The European Lead Factory has announced that it can now offer two types of phenotypic screening:
- A high-throughput, but “lower content” phenotypic approach that is suited to screening ELF’s entire compound collection, and
- A more complex “high content” screening approach using microscopy or flow cytometry to probe phenotype on a smaller subset of the compound collection
While low content assays can be live measurements or have fixed end points and involve well-averaged readouts, high content assays can be much more complex, based on live or fixed cells, multiple cell types and usually have more than one parameter as a readout. The complexity of the latter workflow makes it better suited to being performed on a smaller representative subset of the large collection.
Phenotypic screening historically has been the basis for the discovery of many drugs. Compounds are screened in cellular or animal disease models to identify compounds that cause a desirable change in phenotype. Only after the compounds have been discovered are efforts made to determine the biological targets of the compounds - a process known as target deconvolution.
Proposals for phenotypic screening approaches follow the normal review and selection process. A dedicated application form is available here.
The submission deadline for the next review and selection round is February 7, 2020.
Great news! European Lead Factory has restarted.
Pivot Park Screening Centre has successfully completed the first ultra-High Throughput Screening in IMI’s ESCulab project, and as such restarting the operations of the European Lead Factory. The screening on the European Compound Collection of ~500.000 compounds using a biochemical 1536-wells assay was finished within 4 days. Currently triaging of the UK owned program is ongoing within the Consortium, applying further biochemical and biophysical follow-up assays as well as the resynthesis of promising hits.
The programme is currently accepting proposals http://www.europeanleadfactory.eu/drug-target-assays.
The European Lead Factory has been funded for another round of screening activities but under a new name European Screening Centre: unique library for attractive biology ESCulab. Over the next five years, the European Lead Factory will initiate 185 new drug discovery projects by screening medically relevant drug targets from European researchers, small and medium-sized enterprises and pharmaceutical industry against the ELF library of 550,000 unique chemical compounds.
The European Lead Factory was launched in 2013 and set up a joint collection of half a million compounds and a state-of-the-art high throughput screening centre. By the time the project ended last year, they had delivered results to researchers in universities, small biotechs and large companies across Europe, helping them to identify potential new drug candidates and breathing new life into a range of disease areas. In many cases, the seeds sown by the European Lead Factory resulted in new patents, partnering deals, and two start-ups. Now, a new IMI project, ESCulab will build on the work of the European Lead Factory. This means that researchers with drug targets can apply to screen the project’s compound collection for hits and get help developing any compounds further if they like. Jon de Vlieger, coordinator of the ESCulab consortium at Lygature, said: ‘It’s truly exciting to continue the onboarding of new and innovative proposals for screening and provide high quality starting points for drug discovery to academics and SMEs throughout Europe. In an effort to broaden our scope we are not only looking for target-based approaches, but now also enable phenotypic screens.’
You can apply here. If you don't have an assay in a format suitable for ultra high-throughput screening it is worth noting that the Wellcome Trust have small awards designed to help with the technology change required for HTS.
The European Lead Factory hold annual meetings intended to support early career scientists, this years meeting will focus on "Hit to Lead optimisation". The meeting will be held at Janssen Pharmaceutica NV, Beerse, Belgium, November 6th - 7th 2017.
Full details are here https://www.europeanleadfactory.eu/early-career-researcher-event/.
Free participation (incl. reimbursement of travel costs up to € 250, accommodation, access to the social get-together) at the conference.
The draft agenda is here.
A great opportunity for those just starting on their drug discovery career.
We are now starting to see some of the results of the screening of academic projects at the European Lead factory that was initiated in 2013.
Dr Mahlapuu’s group, based at the University of Gothenburg, first identified a new target which could be used to reverse metabolic complications in type 2 diabetes. With the help of the European Lead Factory experts, she then screened the Joint European Compound Library of the then 320,000 industry compounds and identified a set of selective and potent small molecules which interfere with this target.
They have now formed a spinout company to develop these leads. ScandiCure has received 1 MSEK from the 2016 SWElife program to continue the development of first-in-class anti-diabetic drug based on small molecule antagonists of a novel key mediator - serine/threonine protein kinase 25 (STK25).
The latest newsletter from the European Lead Factory has just been published and highlights a number of notable achievements.
As a result of the screening campaigns >3000 qualified hits have been awarded to private and public target owners. 72 public target programmes have been accepted, 48 high throughput screens finished and 41 hit lists with associated data reports handed over to the target owners. >150 bespoke assays have been developed in order to extract the most interesting hits for public programmes.
There are now 450,000 compounds in the compound library of which 120,000 are novel compound specifically synthesised for the ELF.
You can read more details here https://www.europeanleadfactory.eu/results/
The European Lead Factory is a collaborative public-private partnership aiming to deliver innovative drug discovery starting points. Having established the first European Compound Library and the first European Screening Centre, the EU Lead Factory aims to give free access to up to 500,000 novel compounds, a unique industry-standard uHTS platform, and much more.
We are now starting to see publications describing these endeavours..