 Molecular
Pharmacology Profiles The direct mechanism of action
of a drug via its interaction with its various targets
and off-target sites is critical
to understanding the gene expression changes that it induces.
In order to employ the expression data optimally to make
accurate
predictions of potential efficacy and toxicity of leads and
drug candidates, all paradigm compounds are evaluated in
a large standardized set of key molecular pharmacology assays
to generate full in vitro activity and target interaction
profiles. The fact that there is a homogeneous set of assays
performed under uniform conditions makes it possible for
the data to act as a reference set of information against
which
the assay profiles of novel compounds may be compared.
The current release of the database includes
130 key pharmacology bioassays performed by Ricerca Biosciences,
a DrugMatrix partner and the world leader in this area. The
initial assays were chosen to demonstrate off-target effects,
including toxicology and drug metabolism. We
have chosen assays
for current research targets and target sites of leading
drugs. In this first release, the profile consists of 90
receptor-type
binding assays, 33 enzyme assays, and 7 ADME assays. The
receptor assays cover a wide selection of receptor types
in all the major therapeutic areas.
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