Compound Profiling
Compound profiling is a challenging, but integral component of the drug discovery process. Traditional compound profiling includes compound selection, as well as candidate optimization, particularly as the candidates move through the development processes. With advanced technologies and assays, scientists can more efficiently identify a compound’s effectiveness and specificity for a given target. Identifying potential off-target interactions, is also an important component to compound profiling. Catching potential deleterious side-effects early in the development process significantly reduces risk and minimizes pursuit of dead-end candidates.Well designed compound screening can reveal a compound’s potential as a drug during development, before it advances to the more-costly stages of preclinical and clinical trials. Pharmacological profiling can also be used for quality control during the drug-development process or even to reprofile a drug to determine secondary therapeutic activities that lead to new ways of using an existing drug.
Caliper provides a comprehensive suite of automation solutions for compound profiling. Caliper’s RapidPlate Liquid Handler can quickly and precisely reformat 96- and 384-well plates (96 to 384 or 384 to 96) to perform various operations, including plate replication and assay assembly. In addition, the Sciclone ALH 3000 Liquid Handling Workstation provides 96- and 384-channel heads that can pipette low or high volumes for procedures that range from assay optimization to preparing proteins for mass spectrometry. Sciclone also includes an optional independent, eight-channel “Z8” pipettor for accessing individual wells along with an eight-channel, bulk-reagent dispenser for broadcasting reagents across a plate. Our compact Zephyr Filtration Workstation is optimized for automating filter binding assays, as well as plate replication.
Caliper has also revolutionized enzymatic assays such as kinases, phosphatases, proteases, phosphodiesterases with our LabChip EZ Reader and LabChip EZ Reader II. These systems are bench-top units designed to be used with our ProfilerPro Kinase Selectivity Assay Kits which contain all the necessary reagents and controls to carry out in-house kinase profiling.
In addition to providing in-house kinase profiling solutions, Caliper provides outsourced kinase profiling through its Discovery Alliances & Services division (CDAS) as well as a wide range of other in vitro profile programs including: General Side Effect Profile, GPCR profile, and Therapeutic Profiles (Cancer/Immunology, Pain/Inflammation, Cardiovascular, CNS).
CDAS has also created a database (Side Effect DataBase-SED) of known reference agents, marketed pharmaceuticals, failed drugs, and agrochemicals which have been profiled through a set of 60 GPCR, ion channel, nuclear receptor, transporter and enzyme assays. Many of these compound SEDSelect™ profiles are available for purchase online through our website.
Beyond the in vitro profiling services, CDAS has long recognized the value of animal models, and as a result has developed a comprehensive In Vivo Compound Profiling program. This customized battery of pharmacological tests—measuring over 450 parameters relevant to 15 therapeutic areas—involves three steps: 1) assess the therapeutic efficacy of optimized lead compounds and/or drug development candidates by analyzing their effects on key physiological functions in animals; 2) screen for potential side-effects caused by the administration of such compounds; and 3) discover disease indications for such compounds that were not previously known, thus expanding the market potential of those drug candidates.
When it comes to compound profiling, Caliper is uniquely positioned. From liquid handling instruments to bench top profiling solutions, our products help researchers efficiently identify potential drug candidates and move them through development. increasing the quality of compound leads. In addition, Caliper’s CDAS business unit provides customers with a comprehensive outsourcing solution, leveraging our in vivo and in vitro expertise.
