3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.

Ionotropic and metabotropic glutamate receptor structure and pharmacology. Psychopharmacology (Berl) (2005) 2.25

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. Mol Pharmacol (2012) 1.15

ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res (2012) 2.51

3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J Med Chem (2003) 2.17

Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers. Synapse (2005) 1.90

Small molecules can selectively inhibit ephrin binding to the EphA4 and EphA2 receptors. J Biol Chem (2008) 1.80

HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus. Assay Drug Dev Technol (2007) 1.40

Chemical biology investigation of cell death pathways activated by endoplasmic reticulum stress reveals cytoprotective modulators of ASK1. J Biol Chem (2008) 1.33

In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol (2003) 1.33

Exploring eye movements in patients with glaucoma when viewing a driving scene. PLoS One (2010) 1.26

The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats. Neuropsychopharmacology (2010) 1.23

The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety. Neuropsychopharmacology (2004) 1.23

Preclinical studies of celastrol and acetyl isogambogic acid in melanoma. Clin Cancer Res (2007) 1.20

Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system. Anal Biochem (2003) 1.19

Phosphomannose isomerase inhibitors improve N-glycosylation in selected phosphomannomutase-deficient fibroblasts. J Biol Chem (2011) 1.19

Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors. Bioorg Med Chem Lett (2004) 1.17

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). J Med Chem (2009) 1.13

Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J Pharmacol Exp Ther (2004) 1.13

Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Bioorg Med Chem Lett (2008) 1.11

5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg Med Chem Lett (2004) 1.10

Outcomes of endolymphatic shunt surgery for Ménière's disease: comparison with intratympanic gentamicin on vertigo control and hearing loss. Otol Neurotol (2010) 1.04

Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorg Med Chem Lett (2012) 1.03

Investigation of potential mechanisms regulating protein expression of hepatic pyruvate dehydrogenase kinase isoforms 2 and 4 by fatty acids and thyroid hormone. Biochem J (2003) 1.03

[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther (2002) 1.02

How does glaucoma look?: patient perception of visual field loss. Ophthalmology (2013) 1.02

Evaluation of the role of peroxisome-proliferator-activated receptor alpha in the regulation of cardiac pyruvate dehydrogenase kinase 4 protein expression in response to starvation, high-fat feeding and hyperthyroidism. Biochem J (2002) 1.01

A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors. Chem Biol Drug Des (2011) 1.01

Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. J Med Chem (2004) 1.00

Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology (2004) 0.99

Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles. Org Lett (2010) 0.98

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem (2003) 0.98

Glaucoma and reading: exploring the effects of contrast lowering of text. Optom Vis Sci (2012) 0.97

Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators. ACS Chem Neurosci (2011) 0.97

KD5170, a novel mercaptoketone-based histone deacetylase inhibitor, exerts antimyeloma effects by DNA damage and mitochondrial signaling. Mol Cancer Ther (2008) 0.95

Total synthesis of ionomycin using ring-opening strategies. Org Lett (2002) 0.95

Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNOS dimerization inhibitors that are orally active in pain models. J Med Chem (2010) 0.93

Do patients with glaucoma have difficulty recognizing faces? Invest Ophthalmol Vis Sci (2012) 0.92

Eye movements and reading in glaucoma: observations on patients with advanced visual field loss. Graefes Arch Clin Exp Ophthalmol (2014) 0.91

Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP. Bioorg Med Chem Lett (2011) 0.91

Saccadic eye movements and face recognition performance in patients with central glaucomatous visual field defects. Vision Res (2013) 0.91

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence. J Med Chem (2014) 0.91

KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther (2008) 0.90

Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats. J Med Chem (2010) 0.90

Rapid multistep synthesis of 1,2,4-oxadiazoles in a single continuous microreactor sequence. J Org Chem (2008) 0.89

Expedient synthesis of highly potent antagonists of inhibitor of apoptosis proteins (IAPs) with unique selectivity for ML-IAP. ACS Chem Biol (2013) 0.89

Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia. J Med Chem (2011) 0.89

Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor. Bioorg Med Chem Lett (2005) 0.87

Structure-activity relationship and improved hydrolytic stability of pyrazole derivatives that are allosteric inhibitors of West Nile Virus NS2B-NS3 proteinase. Bioorg Med Chem Lett (2009) 0.87

Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS). Beilstein J Org Chem (2013) 0.87

One-step continuous flow synthesis of highly substituted pyrrole-3-carboxylic acid derivatives via in situ hydrolysis of tert-butyl esters. Org Lett (2010) 0.86

Diabetogenic impact of long-chain omega-3 fatty acids on pancreatic beta-cell function and the regulation of endogenous glucose production. Endocrinology (2003) 0.84

Small-molecule IAP antagonists sensitize cancer cells to TRAIL-induced apoptosis: roles of XIAP and cIAPs. Mol Cancer Ther (2013) 0.83

Acute omega-3 fatty acid enrichment selectively reverses high-saturated fat feeding-induced insulin hypersecretion but does not improve peripheral insulin resistance. Diabetes (2004) 0.83

Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence. J Med Chem (2012) 0.82

Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology. Bioorg Med Chem Lett (2004) 0.82

PPARalpha activation and increased dietary lipid oppose thyroid hormone signaling and rescue impaired glucose-stimulated insulin secretion in hyperthyroidism. Am J Physiol Endocrinol Metab (2008) 0.82

Peroxisome proliferator-activated receptor-alpha and glucocorticoids interactively regulate insulin secretion during pregnancy. Diabetes (2006) 0.81

3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett (2005) 0.81

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett (2005) 0.81

Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. Bioorg Med Chem Lett (2005) 0.81

Bone-anchored hearing aid subjective benefit for unilateral deafness. Laryngoscope (2010) 0.81

Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models. J Med Chem (2009) 0.80

Peroxisome proliferator-activated receptor-alpha activation during pregnancy attenuates glucose-stimulated insulin hypersecretion in vivo by increasing insulin sensitivity, without impairing pregnancy-induced increases in beta-cell glucose sensing and responsiveness. Endocrinology (2003) 0.80

Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP. Bioorg Med Chem Lett (2013) 0.80

Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease. J Med Chem (2002) 0.79

Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptor. Bioorg Med Chem Lett (2004) 0.79

Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists. Bioorg Med Chem Lett (2009) 0.79

In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4-yl) ethynyl]-pyridine (MTEP). Neurosci Lett (2005) 0.79

Inhibitors of tissue-nonspecific alkaline phosphatase (TNAP): from hits to leads. Methods Mol Biol (2013) 0.79

Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation. ACS Chem Biol (2011) 0.78

Novel approach to pro-drugs of lactones: water soluble imidate and ortho-ester derivatives of a furanone-based COX-2 selective inhibitor. Bioorg Med Chem Lett (2005) 0.78

2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. Bioorg Med Chem Lett (2004) 0.78

PPARalpha activation reverses adverse effects induced by high-saturated-fat feeding on pancreatic beta-cell function in late pregnancy. Am J Physiol Endocrinol Metab (2006) 0.78

Amphiphilic suramin dissolves Matrigel, causing an 'inhibition' artefact within in vitro angiogenesis assays. Int J Exp Pathol (2013) 0.77

Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor. Bioorg Med Chem Lett (2008) 0.77

Pharmacological characterization of (S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HCl (SIB-1508Y, Altinicline), a novel nicotinic acetylcholine receptor agonist. Brain Res (2008) 0.77

Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia. Bioorg Med Chem Lett (2005) 0.76

Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. Bioorg Med Chem Lett (2004) 0.76

Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases. J Pharmacol Exp Ther (2010) 0.76

Translational enhancers of EAAT2: therapeutic implications for neurodegenerative disease. J Clin Invest (2014) 0.75

Discovery of novel modulators of metabotropic glutamate receptor subtype-5. Bioorg Med Chem (2004) 0.75

2-Aminopyridines via reaction of pyridine N-oxides and activated isocyanides. J Org Chem (2014) 0.75