ActivX – in situ kinase profiling

ActivX is a biotech company developing activity-based profiling systems for several families of drug targets (including kinases and serine hydrolases). The utility of these probes in facilitating drug discoveries has been validated for multiple therapeutic areas including metabolic diseases, oncology and pain management.

ActivX – in situ kinase profiling


ATP- and GTP-utilizing enzymes are major oncology targets due to their central role in nearly all signaling pathways. ActivX has more than 10 years’ experience in developing active site probes for the profiling of a wide range of enzyme classes in native proteomes (including kinases, GTPases, serine hydrolases and cathepsins). ActivX uses its unique technology to identify target and off-target activities of drug candidates in the protein kinase and protease families, mainly focusing on hematology, oncology, inflammatory and metabolic diseases. ActivX’s technology allows fast identification and development of highly selective drugs.

The KiNativ In Situ Kinase Profiling Platform is able to broadly and quantitatively profile protein and lipid kinases in any type of cell or tissue lysate. This in situ technology allows for kinase binding measurements under conditions where critical protein-protein interactions or phosphorylation events are preserved. KiNativ is a very powerful and useful unified assay platform supporting kinase drug development from initial hit validations.

Founded in June 2000, ActivX was acquired by Kyorin Pharmaceuticals in December 2004 after two years of close collaboration. Since then, ActivX performs early stage R&D and clinical developments for Kyorin but also provides fee-for-service activity-based profiling for pharmaceutical, biotech and academic customers. Paul Schimmel, Benjamin Cravatt, Hugh Rosen, Dale Boger and David Pompliano are the Scientific advisors of this Biotech company based in La Jolla (USA). The Board of Directors is composed of John Kozarich, Yoh Ito, Masakatsu Komuro, Kei Takahashi and Koichiro Hagihara. Management’s Team includes also Lorrie Daggett, Tyzoon Nomanbhoy, Jonathan Rosenblum, Kevin Shreder and Helge Weissig. ActivX is currently focused on discovery of new oncology drugs, and already developed KRP-104, an oral anti-diabetic poised to enter global Phase 3 clinical studies. In 2006, ActivX launched KiNativ kinase-profiling platform which is now used by more than 30 major pharmaceutical and biopharmaceutical companies to accelerate kinase drug discovery. ActivX is still expanding its drug discovery and development efforts with a highly qualified R&D team.

More about ActivX :

ActivX – in situ kinase profiling – active site probes – KiNativ In Situ Kinase Profiling Platform – KRP-104 – anti-diabetic

ActivX – kinases – serine hydrolases – GTPases – serine hydrolases – cathepsins – Kyorin