Ishida, Akiharu published the artcileDesign, synthesis, and biological evaluation of novel somatostatin receptor subtype-2 agonists: Optimization for potency and risk mitigation of hERG and phospholipidosis, Safety of tert-Butyl piperidin-4-ylcarbamate, the main research area is ERG phospholipidosis somatostatin receptor subtype 2 agonist; Agonist; G-protein coupled receptor (GPCR); PKa; Phospholipidosis; SSTR2; Somatostatin; cLogP; hERG.
Somatostatin receptors are members of G-protein coupled receptor superfamily. Receptors can be classified into five subtypes, SSTR1 to 5. The highly potent and orally active SSTR2 agonist 7, which had been identified by our group, was found out to have toxicol. liabilities such as hERG inhibition and phospholipidosis (PLD). We investigated the relationship between in silico physicochem. properties and hERG and PLD, and explored well-balanced agonists to identify amide 19 and benzimidazole 30. As a result of this exploration, we found out that the value of (cLogP) [2] + (pKa) [2] needs to be less than 110 to mitigate the liabilities.
Bioorganic & Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (ERG). 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Safety of tert-Butyl piperidin-4-ylcarbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem