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In Vitro Pharmacology >> Kinases >> Biochemical

Unmatched expertise and experience in kinase drug discovery

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Unmatched expertise and experience in kinase drug discovery

Our direct filter-binding radiometric kinase activity assay has long been established as the most reliable, robust gold-standard assay against which all other assay formats are measured. Many of our clients prefer to use our KinaseProfiler™ services to avoid the complications of on-site radioactive licensing while enjoying the benefits of this assay format performed by the pioneers in commercial screening. We can also utilize TR-FRET technology to measure substrate phosphorylation when a greater level of throughput is desired to support high throughput screens.

Our IC50Profiler™ service enables you to follow up hits identified from a standard KinaseProfiler™ study by determining an IC50 value for your test compound against the kinase of interest. Our IC50 curves consist of 9 test compound concentrations tested at half-log dilutions along with vehicle control wells. Your report will include a graphical representation of the data and the estimated IC50 value.

The combined expertise of Cerep, Panlabs and KinaseProfiler™ allows you to expand your outsourcing choices while enjoying the confidence that your results are being securely provided by a professional team dedicated to the integrity of your research. Being a preferred partner for Pharma, Eurofins is the natural choice for your kinase screening and profiling needs.

Advantages of KinaseProfiler™ services:

  • One week guaranteed turnaround time to drive SAR*
  • Choose from over 600 radiometric and TR-FRET (HTRF® or LANCE®) kinase activity assays, one of the largest panels in the industry
  • Unparalleled quality control
    • Low variation across replicates (including controls)
  • Selection of ATP concentrations, including Km and 10 µM
  • Single point or full 10-point IC50 curves
  • HTRF® lipid PI3 Kinase assays
  • Flexibility to include non-standard solvents or pre-incubation
  • Reserve assay slots to allow a steady flow of compounds for the fastest possible throughput

 Figure 1. Differences in potency of imatinib (Gleevec®) inhibition of wild-type and mutant Abl

Activity of wild-type Abl and T315I Abl mutant was measured via incorporation of radioactivity from 10 μM γ-[32P]-ATP into EAYAAPFAKKK peptide in the presence of the indicated compound concentrations.

*The guarantee must be requested at the time of ordering and is available for most projects, including KinaseProfiler™, IC50 Profiler™, and PhosphataseProfiler™. Eligible projects are activated each Friday and data reports are delivered on or before the following Friday.

**Services mentioned in report for Cerep, EMD Millipore and Ricercia Biosciences are now operated by Eurofins