First set of selected compounds against DRAK2 kinase

Several compounds derived from thienopyrimidine scaffolds were recently synthesized to be tested as inhibitors of DRAK2/STK17B kinase. Among these, a set of 12 were selected to determine their potency as IC50 values on a DRAK2 cellular assay. These compounds have different functional groups around the phenyl ring and variation in the position of the sulfur Read More …

Synthesis of a selective inhibitor for DRAK2 kinase

Towards the SGC goal of creating a kinase chemogenomic set (KCGS) we have been receiving and profiling kinase inhibitors donated by pharmaceutical companies. One such compound is PFE-PKIS 43 (Scheme 1a). We received this compound from Pfizer and it was screened against 403 kinases at DiscoverX. This compound, originally synthesized and published as part of Read More …

Chemical probes for understudied kinases

One of the ongoing projects at SGC-UNC is the development of chemical probes for understudied kinases (e.g. MST1-4, TAOK1-3, DCAMKL1, MAP3K2 and MAP3K3). A chemical probe is defined as a small molecule that selectively and potently modulates a protein’s function. Generating chemical probes for understudied kinases is important so we can further understand the biology Read More …