Evaluation and optimization of drug metabolism and pharmacokinetic data plays an important
role in drug discovery and development and several reliable in vitro ADME models are …

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a
novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been …

In vitro covalent binding assessments of drugs have been useful in providing retrospective
insights into the association between drug metabolism and a resulting toxicological response. …

The therapeutic benefits of the antidepressant nefazodone have been hampered by several
cases of acute hepatotoxicity/liver failure. Although the mechanism of hepatotoxicity remains …

In vitro covalent binding studies in which xenobiotics are shown to undergo metabolism-dependent
covalent binding to macromolecules have been commonly used to shed light on the …

The primary pathway of clearance of the methylenedioxyphenyl-containing compound and
selective serotonin reuptake inhibitor paroxetine in humans involves P450 2D6-mediated …

Therapy with the antidepressant trazodone has been associated with several cases of
idiosyncratic hepatotoxicity. While the mechanism of hepatotoxicity remains unknown, it is …

The current study examined the bioactivation potential of a nonpeptidyl thrombopoietin
receptor agonist, 1-(3-chloro-5-((4-(4-fluoro-3-(trifluoromethyl)phenyl)thiazol-2-yl)carbamoyl)…

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 synthesis and structure−activity relationship studies on 5-trifluoromethylpyrido[4,3-d]pyrimidin-4(3H)-ones
as antagonists of the human calcium receptor (CaSR) have been recently …