Backbone N-methylation is common among peptide natural products and has a substantial
impact on both the physical properties and the conformational states of cyclic peptides. …

The measurement of the effect of new chemical entities on human UDP-glucuronosyltransferase
(UGT) marker activities using in vitro experimentation represents an important …

The importance of uridine 5‘-diphosphate-glucuronosyltranferases (UGT) 2B15 and other
UGT enzymes (1A1, 1A6, and 1A9) in glucuronidating acetaminophen (APAP) is demonstrated…

In vitro metabolism/bioactivation of structurally related central nervous system agents
nefazodone (hepatotoxin) and aripiprazole (nonhepatotoxin) were undertaken in human liver …

The contribution of drug metabolites to the pharmacologic and toxicologic activity of a drug
can be important; however, for a variety of reasons metabolites can frequently be difficult to …

Abrocitinib is an oral once-daily Janus kinase 1 selective inhibitor being developed for the
treatment of moderate-to-severe atopic dermatitis. This study examined the disposition of …

Gemfibrozil coadministration generally results in plasma statin area under the curve (AUC)
increases, ranging from moderate (2- to 3-fold) with simvastatin, lovastatin, and pravastatin to …

The synthesis and SAR for a series of diaminopyrimidines as PYK2 inhibitors are described.
Using a combination of library and traditional medicinal chemistry techniques, a FAK-…

… The samples were then centrifuged at 14 000 rpm (15 000 g) for 10 min, supernatants
removed, mixtures dried under N 2 and reconstituted in mobile phase consisting of 84% 20 mm …

N-Methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide (axitinib) is an
oral inhibitor of vascular endothelial growth factor receptors 1–3, which is approved for the …