Published in J Med Chem on March 25, 2010
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A critical assessment of docking programs and scoring functions. J Med Chem (2006) 5.78
Automated design of ligands to polypharmacological profiles. Nature (2012) 3.54
N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature (2010) 2.90
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
Evaluation of direct transport pathways of glycine receptor antagonists and an angiotensin antagonist from the nasal cavity to the central nervous system in the rat model. Pharm Res (2008) 1.93
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. Antimicrob Agents Chemother (2010) 1.49
Molecular and serologic tracing of a transfusion-transmitted hepatitis A virus. Transfusion (2004) 1.45
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena. Bioorg Med Chem Lett (2008) 1.40
Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochem Pharmacol (2010) 1.33
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors. J Med Chem (2011) 1.33
The anti-trypanosome drug fexinidazole shows potential for treating visceral leishmaniasis. Sci Transl Med (2012) 1.32
Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors. J Pharmacol Exp Ther (2010) 1.30
Structure-activity studies on neuropeptide S: identification of the amino acid residues crucial for receptor activation. J Biol Chem (2006) 1.13
Transfusion efficacy of ABO major-mismatched platelets (PLTs) in children is inferior to that of ABO-identical PLTs. Transfusion (2008) 1.07
Oxaliplatin-induced immune pancytopenia. Transfusion (2005) 1.07
Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo. Synapse (2003) 1.06
Target validation: linking target and chemical properties to desired product profile. Curr Top Med Chem (2011) 1.04
Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze. Peptides (2006) 1.03
Organocatalyzed enantioselective fluorocyclizations. Angew Chem Int Ed Engl (2011) 1.03
Oxypurinol directly and immediately activates the drug-specific T cells via the preferential use of HLA-B*58:01. J Immunol (2014) 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
Pneumonia associated with a dental unit waterline. Lancet (2012) 1.02
Avidity determines T-cell reactivity in abacavir hypersensitivity. Eur J Immunol (2012) 1.00
Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases. Chem Biol (2010) 1.00
Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators. J Med Chem (2010) 0.97
Different susceptibility to social defeat stress of BalbC and C57BL6/J mice. Behav Brain Res (2010) 0.97
Occupancy of brain dopamine D3 receptors and drug craving: a translational approach. Neuropsychopharmacology (2012) 0.97
Assessing brain free fraction in early drug discovery. Expert Opin Drug Metab Toxicol (2010) 0.96
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
A comparative study of the CYP450 inhibition potential of marketed drugs using two fluorescence based assay platforms routinely used in the pharmaceutical industry. Drug Metab Lett (2011) 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
Stable expression and functional characterization of a human nicotinic acetylcholine receptor with α6β2 properties: discovery of selective antagonists. Br J Pharmacol (2011) 0.92
Expression analysis of brain-derived neurotrophic factor (BDNF) mRNA isoforms after chronic and acute antidepressant treatment. Brain Res (2004) 0.91
Dopamine responsiveness to drugs of abuse: A shell-core investigation in the nucleus accumbens of the mouse. Synapse (2003) 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
Evaluation of cytochrome P450 inhibition assays using human liver microsomes by a cassette analysis /LC-MS/MS. Drug Metab Lett (2010) 0.89
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
In vitro and in vivo pharmacological characterization of the novel UT receptor ligand [Pen5,DTrp7,Dab8]urotensin II(4-11) (UFP-803). Br J Pharmacol (2006) 0.89
The R enantiomer of the antitubercular drug PA-824 as a potential oral treatment for visceral Leishmaniasis. Antimicrob Agents Chemother (2013) 0.89
Combining PET biodistribution and equilibrium dialysis assays to assess the free brain concentration and BBB transport of CNS drugs. J Cereb Blood Flow Metab (2012) 0.89
Performance Assessment in Fingerprinting and Multi Component Quantitative NMR Analyses. Anal Chem (2015) 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
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett (2010) 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
Receptor occupancy and brain free fraction. Drug Metab Dispos (2009) 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
The efficacy of sodium channel blockers to prevent phencyclidine-induced cognitive dysfunction in the rat: potential for novel treatments for schizophrenia. J Pharmacol Exp Ther (2011) 0.85
Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors. ChemMedChem (2011) 0.85
Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology (2012) 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
Efficacy of individual nucleic acid amplification testing in reducing the risk of transfusion-transmitted hepatitis B virus infection in Switzerland, a low-endemic region. Transfusion (2010) 0.84
Alterations of behavioral and endocrinological reactivity induced by 3 brief social defeats in rats: relevance to human psychopathology. Psychoneuroendocrinology (2009) 0.84
Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo. PLoS One (2012) 0.84
Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophrenia. Bioorg Med Chem Lett (2011) 0.84
Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds. J Med Chem (2010) 0.84
Brain penetration of local anaesthetics in the rat: Implications for experimental neuroscience. J Neurosci Methods (2009) 0.83
The relationship between sodium channel inhibition and anticonvulsant activity in a model of generalised seizure in the rat. Epilepsy Res (2009) 0.83
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
Slow dissociation of partial agonists from the D₂ receptor is linked to reduced prolactin release. Int J Neuropsychopharmacol (2011) 0.82