Although GPCRs are recognized as the most successful class of druggable targets in the human genome, marketed drugs modulate only about 80 proteins from this very large family. In recognition of their prominence in drug discovery efforts, we have prioritized GPCRs for our next strategic growth phase. We plan to identify chemical probes and best-available compounds for as many of these receptors as we can. We will also highlight commonly used but nonselective compounds (historic compounds) that researchers mistakenly apply as probes to study GPCRs.
April 7, 2017
March 17, 2017
The Shamrock, a three-leaf clover, is the traditional symbol for the Irish and often appears in and around St. Patrick’s Day celebrations. Some rare clovers have four leaves, and they are considered lucky. Like four-leaf clovers, quality chemical probes are a rarity, and we are dedicated to finding these ‘lucky’ compounds on behalf of our users. Enjoy the parades and other festivities this weekend; if you are a fan of the NCAA, enjoy the madness that March brings; and check in with us to find your chemical probes before you start your next experiment.
February 24, 2017
We were awed this week when scientists reported the discovery of seven earth-like planets just 39 light-years away. This discovery highlights just how many exciting things remain for us to discover and explore. While discoveries of this magnitude are rare and should be celebrated, we believe it’s also important to celebrate the incremental achievements that make such awesome discoveries possible.
February 17, 2017
The Chemical Probes Portal is excited to announce a growth campaign focusing on the Bromodomain and BCL2 family proteins. These classes of proteins are known to contain important drug targets, particularly for cancer, and have seen a lot of chemical probe activity.
Bromodomains are epigenetic proteins that ‘read’ information conveyed through chromatin modifications by binding to acetylated histones. Through the recruitment of protein partners, these proteins impact gene expression.
February 10, 2017
February 3, 2017
January 27, 2017
This month, we updated our PARP inhibitor records based on a new and important publication reporting potency and selectivity information for 11 PARP family inhibitors that are commonly used as chemical probes (Thorsell et al., 2016). This paper reports several key new observations about the activity of these inhibitors, prompting us to revisit and update the probe and historic compound records.
January 13, 2017
The Chemical Probes Portal is excited to announce a growth campaign focusing on the Tyrosine Kinases. This class of proteins is already known to contain important drug targets, as the class includes many growth factor receptors that drive tumor growth. Tyrosine kinases come in two basic flavors, receptor and non-receptor kinases, and not all of them have been well studied.
January 10, 2017
Portal News is now available http://eepurl.com/cwOnAf. In this issue, we highlight how the rigorous application of chemical probes in biological systems can lead to better probes and improve drug discovery efforts through a case study of ABT-199 (venetoclax). We also highlight two programs that we rolled out late in 2016: Historic Compounds and Vendor Links.
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December 12, 2016
The Portal now features a new class of compounds called Historic Compounds. These small molecules are typically non-selective or not sufficiently potent compared with other available chemical probes to merit the probe designation.