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. EZM0414 is a potent, orally active, and selective inhibitor of the SET domain containing 2 (SETD2) protein. SETD2 protein is a histone methyltransferase, that acts in various cellular processes, including transcriptional elongation and regulation, alternative RNA splicing, and DNA damage repair. SETD2 also demonstrates tumor suppressor behavior. Using the strategy “escaping from flatland” led to drug candidate EZM0414 which shows good pharmacokinetics and robust pharmacodynamic activity in a xenograft model.

You can find the analogs to this molecule here!

2. MK-0159 is an orally bioavailable and selective CD38 enzymatic inhibitor, that showed potent cellular inhibition in human endothelial and epithelial cells. CD38 expression is upregulated in age-associated inflammation and some metabolic diseases. It is also known that CD38 is activated upon ischemia/reperfusion (I/R). MK-0159 shows good microsomal stability, increases NAD+, and reduces ADPR in blood and heart. MK-0159 demonstrates strong protection from myocardial damage upon cardiac I/R injury in mice.

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!