We are happy to continue our series of posts which are inspired by Drug Hunter’s “Molecules of the Month”!
Here are two molecules that were recently highlighted by Drug Hunter!
1. GDC-2394 is an oral, potent, and selective inhibitor of NLRP3, a member of the NOD-like family of receptors (NLRs). The study of the NLRP3 inflammasome inhibition is still actual because numerous inflammatory and autoimmune diseases are related to its wrong activation. Using lipophilic ligand efficiency (LLE) optimization a series of sulfonylureas were identified. Studies in preventing renal and liver toxicity led to the identification of GDC-2394. Currently, this drug candidate displays suitable in vitro and in vivo safety profiles for promotion in further human clinical trials.
You can find the analogs to this molecule here!
2. BAY-069 is a potent branched-chain amino acid transaminases 1/2 (BCAT1/2) inhibitor. The BCATs are enzymes that are involved in the synthesis and breakdown of branched-chain amino acids and are known to play a key role in different cancer types. BAY-069 is an example of a new structural class of BCAT1/2 inhibitors identified from SAR analysis and X-ray crystallographic studies. Due to the unique selectivity profile in various in vitro panels, BAY-069 was accepted as a donated chemical probe by the SGC as a tool compound for a better understanding of BCAT inhibition in tumor metabolism.
You can find the analogs to this molecule here!
Use chem-space.com/search to find off-the-shelf and Make-on-Demand molecules of your interest!