DiscoveRx® acquired the KINOMEscan kinase screening services division from San Diego-based Ambit Biosciences. With this deal DiscoveRx says that it now offers over 400 functional cell-based GPCR and kinase assays as well as a panel of 442 kinase assays.
KINOMEscan is a high-throughput method for screening small molecule compounds against large numbers of human kinases. It provides a fast, accurate, uniform, and quantitative profile that details how well each compound binds to both intended and unintended targets, according to DiscoverRx.
“The acquisition of KINOMEscan represents our commitment to build a company and a brand that positions us as the leading solution provider across the drug discovery continuum,” remarks Pyare Khanna, Ph.D., CEO and president of DiscoveRx. Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, CA, with an additional office in Birmingham, U.K. It is dedicated to the development and commercialization of solutions to study GPCRs, kinases, and other major drug target classes.
The company holds extensive intellectual property in the area of ß-galactosidase enzyme fragment complementation (EFC) for biochemical and cell-based assays. Its EFC platform is a homogeneous, nonradioactive detection technology based on two genetically engineered ß-galactosidase fragments: a large protein fragment (enzyme acceptor, or EA) and a small peptide fragment (enzyme donor, or ED). Separately, the ß-gal fragments are inactive, but in solution they rapidly recombine to form active ß-galactosidase enzyme that hydrolyzes substrate, producing an easily detectable chemiluminescent or fluorescent signal.
HitHunter™ assays are based on EFC technology and have been developed for GPCR second messenger signaling, kinase activity and binding, nuclear hormone receptor binding, and protease activity. They are formatted such that analytes are detected in solution, without separation or wash steps. This reportedly provides improved sensitivity and precision compared to conventional immunoassays.
In the HitHunter assays ED is conjugated to ligand of interest (cAMP, cortisol, or cGMP), which competes against free ligand for binding to a protein. Depending on the ligand of interest, the binding protein can be an antibody, an enzyme, or a receptor. A positive signal is generated in direct proportion to the amount of free ligand bound by the binding protein.
PathHunter™ assays also are based on the EFC platform and used for protein-protein interactions and protein trafficking. They can be leveraged in whole cells using standard 96-, 384-, or 1,535-well protocols on standard plate readers.
“With the majority of pharmaceutical drug discovery programs centered around the GPCR and kinase target classes, the addition of the KINOMEscan platform, a proven technology for high-throughput kinase screening and profiling, complements our PathHunter and HitHunter cell-based kinase and GPCR assay platforms,” says Dr. Khanna.