Millipore Technical Publications |
 | DS- TB2777EN00 | |
The Importance of Being Profiled: Improving Drug Candidate Safety and Efficacy Using Cross-target Profiling | ||
| Lit No: | TB2777EN00 | |
| Year: | 2011 | |
| Profiling of putative lead compounds against a
representative panel of important enzymes, receptors, ion
channels and transporters is an excellent way to establish
a preliminary view of potential issues that might later
hamper development. An early idea of which off-target
activities must be minimized can save valuable time and
money during the preclinical lead optimization phase if
pivotal questions are asked beyond the usual profiling
at hERG. The best data for critical evaluation of activity
at GPCRs and ion channels is obtained using functional
assays, since binding assays cannot detect all interactions
and do not provide information on whether the
interaction is that of an agonist, antagonist, or allosteric
modulator. This overview discusses the benefits of in
vitro assays, specific decision points where profiling can
be of immediate benefit, and highlights relevant profiling
services offered by EMD Millipore .
Click the PDF above for the full document. | |
| |
| |
