Innovating Your Drug Discovery

Chemical Probes Portal – Know Your Selectivity!

The Chemical Probes Portal is a new online resource for anyone using tool compounds in their research.  We can learn a lot from high quality chemical probes that are potent, selective, and cell-permeable inhibitors of protein function. Chemical probes with sufficient selectivity enable target validation by defining the role of that target when used in phenotypic assays and disease models.

Many useful chemical probes, however, are only partially selective.  They may not meet the criteria set forth by the Structural Genomics Consortium (SGC) for their chemical probes:

  • in vitro potency of <100 nM
  • >30-fold selectivity versus other subfamilies
  • demonstration of on-target effect in cells at < 1 μM

Partially selective tools can still be useful, but require more careful data interpretation. In some cases they should be used only in combination with other selective probes or with genetic tools.

This Is Why It Is Important to Know the Selectivity of Chemical Probes

Although the information on probe selectivity and activity in cell-based assays is critical to accurate experimental conclusions, these details are neither easily nor consistently available.  The information may be spread piecemeal among a number of publications, behind firewalls, or not published at all.

In order to address the need for ready access to this information, the Chemical Probes Portal has been established as a community-driven resource to provide recommendations on the best available chemical probes and guidance for their use. Kudos to the Wellcome Trust for their support and to the SGC, Institute of Cancer Research, and Broad Institute for their endorsement.  As a community resource, it will be most effective if all of us contribute.

Additional Reading on the Role and Value of Chemical Probes

DiscoverX Offers the Broadest Range of Profiling Panels for Validation of Chemical Probes