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DiscoverX and the SGC Announce Major Milestone in Development of Kinase Chemogenomic Set

05:10 EDT 3 Aug 2017 | PR Newswire

FREMONT, Calif., Aug. 3, 2017 /PRNewswire/ -- DiscoverX Corporation, the leading supplier of innovative cell-based assays and services for drug discovery and development, in collaboration with the Structural Genomics Consortium (SGC) at the University of North Carolina at Chapel Hill today announced the completion of an important milestone and extension of their partnership to develop selective and potent chemical probes for the unexplored human kinome. A publication describing the teams' significant progress toward achieving a comprehensive Kinase Chemogenomic Set (KCGS) appears this week online in the journal PLOS ONE http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0181585.

The kinase family of 500 enzymes provides a tremendous opportunity for drug discovery with over 30 inhibitors approved for the treatment of human disease. Development of selective inhibitors to interrogate this important family of proteins is a critical step to better understand the roles they play in human disease. A publicly available KCGS enables the community to openly collaborate on the discovery and development of new therapies. This collaborative project between industrial and academic scientists will continue to expand the KCGS with the goal of full coverage of all human protein kinases. This expansion, combined with the use of the set in varied disease-relevant phenotypic screens and sharing of the resulting data in the public domain, is the best mechanism to ensure that the therapeutic potential of as many protein kinases as possible will be uncovered.

David Drewry, Ph.D., a research associate professor at the UNC Eshelman School of Pharmacy, SGC-UNC principal investigator and KCGS project leader, said, "With this publication we are sharing our goals, and announcing to the community our progress towards construction of a comprehensive KCGS. In the paper, we disclose the results of broad kinome screening of a compound set we call Published Kinase Inhibitor Set 2. We are releasing these results into the public domain in keeping with our mission to support the discovery of new medicines through open access science. These results now put us about halfway towards our goal of complete kinome coverage. We sincerely thank all of our co-author partners whose vision, generosity, and hard work makes the construction of this set possible."

DiscoverX, through its KINOMEscan offering, is the leading provider of kinase screening services and has successfully partnered with multiple organizations to bring kinase inhibitor programs into the clinic. Todd R. Nelson Ph.D., CEO of DiscoverX, stated, "Through the extension of our work with the SGC and continued expansion of the KCGS, DiscoverX continues to take a leading role supporting the discovery and development of therapeutic molecules, especially in the areas of oncology, immunology, and neuroscience."

About DiscoverXDiscoverX Corporation, headquartered in Fremont, CA, USA, is a leader in the design, manufacture and sale of biochemical and cell-based assays for the drug discovery & life science markets. This industry-leading portfolio of products and services, under the KINOMEscan®, PathHunter® and BioMAP® brands, are used to aid life science research and enable rapid development of safe and effective biologic and small molecule drugs, by improving research productivity, effectiveness of screening, lead optimization & bioanalytical campaigns, as well as providing predictive tools that deliver physiologically relevant insights on drug molecules from early discovery through pre-clinical development. DiscoverX embodies a pioneering approach to creating life science tools that have been widely adopted across the globe in pharmaceutical, biotechnology and academic laboratories. Learn more at discoverx.com.

About the Structural Genomics Consortium (SGC)The SGC is a pre-competitive public-private partnership that accelerates research in human biology and drug discovery by making all of its research output freely available to the scientific community. To achieve its mission, the organization is building an open and collaborative network of scientists: the SGC has active research facilities at six leading academic institutions across the globe (Toronto-Canada, Oxford-UK, UNICAMP-Brazil, Karolinska-Sweden, UNC Chapel Hill-USA and Frankfurt-Germany), and SGC scientists collaborate with more than 300 researchers in academia and industry. The SGC is a registered charity (number 1097737) that receives funds from AbbVie, Bayer Pharma AG, Boehringer Ingelheim, Canada Foundation for Innovation, Eshelman Institute for Innovation, Genome Canada, Innovative Medicines Initiative (EU/EFPIA), Janssen, Merck & Co., Novartis Pharma AG, Ontario Ministry of Economic Development and Innovation, Pfizer, São Paulo Research Foundation-FAPESP, Takeda, and Wellcome Trust. For more information, visit www.thesgc.org.  PKIS2, a collection of >300 fully annotated kinase inhibitors donated by GSK, Pfizer, and Takeda, is currently available from the SGC UNC by completing an on-line request.

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