clear the fridge, empty the shelves and send through your compounds for free antimicrobial screening against 5 bacteria and 2 fungi. We would also like to acknowledge the contribution of the French National Chemical Library that has safely arrived in Brisbane last week!

So if you have compounds sitting in the back of cupboards why not send them to be tested