Published in Bioorg Med Chem Lett on February 13, 2013
The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One (2014) 0.81
A high through-put screen for small molecules modulating MCM2 phosphorylation identifies Ryuvidine as an inducer of the DNA damage response. PLoS One (2014) 0.76
AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther (2004) 2.08
Structure-based design of novel inhibitors of the MDM2-p53 interaction. J Med Chem (2012) 2.01
A biochemical rationale for the discrete behavior of nitroxyl and nitric oxide in the cardiovascular system. Proc Natl Acad Sci U S A (2003) 1.78
Efficient labeling of fission yeast Schizosaccharomyces pombe with thymidine and BUdR. Nucleic Acids Res (2003) 1.51
Rapid activation of ATM on DNA flanking double-strand breaks. Nat Cell Biol (2007) 1.49
DNA damage and decisions: CtIP coordinates DNA repair and cell cycle checkpoints. Trends Cell Biol (2010) 1.44
Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents. Bioorg Med Chem Lett (2006) 1.29
The physiological chemistry and biological activity of nitroxyl (HNO): the neglected, misunderstood, and enigmatic nitrogen oxide. Chem Res Toxicol (2005) 1.24
Suppressors of Bir1p (Survivin) identify roles for the chromosomal passenger protein Pic1p (INCENP) and the replication initiation factor Psf2p in chromosome segregation. Mol Cell Biol (2005) 1.20
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction. J Med Chem (2009) 1.19
New air-stable catalysts for general and efficient suzuki-miyaura cross-coupling reactions of heteroaryl chlorides. Org Lett (2006) 1.10
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. J Med Chem (2014) 1.08
On the total synthesis and determination of the absolute configuration of rishirilide B: exploitation of subtle effects to control the sense of cycloaddition of o-quinodimethides. Chemistry (2003) 1.07
Isovist analysis captures properties of space relevant for locomotion and experience. Perception (2007) 1.02
An aldol-based synthesis of (+)-peloruside a, a potent microtubule stabilizing agent. J Am Chem Soc (2009) 1.02
Anion-aromatic bonding: a case for anion recognition by pi-acidic rings. J Am Chem Soc (2002) 1.01
Comparison of the reactivity of nitric oxide and nitroxyl with heme proteins. A chemical discussion of the differential biological effects of these redox related products of NOS. J Inorg Biochem (2003) 1.00
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1). J Med Chem (2011) 0.98
Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitors. Biochim Biophys Acta (2011) 0.96
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. J Med Chem (2014) 0.93
Nitroxyl disulfides, novel intermediates in transnitrosation reactions. J Am Chem Soc (2003) 0.92
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice. J Med Chem (2008) 0.91
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J Med Chem (2008) 0.91
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold. J Med Chem (2008) 0.91
Theoretical evidence for enhanced NO dimerization in aromatic hosts: implications for the role of the electrophile (NO)(2) in nitric oxide chemistry. J Am Chem Soc (2005) 0.90
Rational design and binding mode duality of MDM2-p53 inhibitors. J Med Chem (2013) 0.89
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction. J Med Chem (2014) 0.88
Discovery of acetyl-coenzyme A carboxylase 2 inhibitors: comparison of a fluorescence intensity-based phosphate assay and a fluorescence polarization-based ADP Assay for high-throughput screening. Assay Drug Dev Technol (2007) 0.87
Improvement of the synthesis and pharmacokinetic properties of chromenotriazolopyrimidine MDM2-p53 protein-protein inhibitors. Bioorg Med Chem Lett (2010) 0.87
Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J Med Chem (2009) 0.87
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors. Bioorg Med Chem Lett (2007) 0.86
Conformation-dependent state selectivity in O-O cleavage of ONOONO: an "inorganic cope rearrangement" helps explain the observed negative activation energy in the oxidation of nitric oxide by dioxygen. J Am Chem Soc (2002) 0.86
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. J Med Chem (2012) 0.83
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists. J Med Chem (2014) 0.82
2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors. Bioorg Med Chem Lett (2012) 0.82
Baseline resolution of isomers by traveling wave ion mobility mass spectrometry: investigating the effects of polarizable drift gases and ionic charge distribution. J Mass Spectrom (2013) 0.81
A soluble base for the copper-catalyzed imidazole N-arylations with aryl halides. J Org Chem (2005) 0.81
Structure-activity relationship (SAR) investigations of tetrahydroquinolines as BKCa agonists. Bioorg Med Chem Lett (2010) 0.81
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives. J Med Chem (2011) 0.80
Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists. J Med Chem (2012) 0.80
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux. Bioorg Med Chem Lett (2012) 0.80
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility. Bioorg Med Chem (2014) 0.79
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2). Bioorg Med Chem Lett (2003) 0.79
One-pot microwave assisted preparation of pyrazoloquinazolinone libraries. Mol Divers (2003) 0.79
Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease. J Med Chem (2014) 0.79
Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors. J Med Chem (2012) 0.79
Peroxynitrate and peroxynitrite: a complete basis set investigation of similarities and differences between these NOx species. J Am Chem Soc (2003) 0.78
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J Med Chem (2007) 0.78
Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors. J Med Chem (2010) 0.78
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold. Bioorg Med Chem Lett (2012) 0.78
An efficient, regioselective amination of 3,5-disubstituted pyridine N-oxides using saccharin as an ammonium surrogate. Org Lett (2012) 0.78
Palladium-catalyzed coupling of aldehyde-derived hydrazones: practical synthesis of triazolopyridines and related heterocycles. Angew Chem Int Ed Engl (2010) 0.77
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core. Bioorg Med Chem Lett (2010) 0.77
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors. J Med Chem (2015) 0.77
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase. J Med Chem (2013) 0.77
Evaluation of a commercial packed bed flow hydrogenator for reaction screening, optimization, and synthesis. Beilstein J Org Chem (2011) 0.77
Assessment of the integrity of compounds stored in assay-ready plates using a kinase sentinel assay. Comb Chem High Throughput Screen (2013) 0.77
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem (2014) 0.76
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases. J Med Chem (2012) 0.76
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups. Bioorg Med Chem Lett (2011) 0.76
Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening. Chem Res Toxicol (2010) 0.76
Azole-based inhibitors of AKT/PKB for the treatment of cancer. Bioorg Med Chem Lett (2010) 0.76
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid. J Med Chem (2012) 0.76
C-nitroso donors of nitric oxide. J Org Chem (2009) 0.76
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides. J Med Chem (2007) 0.76
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7. Bioorg Med Chem Lett (2013) 0.76
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J Med Chem (2014) 0.76
Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists. Bioorg Med Chem Lett (2002) 0.76
Impact of glycation on antibody clearance. AAPS J (2014) 0.76
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J Med Chem (2014) 0.76
Palladium-catalyzed chemoselective monoarylation of hydrazides for the synthesis of [1,2,4]triazolo[4,3-a]pyridines. Org Lett (2010) 0.75
Synthesis and evaluation of thiazole carboxamides as vanilloid receptor 1 (TRPV1) antagonists. Bioorg Med Chem Lett (2005) 0.75
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. J Med Chem (2012) 0.75
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics. Bioorg Med Chem Lett (2010) 0.75
Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity. Bioorg Med Chem Lett (2013) 0.75
Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease. Bioorg Med Chem Lett (2013) 0.75
Correction to Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of β-Secretase. J Med Chem (2017) 0.75
High capacity homogeneous non-radioactive cortisol detection assays for human 11beta-hydroxysteroid dehydrogenase type 1. Assay Drug Dev Technol (2007) 0.75
Structure guided P1' modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease. Bioorg Med Chem Lett (2012) 0.75
Disubstituted 1-aryl-4-aminopiperidine library synthesis using computational drug design and high-throughput batch and flow technologies. ACS Comb Sci (2013) 0.75
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2. Bioorg Med Chem Lett (2011) 0.75
Fission yeast enters a joyful new era. Genome Biol (2002) 0.75
Crankshaft motion in a highly congested bis(triarylmethyl)peroxide. J Am Chem Soc (2004) 0.75
Remarkable efficiency of the aryne chemistry of (dehydro)octafluoro[2.2]paracyclophane when using the Cadogan method. J Org Chem (2007) 0.75