in vitro PHARMACOLOGY 2011 CATALOG - Cerep

196 in vitro pharmacology 2011 catalog
CEREP
standard profiles
At January 1, 2011, Cerep offers 15 standard profiles. While some, extensively used by many of our customers, remain the
same as in 2010, others have evolved to include widely requested assays.
Compared to 2010:
Two new profiles have been created, the Cellular functional GPCR profile, designed to identify potential off-target activities
early in the drug discovery process, and the PDE High-throughput profile, designed to determine the inhibitory activity and
selectivity of compounds on the PDE superfamily.
The ADME-Tox Option II [Lead Selection/Prioritization] profile, has been expanded to incorporate a complete panel of
CYP isozymes for evaluation of a compound’s CYP inhibition potential.
❚ ExpresS profile [55 binding assays]
Ref. P1
Suggested testing: 10 µM (n=2)
Q 5 business days
The ExpresS Profile is a fast turnaround selectivity/specificity profile drawn from the Highthroughput
profile (see below). The majority of the 55 binding assays in the ExpresSProfile panel
are human recombinant receptors.
With a one week turnaround time, the ExpresS Profile greatly accelerates the "risk assessment"
of lead compounds.
❚ High-throughput profile [80 binding assays]
Ref. P3
Suggested testing: 10 µM (n=2)
Q 2 weeks
The High-throughput profile consists of a broad collection of 80 transmembrane and soluble
receptors, ion channels and monoamine transporters. It has been specifically designed to
provide information not only on potential limitations or liabilities of drug candidates, but also
for off-target activity identification.
Used either for risk assessment, selectivity/specificity, or for identification of new activities,
the high-throughput profile is a rapid and cost effective way of prioritizing the most promising
compounds in hit-to-lead selection process.
Cellular functional GPCR assays are available on 66 % of the assays in this profile.
❚ ExpresS DIVERSITY KINASE profile [48 enzyme assays]
Ref. P10
Suggested testing: 10 µM (n=2)
Q 5 business days
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
The ExpresS Diversity kinase profile is a fast turnaround profile containing 48 biochemical kinase
assays. The assays were selected taking into consideration the diversity of assay families and the
automation level of each assay to maintain the one week turnaround time. As Kinase-inhibitory
compounds often interact with a spectrum of kinases, identification of those with improved selectivity
is essential. This need can be supported by rapid profiling of your libraries on ExpresS Diversity
kinase profile.
All assays are part of the Comprehensive kinase profile (See page 198).
For list of assays included in standard profiles and updated information:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time