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. Compound 23 is an oral and highly selective cathepsin K (Cat K) inhibitor. Cat K is a cysteine protease involved in bone metabolism and is an attractive therapeutic target for disease-modifying osteoarthritis. Lead optimization of previously known preclinical compound led to Compound 23 containing oxazole moiety. It shows better selectivity profiles and inhibits Cat K in “in vivo” disease studies by reducing levels of urinary C-telopeptide.
You can find the analogs to this molecule here!
2. ACT-660602 is an orally active antagonist of chemokine receptor CXCR3. CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in different pathologies, in particular autoimmune diseases. There are three chemokine ligands (CXCL9, CXCL10, CXCL11) that activate it. Furthermore, CXCR3 enables the recruitment of immune cell subsets that leads to inflamed tissue damage and organ destruction. Lead optimization with structural modifications after HTS investigations led to ACT-660602 which demonstrates high biological potency in inhibiting cell migration with improvements of the metabolic stability and hERG issue.
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!
