Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.

Progress in corticotropin-releasing factor-1 antagonist development. Drug Discov Today (2010) 1.32

Calcitonin and calcitonin receptor-like receptors: common themes with family B GPCRs? Br J Pharmacol (2012) 0.97

Crystal structure of human cytochrome P450 2D6. J Biol Chem (2005) 2.34

From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett (2007) 2.06

Differences in the central nervous system distribution and pharmacology of the mouse 5-hydroxytryptamine-6 receptor compared with rat and human receptors investigated by radioligand binding, site-directed mutagenesis, and molecular modeling. Mol Pharmacol (2003) 1.78

Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol (2013) 1.65

Effects of interferon-alpha on rhesus monkeys: a nonhuman primate model of cytokine-induced depression. Biol Psychiatry (2007) 1.51

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res (2010) 1.48

In vivo quantification of regional dopamine-D3 receptor binding potential of (+)-PHNO: Studies in non-human primates and transgenic mice. Synapse (2009) 1.47

Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens. J Med Chem (2002) 1.42

Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena. Bioorg Med Chem Lett (2008) 1.40

Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design. J Med Chem (2009) 1.37

GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther (2007) 1.30

Oleispira antarctica gen. nov., sp. nov., a novel hydrocarbonoclastic marine bacterium isolated from Antarctic coastal sea water. Int J Syst Evol Microbiol (2003) 1.23

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett (2012) 1.16

The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia. Sleep (2012) 1.04

Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze. Peptides (2006) 1.03

Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J Med Chem (2013) 1.02

1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists. J Med Chem (2007) 1.02

Modeling the pore structure of voltage-gated sodium channels in closed, open, and fast-inactivated conformation reveals details of site 1 toxin and local anesthetic binding. J Mol Model (2006) 1.01

Differential effects of the CRF-R1 antagonist GSK876008 on fear-potentiated, light- and CRF-enhanced startle suggest preferential involvement in sustained vs phasic threat responses. Neuropsychopharmacology (2008) 1.00

2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD-307243) causes instantaneous current through human ether-a-go-go-related gene potassium channels. Mol Pharmacol (2007) 0.98

Different susceptibility to social defeat stress of BalbC and C57BL6/J mice. Behav Brain Res (2010) 0.97

Lipoxin A4 and aspirin-triggered 15-epi-lipoxin A4 inhibit human neutrophil migration: comparisons between synthetic 15 epimers in chemotaxis and transmigration with microvessel endothelial cells and epithelial cells. J Immunol (2003) 0.96

Assessing brain free fraction in early drug discovery. Expert Opin Drug Metab Toxicol (2010) 0.96

Design, synthesis and bioactions of novel stable mimetics of lipoxins and aspirin-triggered lipoxins. Prostaglandins Leukot Essent Fatty Acids (2005) 0.95

Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist. J Psychopharmacol (2011) 0.95

Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase. Bioorg Med Chem Lett (2005) 0.94

SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test. Neuropsychopharmacology (2007) 0.93

1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists. J Med Chem (2010) 0.92

CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. J Med Chem (2003) 0.91

GSK1614343, a novel ghrelin receptor antagonist, produces an unexpected increase of food intake and body weight in rodents and dogs. Neuroendocrinology (2011) 0.91

Crude oil-induced structural shift of coastal bacterial communities of rod bay (Terra Nova Bay, Ross Sea, Antarctica) and characterization of cultured cold-adapted hydrocarbonoclastic bacteria. FEMS Microbiol Ecol (2004) 0.91

Expression analysis of brain-derived neurotrophic factor (BDNF) mRNA isoforms after chronic and acute antidepressant treatment. Brain Res (2004) 0.91

Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. J Med Chem (2008) 0.90

5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors. Bioorg Med Chem Lett (2012) 0.90

Strain-specific outcomes of repeated social defeat and chronic fluoxetine treatment in the mouse. Pharmacol Biochem Behav (2010) 0.89

Social defeat-induced contextual conditioning differentially imprints behavioral and adrenal reactivity: a time-course study in the rat. Physiol Behav (2007) 0.89

Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator. J Med Chem (2010) 0.87

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett (2011) 0.86

Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence. J Med Chem (2010) 0.86

Transient forebrain over-expression of CRF induces plasma corticosterone and mild behavioural changes in adult conditional CRF transgenic mice. Pharmacol Biochem Behav (2009) 0.86

Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol (2005) 0.86

CRF1 receptor activation increases the response of neurons in the basolateral nucleus of the amygdala to afferent stimulation. Front Behav Neurosci (2008) 0.86

Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. Drug Metab Dispos (2010) 0.85

Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors. Bioorg Med Chem Lett (2011) 0.85

Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists. Bioorg Med Chem Lett (2005) 0.85

Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. J Med Chem (2008) 0.85

Modeling GPCR active state conformations: the β(2)-adrenergic receptor. Proteins (2011) 0.85

Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia. Bioorg Med Chem Lett (2011) 0.84

Structural determinants of drugs acting on the Nav1.8 channel. J Biol Chem (2009) 0.84

Alterations of behavioral and endocrinological reactivity induced by 3 brief social defeats in rats: relevance to human psychopathology. Psychoneuroendocrinology (2009) 0.84

Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist. J Med Chem (2009) 0.84

Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav Pharmacol (2009) 0.84

Single exposure to social defeat increases corticotropin-releasing factor and glucocorticoid receptor mRNA expression in rat hippocampus. Brain Res (2005) 0.83

Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists. J Med Chem (2010) 0.83

Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): in vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity. Neuropharmacology (2006) 0.83

The association of rs4307059 and rs35678 markers with autism spectrum disorders is replicated in Italian families. Psychiatr Genet (2012) 0.82

Characterising the plasma-target occupancy relationship of the neurokinin antagonist GSK1144814 with PET. J Psychopharmacol (2014) 0.82

Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists. Bioorg Med Chem Lett (2010) 0.81

Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists. Bioorg Med Chem (2003) 0.81

Studies towards the identification of a new generation of atypical antipsychotic agents. Bioorg Med Chem Lett (2006) 0.81