An automated multistep high-throughput screening assay for the identification of lead inhibitors of the inducible enzyme mPGES-1.

Identification and development of mPGES-1 inhibitors: where we are at? Future Med Chem (2011) 1.04

Interconnection of competence, stress and CiaR regulons in Streptococcus pneumoniae: competence triggers stationary phase autolysis of ciaR mutant cells. Mol Microbiol (2004) 2.10

Microsomal prostaglandin E synthase-1 is a major terminal synthase that is selectively up-regulated during cyclooxygenase-2-dependent prostaglandin E2 production in the rat adjuvant-induced arthritis model. J Immunol (2003) 1.35

Deletion of microsomal prostaglandin E2 (PGE2) synthase-1 reduces inducible and basal PGE2 production and alters the gastric prostanoid profile. J Biol Chem (2004) 1.29

Statistical and graphical methods for quality control determination of high-throughput screening data. J Biomol Screen (2003) 1.27

MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. J Pharmacol Exp Ther (2008) 1.23

Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886. Bioorg Med Chem Lett (2005) 1.15

Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. Br J Pharmacol (2002) 1.13

Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization. Nat Chem Biol (2013) 1.10

Mutational dissection of the S/T-kinase StkP reveals crucial roles in cell division of Streptococcus pneumoniae. Mol Microbiol (2012) 1.09

Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. Bioorg Med Chem Lett (2007) 1.05

Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem (2011) 0.97

Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438). Bioorg Med Chem Lett (2009) 0.95

Genome-scale analysis of Mycoplasma agalactiae loci involved in interaction with host cells. PLoS One (2011) 0.94

In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother (2013) 0.93

Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors. Bioorg Med Chem Lett (2009) 0.93

Substituted coumarins as potent 5-lipoxygenase inhibitors. Bioorg Med Chem Lett (2006) 0.93

Critical role of dispensable genes in Mycoplasma agalactiae interaction with mammalian cells. Infect Immun (2010) 0.93

Tyrosine-kinases in bacteria: from a matter of controversy to the status of key regulatory enzymes. Amino Acids (2009) 0.92

Pharmacological characterization of a selective COX-2 inhibitor MF-tricyclic, [3-(3,4-difluorophenyl)-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone], in multiple preclinical species. Eur J Pharmacol (2007) 0.92

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing. J Biol Chem (2007) 0.92

Thiazole analog as stearoyl-CoA desaturase 1 inhibitor. Bioorg Med Chem Lett (2009) 0.88

In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in dogs with experimentally induced synovitis. Am J Vet Res (2004) 0.87

In vivo inhibition of serine protease processing requires a high fractional inhibition of cathepsin C. Mol Pharmacol (2008) 0.86

Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors. Bioorg Med Chem Lett (2010) 0.83

Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. Bioorg Med Chem Lett (2002) 0.82

Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods. J Biomol Screen (2011) 0.82

SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors. Bioorg Med Chem Lett (2010) 0.81

Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. Bioorg Med Chem Lett (2002) 0.81

5-oxo-6,8,11,14-eicosatetraenoic acid stimulates the release of the eosinophil survival factor granulocyte/macrophage colony-stimulating factor from monocytes. J Biol Chem (2004) 0.81

Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy. Bioorg Med Chem Lett (2011) 0.80

Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C. Bioorg Med Chem Lett (2009) 0.80

Trisubstituted ureas as potent and selective mPGES-1 inhibitors. Bioorg Med Chem Lett (2011) 0.79

Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein. Bioorg Med Chem Lett (2008) 0.79

A multiplexed cell assay in HepG2 cells for the identification of delta-5, delta-6, and delta-9 desaturase and elongase inhibitors. J Biomol Screen (2010) 0.79

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines. Bioorg Med Chem Lett (2011) 0.78

Pyridazinones as selective cyclooxygenase-2 inhibitors. Bioorg Med Chem Lett (2003) 0.78

3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. Bioorg Med Chem Lett (2003) 0.78

Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. Bioorg Med Chem Lett (2003) 0.78

Discovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series. Bioorg Med Chem Lett (2011) 0.78

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines. Bioorg Med Chem Lett (2011) 0.78

Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors. Bioorg Med Chem Lett (2003) 0.77

Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1. Bioorg Med Chem Lett (2010) 0.77

Design and synthesis of potent, isoxazole-containing renin inhibitors. Bioorg Med Chem Lett (2012) 0.76

Impact of primer-induced conformational dynamics of HIV-1 reverse transcriptase on polymerase translocation and inhibition. J Biol Chem (2011) 0.76

The discovery and synthesis of potent zwitterionic inhibitors of renin. Bioorg Med Chem Lett (2011) 0.76

Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. Bioorg Med Chem Lett (2011) 0.75

Identification of an indole series of prostaglandin D2 receptor antagonists. Bioorg Med Chem Lett (2006) 0.75

Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors. Bioorg Med Chem Lett (2011) 0.75

Resorufin butyrate as a soluble and monomeric high-throughput substrate for a triglyceride lipase. J Biomol Screen (2011) 0.75

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines. Bioorg Med Chem Lett (2011) 0.75

3,4-Diarylpiperidines as potent renin inhibitors. Bioorg Med Chem Lett (2012) 0.75

Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors. Bioorg Med Chem Lett (2011) 0.75

Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. Bioorg Med Chem Lett (2005) 0.75

Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile. Bioorg Med Chem Lett (2002) 0.75

In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in cats with lipopolysaccharide-induced pyrexia. Am J Vet Res (2005) 0.75