A growing team of groundbreaking scientists around the world are now sharing their lab notebooks online
Scaffold hopping is a strategy utilized in medicinal chemistry where the core chemical structure of a promising drug candidate is replaced isosterically, which leads to structurally novel compounds. There are many reasons for undertaking this exercise including; improving potency, changing physiochemical properties such as solubility and clogP, enhance ADME properties and to move into new Read More …
Access to large amounts of core building blocks is essential in drug discovery programs. It enables rapid synthesis of a series which can then give structure activity relationships (SAR) of the drugs and their target. SAR data allows medicinal chemists to determine the group(s) in a structure evoke a change in activity, whether positive or Read More …
One goal of the CaMKK2 project is to explore the chemistry and biology of novel hinge binders. Various hinge binders showing CaMKK2 inhibition have been identified in the literature and through testing of compounds synthesized in the SGC. Of note in this search was a recent publication by Price et al. (Bioorg. Med. Chem. Lett., Read More …
The goal of the Structural Genomics Consortium (SGC) is to discover and share selective small molecule inhibitors of protein kinases. Kinases have key roles in cell signaling, regulation of cell cycle progression, metabolism and other significant biological function. Cancers, immunological and metabolic diseases, among other ailments are caused by deregulation of kinase function. Protein kinases Read More …
