Maria Kaleta

TL;DR: Novel biphenyloxy-alkyl derivatives of piperidine and azepane were synthesized and evaluated for their binding properties at the human histamine H3 receptor and demonstrated easy hydroxylation of the biphenYL ring.

TL;DR: A series of twenty new tert-amyl phenoxyalkylamine derivatives was synthesized and evaluated on their binding properties at human histamine H3 receptor (hH3R) to estimate "drug-likeness" of selected compounds in silico and experimental evaluation of lipophilicity, metabolic stability and cytotoxicity was performed.

TL;DR: This study focuses on the design, synthesis, molecular modeling and biological evaluation of a novel group of alkyl-1,3,5-triazinyl-methylpiperazines, which exhibited hH4R affinity with a Ki of 160 nM and behaved as antagonist in functional assays.

TL;DR: GPR18 inactive form homology model was built on the basis of the evolutionary closest homologous template: Human P2Y1 Receptor crystal structure and showed active/nonactive ligands differentiating properties with acceptable confidence, enabling preliminary assessment of proteinligand interactions for a set of previously described ligands.