Business Wire

Enamine Supplies DSI Poised Fragment and Analogue Libraries to Diamond Light Source XChem Facility and SGC Oxford Screening Efforts

Del

Diamond Light Source (Diamond) and the Structural Genomic Consortium (SGC) Oxford announced today that Enamine, a chemical company and producer of novel chemical building blocks and screening libraries, will become a key supplier of poised fragment and analogue libraries to its XChem facility. Enamine will offer a new generation of the hit-finding library, Diamond-SGC-iNEXT (DSI) Poised Library to enable fast and productive fragment-based lead discovery (FBLD).

Diamond, in collaboration with the SGC Oxford, set up the XChem facility for fragment screening by X-ray crystallography to ensure public access to efficient FBLD. In addition, to enable fast and productive lead development, the collaboration developed the concept of “poised fragments” (Cox et al., Chemical Science, 2016), which constitutes its frontline screening strategy. FBLD is a common approach in academia and industry for developing new chemical probes and drug starting points (leads) from weak starting evidence, namely fragment hits. The hits must be chemically altered to improve their binding strength to the target protein, along with other properties.

The DSI Poised Library comprises 768 highly soluble fragments. Each compound is accompanied by its own virtual chemical space, which is readily accessible for synthesis and available for purchase through Enamine. Any hit from this library can be developed with follow-up chemistry within a maximum of three weeks using Enamine’s ground-breaking REAL database.

Prof Frank von Delft, Head of the XChem Collaboration and Principal Beamline Scientist at Diamond Light Source, explained: “The XChem facility has already helped over 60 users find thousands of hits across over 80 targets. To address the subsequent challenge, that chemical elaboration is generally expensive and time consuming, we developed and published the poised approach. Poised fragments can be synthesised in one step from commercially available starting materials using robust, high-yielding reactions, so that libraries of analogues can be synthesised quickly and at a low cost. Coupled with high-throughput biophysical methods, such as XChem screening but also NMR or SPR, this should provide a cost-efficient approach to early-stage fragment-based lead design.”

Dr Anthony Bradley, Project Leader on Fragment Development at SGC Oxford, added: “We quickly discovered that to realise the full power of the approach, we urgently needed to address the problem of compound supply. We are thus delighted to work with Enamine for the materialisation of the DSI Poised Library, fully benefiting from Enamine’s extensive stock of building blocks, capabilities and proven industry solutions. This puts both the primary library and follow-up analogue series within budgets and timelines of even exploratory compound discovery efforts worldwide. The SGC Oxford will be making extensive use of this offering in its many ongoing and future compound development projects.”

Michael Bossert, Head of Strategic Alliances at Enamine, commented: “The high technological degree of specialisation of Diamond and its unique XChem facility, was key to this collaboration. It is important to collaborate with high-tech companies in order to launch high-value technology-based products that aim to improve our customers R&D efficiencies and discovery project successes.”

Prof Paul Brennan, Principal Investigator for Medicinal Chemistry at SGC Oxford, and senior author of the original publication, added: “It is incredibly gratifying to see our original Diamond-SGC Poised Library (DSPL) and poised approach become a commercial offering. We hope this will allow it to become an essential tool in accelerating the development of small molecules probes and drugs.”

The library will be available to a non-exclusive group of nine research institutes operating X-ray and NMR screening located in Europe, USA and China. The European institutes include the partners of the iNEXT fragment screening effort: Diamond, EMBL and ESRF (Grenoble), NKI (Amsterdam), BMRZ (Frankfurt), FMP (Berlin) and CIRMMP (Florence). Other scientists interested in accessing and using the library for their own research are invited to do so.

For further information about the DSI Poised Library: https://xchem.github.io/oxxchem/DSI_poised_fragment_library.xlsx

ENDS

For high-resolution images, please contact lorna.cuddon@zymecommunications.com

Contact information

Zyme Communications
Lorna Cuddon
E: lorna.cuddon@zymecommunications.com
T: +44 7811996942

Om Business Wire

Business Wire
Business Wire
24 Martin Lane
EC4R 0DR London

+44 20 7626 1982http://www.businesswire.co.uk

Business Wire, a Berkshire Hathaway company, is the global leader in multiplatform press release distribution.

Følg saker fra Business Wire

Registrer deg med din epostadresse under for å få de nyeste sakene fra Business Wire på epost fortløpende. Du kan melde deg av når som helst.

Siste saker fra Business Wire

Schlumberger Announces Full-Year and Fourth-Quarter 2017 Results19.1.2018 12:00Pressemelding

Schlumberger Limited (NYSE:SLB) today reported results for full-year 2017 and the fourth quarter of 2017. Full-Year Results (Stated in millions, except per share amounts) Twelve Months Ended Change Dec. 31, 2017 Dec. 31, 2016 Year-on-year Revenue $30,440 $27,810 9% Pretax operating income $3,921 $3,273 20% Pretax operating margin 12.9% 11.8% 111 bps Net loss (GAAP basis) $(1,505) $(1,687) n/m Net income, excluding charges and credits* $2,085 $1,550 35% Diluted EPS (loss per share) (GAAP basis) $(1.08) $(1.24) n/m Diluted EPS, excluding charges and credits* $1.50 $1.14 32% *These are non-GAAP financial measures. See section below entitled "Charges & Credits" for details. n/m = not meaningful Full-year 2017 revenue of $30.4 billion increased 9% year-on-year. This included a full year’s activity from the acquired Cameron businesses as compared to three quarters of activity in 2016. Excluding the addition of Cameron, revenue growth was driven by land activity in North America, which increa

The Coca-Cola Company Announces New Global Vision to Help Create a World Without Waste19.1.2018 11:55Pressemelding

The Coca-Cola Company announced today that it is fundamentally reshaping its approach to packaging, with a global goal to help collect and recycle the equivalent of 100% of its packaging by 2030. This press release features multimedia. View the full release here: http://www.businesswire.com/news/home/20180119005104/en/ In 2017, employees from Heartland Coca-Cola Bottling Co. joined with other volunteers in St. Louis to collect and sort 14,480 pounds of debris; 63 percent was diverted for recycling. Coca-Cola then partnered with manufacturer Phoenix Technologies to convert plastic bottles into recycled PET plastic for use in new bottles. (Photo: Business Wire) This goal is the centerpiece of the Company’s new packaging vision for a World Without Waste, which the Coca-Cola system intends to back with a multi-year investment that includes ongoing work to make packaging 100% recyclable. This begins with the understanding that food and beverage containers are an important part of people’s m

Researchers and Scientists from Five Countries Named Winners of King Faisal Prize 201819.1.2018 10:33Pressemelding

Five researchers and scientists from Malaysia, Jordan, Tunisia, the US and the UK have been named winners of the King Faisal Prize 2018 as the 40th edition of the renowned award recognized their distinguished contributions towards humanity. The Prize honours exceptional achievements in five categories: Service to Islam, Islamic Studies, Arabic Language & Literature, Medicine, and Science. This press release features multimedia. View the full release here: http://www.businesswire.com/news/home/20180119005245/en/ His Royal Highness Prince Khalid Al-Faisal, Chairman of King Faisal Prize Board, Abdulaziz (Photo: AETOSWire) Professor Irwandi Jaswir, Deputy Dean of the International Institute for Halal Research and Training (INHART) and Secretary of Council of Professors at the International Islamic University Malaysia (IIUM), has been named the winner in the Service to Islam category for contributions to the development of ‘Halal Science’ and Halal food and consumer goods. Professor Bashar

E.ON Chooses Corinex Broadband over Powerline Technology for their Smart Metering Rollout19.1.2018 06:00Pressemelding

E.ON, an international energy company that serves 32 million customers across multiple countries, has decided to use broadband over powerline (BPL) as the key technology in their communication mix, in the smart metering communication infrastructure for the low voltage part of their grid. E.ON chose Corinex as the solution provider for the initial two years of the deployment. The initial deployment will be several ten thousands of repeaters and head ends providing secure communication for a couple of hundred thousands of households. Corinex Grid Value network management based on IBM Tivoli platform will manage the network. “After extensive field trials, we found that Corinex broadband over powerline technology meets our requirements for mass rollout of smart metering services. We are convinced BPL is ideally suited to address the needs of many other utilities, so E.ON is interested in supporting BPL industry standardization in order to create a broad ecosystem of silicon and system vend

Changes in Executive Management at Sosei19.1.2018 01:54Pressemelding

Sosei Group Corporation (“Sosei” or the “Company”) (TOKYO: 4565), the world leader in GPCR medicine design and development, today announced that Dr. Fiona Marshall has resigned from her position as Executive Vice President and Chief Scientific Officer of Sosei to assume a senior role outside the Company. Dr. Marshall will leave Sosei at the end of February 2018. “As a co-founder of Heptares, I am very proud to have been associated with building a team of talented scientists over the past decade that has made many important breakthroughs in the field of GPCR stabilization and structure-based drug design, a unique technology that now underpins Sosei’s powerful drug discovery capability,” said Dr. Marshall. “With the team in excellent hands, I feel the time is right for me to move on to new challenges and I wish everyone at Sosei the best for what looks set to be an exciting future for the Company.” Peter Bains, Chief Executive Officer of Sosei, added: “Fiona has been a pivotal figure in

DXC Technology Named a 2018 Thomson Reuters Top 100 Global Technology Leader18.1.2018 23:12Pressemelding

DXC Technology (NYSE: DXC) has been recognized as a 2018 Top 100 Global Technology Leader by Thomson Reuters. The inaugural program identifies the tech industry’s most operationally sound and financially successful organizations. The Thomson Reuters Top 100 Global Tech Leaders study, the industry’s first holistic assessment of today’s leading tech companies, utilizes a 28-point data-driven algorithm to objectively identify organizations positioned to thrive in a complex and changing business environment. The patent pending methodology, developed by the Thomson Reuters Boston Innovation Lab, is based on eight principal pillars of performance: Financial Performance, Management and Investor Confidence, Risk and Resilience, Legal Compliance, Innovation, People and Social Responsibility, Environmental Impact, and Reputation. According to Thomson Reuters, these are the companies whose final scores across the pillars outshine over 5,000 other technology companies around the world. “DXC Techno

I vårt presserom finner du alle våre siste saker, kontaktpersoner, bilder, dokumenter og annen relevant informasjon om oss.

Besøk vårt presserom