Published in Bioorg Med Chem Lett on March 03, 2010
Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits. ACS Chem Neurosci (2013) 1.24
Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators. ACS Med Chem Lett (2010) 1.13
Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease. Drug Discov Today (2013) 0.90
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. Bioorg Med Chem Lett (2011) 0.89
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents. J Med Chem (2015) 0.85
Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2. J Med Chem (2015) 0.83
Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators. ACS Med Chem Lett (2012) 0.82
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators. Bioorg Med Chem Lett (2014) 0.80
Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators. ACS Med Chem Lett (2014) 0.78
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett (2005) 3.50
Pharmacokinetics and absorption of posaconazole oral suspension under various gastric conditions in healthy volunteers. Antimicrob Agents Chemother (2008) 2.70
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J Med Chem (2004) 2.46
DISC1 (Disrupted-In-Schizophrenia 1) is a centrosome-associated protein that interacts with MAP1A, MIPT3, ATF4/5 and NUDEL: regulation and loss of interaction with mutation. Hum Mol Genet (2003) 2.39
A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. J Pharmacol Exp Ther (2004) 2.17
Sex-dependent liver gene expression is extensive and largely dependent upon signal transducer and activator of transcription 5b (STAT5b): STAT5b-dependent activation of male genes and repression of female genes revealed by microarray analysis. Mol Endocrinol (2006) 2.17
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg Med Chem Lett (2006) 2.17
Medial patella retinaculum plasty for treatment of habitual patellar dislocation in adolescents. Int Orthop (2012) 2.02
N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc Natl Acad Sci U S A (2003) 1.96
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation. Proc Natl Acad Sci U S A (2009) 1.87
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. J Med Chem (2010) 1.76
Inhibition of a mitotic motor protein: where, how, and conformational consequences. J Mol Biol (2004) 1.58
Molecular insights into the pathogenesis of Alzheimer's disease and its relationship to normal aging. PLoS One (2011) 1.57
Single-dose phase I study to evaluate the pharmacokinetics of posaconazole in new tablet and capsule formulations relative to oral suspension. Antimicrob Agents Chemother (2012) 1.57
Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse. J Neurosci (2003) 1.55
LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease. Proc Natl Acad Sci U S A (2006) 1.50
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett (2008) 1.44
The PI3K/Akt pathway: recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors. Curr Cancer Drug Targets (2008) 1.40
The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation. Curr Top Med Chem (2005) 1.37
Anidulafungin pharmacokinetics and microbial response in neutropenic mice with disseminated candidiasis. Antimicrob Agents Chemother (2006) 1.34
Long-term renormalization of chromatic mechanisms following cataract surgery. Vis Neurosci (2004) 1.32
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist. J Med Chem (2008) 1.28
Identification of genetic pathways activated by the androgen receptor during the induction of proliferation in the ventral prostate gland. J Biol Chem (2003) 1.28
Molecular ecology of pyrethroid knockdown resistance in Culex pipiens pallens mosquitoes. PLoS One (2010) 1.27
Population pharmacokinetics of micafungin in adult patients. Diagn Microbiol Infect Dis (2007) 1.27
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. Bioorg Med Chem Lett (2005) 1.27
Effect of varying amounts of a liquid nutritional supplement on the pharmacokinetics of posaconazole in healthy volunteers. Antimicrob Agents Chemother (2009) 1.27
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. Bioorg Med Chem Lett (2002) 1.23
Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators. Bioorg Med Chem Lett (2009) 1.22
Role of STAT5a in regulation of sex-specific gene expression in female but not male mouse liver revealed by microarray analysis. Physiol Genomics (2007) 1.20
Comparison of drug distribution images from whole-body thin tissue sections obtained using desorption electrospray ionization tandem mass spectrometry and autoradiography. Anal Chem (2008) 1.20
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP. Bioorg Med Chem Lett (2005) 1.19
Inhibition of calcineurin-mediated endocytosis and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors prevents amyloid beta oligomer-induced synaptic disruption. J Biol Chem (2009) 1.18
Multifocal electroretinogram: age-related changes for different luminance levels. Graefes Arch Clin Exp Ophthalmol (2002) 1.17
Adaptation in human visual cortex as a mechanism for rapid discrimination of aversive stimuli. Neuroimage (2007) 1.13
A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. Proc Natl Acad Sci U S A (2004) 1.12
Tumor tracking and motion compensation with an adaptive tumor tracking system (ATTS): system description and prototype testing. Med Phys (2008) 1.11
Retracted A regulatory circuit mediating convergence between Nurr1 transcriptional regulation and Wnt signaling. Mol Cell Biol (2007) 1.11
Liquid microjunction surface sampling probe electrospray mass spectrometry for detection of drugs and metabolites in thin tissue sections. J Mass Spectrom (2008) 1.07
Androgen-mediated improvement of body composition and muscle function involves a novel early transcriptional program including IGF1, mechano growth factor, and induction of {beta}-catenin. J Mol Endocrinol (2009) 1.06
Recent progress in the development of ATP-competitive and allosteric Akt kinase inhibitors. Curr Top Med Chem (2007) 1.06
Impact of pH on plasma protein binding in equilibrium dialysis. Mol Pharm (2008) 1.05
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. J Med Chem (2008) 1.03
Beyond amyloid: the next generation of Alzheimer's disease therapeutics. Mol Interv (2007) 1.01
Pharmacokinetics of posaconazole administered orally or by nasogastric tube in healthy volunteers. Antimicrob Agents Chemother (2009) 1.00
High-throughput screening by RNA interference: control of two distinct types of variance. Cell Cycle (2007) 1.00
Transcriptional profiling of Medicago truncatula under salt stress identified a novel CBF transcription factor MtCBF4 that plays an important role in abiotic stress responses. BMC Plant Biol (2011) 0.99
Pharmacokinetics of different dosing strategies of oral posaconazole in patients with compromised gastrointestinal function and who are at high risk for invasive fungal infection. Antimicrob Agents Chemother (2012) 0.98
Future-oriented decision-making in Generalized Anxiety Disorder is evident across different versions of the Iowa Gambling Task. J Behav Ther Exp Psychiatry (2009) 0.98
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity. Bioorg Med Chem Lett (2007) 0.98
miR-124 radiosensitizes human glioma cells by targeting CDK4. J Neurooncol (2013) 0.97
Increased nuclear factor-erythroid 2 p45-related factor 2 activity protects SH-SY5Y cells against oxidative damage. J Neurochem (2005) 0.97
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand. Bioorg Med Chem Lett (2006) 0.97
Methionine aminopeptidases type I and type II are essential to control cell proliferation. J Cell Biochem (2005) 0.97
Androgenic induction of growth and differentiation in the rodent uterus involves the modulation of estrogen-regulated genetic pathways. Endocrinology (2004) 0.96
Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series. Bioorg Med Chem Lett (2011) 0.96
Involvement of ERK 1/2 activation in electroacupuncture pretreatment via cannabinoid CB1 receptor in rats. Brain Res (2010) 0.96
Solution-phase synthesis of single-crystalline iron phosphide nanorods/nanowires. J Am Chem Soc (2004) 0.96
Serine proteinase over-expression in relation to deltamethrin resistance in Culex pipiens pallens. Arch Biochem Biophys (2005) 0.95
Genome sequence of Anopheles sinensis provides insight into genetics basis of mosquito competence for malaria parasites. BMC Genomics (2014) 0.95
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors. Bioorg Med Chem Lett (2008) 0.95
A mild method for the formation and in situ reaction of imidoyl chlorides: conversion of pyridine-1-oxides to 2-aminopyridine amides. Org Lett (2002) 0.95
A highly efficient Ziehl-Neelsen stain: identifying de novo intracellular Mycobacterium tuberculosis and improving detection of extracellular M. tuberculosis in cerebrospinal fluid. J Clin Microbiol (2012) 0.95
Worry, generalized anxiety disorder, and emotion: evidence from the EEG gamma band. Biol Psychol (2008) 0.94
Positive resources for combating depressive symptoms among Chinese male correctional officers: perceived organizational support and psychological capital. BMC Psychiatry (2013) 0.94
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem (2012) 0.94
Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding. Bioorg Med Chem Lett (2009) 0.94
DISC1 (Disrupted in Schizophrenia-1) is expressed in limbic regions of the primate brain. Neuroreport (2003) 0.94
Comparison of 30-min and 3-h infusion regimens for imipenem/cilastatin and for meropenem evaluated by Monte Carlo simulation. Diagn Microbiol Infect Dis (2010) 0.93
Nonpharmacological amelioration of age-related learning deficits: the impact of hippocampal theta-triggered training. Proc Natl Acad Sci U S A (2005) 0.93
Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold. J Med Chem (2011) 0.93