Published in Bioorg Med Chem Lett on April 01, 2005
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An MMP13-selective inhibitor delays primary tumor growth and the onset of tumor-associated osteolytic lesions in experimental models of breast cancer. PLoS One (2012) 0.93
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Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor. J Med Chem (2012) 0.92
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Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors. J Med Chem (2011) 0.90
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Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors. J Med Chem (2015) 0.89
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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg Med Chem Lett (2011) 0.87
Modulation of NMDA receptor function by inhibition of D-amino acid oxidase in rodent brain. Neuropharmacology (2011) 0.87
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem (2011) 0.87
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Potent, selective pyrimidinetrione-based inhibitors of MMP-13. Bioorg Med Chem Lett (2006) 0.86
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Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1. Bioorg Med Chem Lett (2004) 0.86
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Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy. Cancer Res (2003) 0.85
Pyridone-conjugated monobactam antibiotics with gram-negative activity. J Med Chem (2013) 0.85
Biophysical and biochemical approach to locating an inhibitor binding site on cholesteryl ester transfer protein. Bioconjug Chem (2008) 0.85
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3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. Bioorg Med Chem Lett (2003) 0.84
Effect of tumor necrosis factor-alpha converting enzyme (TACE) and metalloprotease inhibitor on amyloid precursor protein metabolism in human neurons. J Neurochem (2002) 0.84
Engineering autoactivating forms of matrix metalloproteinase-9 and expression of the active enzyme in cultured cells and transgenic mouse brain. Biochemistry (2002) 0.84
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. Bioorg Med Chem Lett (2003) 0.84
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. Bioorg Med Chem Lett (2009) 0.84
Discovery of Dap-3 polymyxin analogues for the treatment of multidrug-resistant Gram-negative nosocomial infections. J Med Chem (2013) 0.83
Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase. Bioorg Med Chem Lett (2013) 0.83
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The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene. Protein Sci (2007) 0.83
Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase. J Med Chem (2012) 0.83
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists. Bioorg Med Chem Lett (2006) 0.82
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency. Bioorg Med Chem Lett (2013) 0.82
How paired is paired? Comparing nitrate concentrations in three iowa drainage districts. J Environ Qual (2013) 0.82
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Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections. J Med Chem (2009) 0.81
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents. Bioorg Med Chem Lett (2012) 0.81
Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections. Bioorg Med Chem Lett (2012) 0.81
Molecular features crucial to the activity of pyrimidine benzamide-based thrombopoietin receptor agonists. Bioorg Med Chem Lett (2008) 0.80