Published in J Med Chem on June 10, 2010
β(2) -adrenoceptor agonists: current and future direction. Br J Pharmacol (2011) 1.30
Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: current and future agents. Respir Res (2010) 1.21
Efficacy and safety of 4 weeks' treatment with combined fluticasone furoate/vilanterol in a single inhaler given once daily in COPD: a placebo-controlled randomised trial. BMJ Open (2012) 1.13
Safety, tolerability, pharmacodynamics and pharmacokinetics of umeclidinium and vilanterol alone and in combination: a randomized crossover trial. PLoS One (2012) 1.08
Effect of verapamil on systemic exposure and safety of umeclidinium and vilanterol: a randomized and open-label study. Int J Chron Obstruct Pulmon Dis (2013) 0.86
New combination treatments in the management of asthma: focus on fluticasone/vilanterol. J Asthma Allergy (2014) 0.80
Role of indacaterol and the newer very long-acting β2-agonists in patients with stable COPD: a review. Int J Chron Obstruct Pulmon Dis (2013) 0.79
Comparison of vilanterol, a novel long-acting beta2 agonist, with placebo and a salmeterol reference arm in asthma uncontrolled by inhaled corticosteroids. J Negat Results Biomed (2014) 0.79
Differential pharmacology and clinical utility of emerging combination treatments in the management of COPD--role of umeclidinium/vilanterol. Int J Chron Obstruct Pulmon Dis (2014) 0.79
Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action. ACS Med Chem Lett (2014) 0.77
Umeclidinium bromide/vilanterol combination in the treatment of chronic obstructive pulmonary disease: a review. Ther Clin Risk Manag (2015) 0.76
Profile of fluticasone furoate/vilanterol dry powder inhaler combination therapy as a potential treatment for COPD. Int J Chron Obstruct Pulmon Dis (2014) 0.75
Umeclidinium in chronic obstructive pulmonary disease: latest evidence and place in therapy. Ther Adv Chronic Dis (2017) 0.75
Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease. Am J Physiol Lung Cell Mol Physiol (2007) 1.58
X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain. J Med Chem (2008) 1.36
In vivo labeling of adult neural progenitors for MRI with micron sized particles of iron oxide: quantification of labeled cell phenotype. Neuroimage (2008) 1.20
In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther (2012) 1.03
Subcellular distribution of GABA(B) receptor homo- and hetero-dimers. Biochem J (2005) 1.03
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series. J Med Chem (2006) 1.02
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs. J Med Chem (2003) 0.98
CRACM/Orai ion channel expression and function in human lung mast cells. J Allergy Clin Immunol (2012) 0.96
Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther (2013) 0.95
Characterization of selective Calcium-Release Activated Calcium channel blockers in mast cells and T-cells from human, rat, mouse and guinea-pig preparations. Eur J Pharmacol (2013) 0.92
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration. Bioorg Med Chem Lett (2009) 0.92
Knowledge-based interaction fingerprint scoring: a simple method for improving the effectiveness of fast scoring functions. J Chem Inf Model (2006) 0.92
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity. Bioorg Med Chem Lett (2008) 0.91
Fluticasone furoate/fluticasone propionate - different drugs with different properties. Clin Respir J (2011) 0.88
A 3,4-trans-fused cyclic protecting group facilitates α-selective catalytic synthesis of 2-deoxyglycosides. Angew Chem Int Ed Engl (2014) 0.87
Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor. Proc Natl Acad Sci U S A (2009) 0.86
Effect of the TRPV1 antagonist SB-705498 on the nasal parasympathetic reflex response in the ovalbumin sensitized guinea pig. Br J Pharmacol (2013) 0.86
4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists. J Med Chem (2007) 0.85
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose. J Med Chem (2011) 0.83
α-Selective organocatalytic synthesis of 2-deoxygalactosides. Angew Chem Int Ed Engl (2012) 0.83
Nanoparticle transport in epithelial cells: pathway switching through bioconjugation. Small (2013) 0.83
Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists. J Med Chem (2013) 0.82
Chiral phosphoramide-catalyzed enantioselective addition of allylic trichlorosilanes to aldehydes. Preparative and mechanistic studies with monodentate phosphorus-based amides. J Org Chem (2006) 0.82
Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation. Bioorg Med Chem Lett (2012) 0.82
The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists. Bioorg Med Chem Lett (2009) 0.82
Delivery of fluorescent probes using iron oxide particles as carriers enables in-vivo labeling of migrating neural precursors for magnetic resonance imaging and optical imaging. J Biomed Opt (2007) 0.81
A refined model for prediction of hydrogen bond acidity and basicity parameters from quantum chemical molecular descriptors. Phys Chem Chem Phys (2009) 0.81
Quantum Isostere Database: a web-based tool using quantum chemical topology to predict bioisosteric replacements for drug design. J Chem Inf Model (2009) 0.81
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy. Bioorg Med Chem Lett (2012) 0.80
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. J Med Chem (2011) 0.80
Oxazolidinones as novel human CCR8 antagonists. Bioorg Med Chem Lett (2006) 0.80
The identification of a series of novel, soluble non-peptidic neuropeptide Y Y2 receptor antagonists. Bioorg Med Chem Lett (2010) 0.80
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics. Bioorg Med Chem Lett (2007) 0.80
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs. Bioorg Med Chem Lett (2011) 0.79
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors. Bioorg Med Chem Lett (2009) 0.79
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an "agreement docking" method. J Med Chem (2005) 0.79
Retrospective docking study of PDE4B ligands and an analysis of the behavior of selected scoring functions. J Chem Inf Model (2005) 0.78
Workshop on using natural language processing applications for enhancing clinical decision making: an executive summary. J Am Med Inform Assoc (2013) 0.78
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists. Bioorg Med Chem Lett (2008) 0.78
Trimethylsilylpyrazoles as novel inhibitors of p38 MAP kinase: a new use of silicon bioisosteres in medicinal chemistry. Bioorg Med Chem Lett (2006) 0.78
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines. Bioorg Med Chem Lett (2008) 0.77
Should medicinal chemists do molecular modelling? Drug Discov Today (2012) 0.77
Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing. J Med Chem (2013) 0.77
Analysis of neighborhood behavior in lead optimization and array design. J Chem Inf Model (2009) 0.77
Uptake and transport of B12-conjugated nanoparticles in airway epithelium. J Control Release (2013) 0.77
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups. J Med Chem (2009) 0.77
Structure-activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors. Bioorg Med Chem Lett (2003) 0.76
Pyrazolopyridines as potent PDE4B inhibitors: 5-heterocycle SAR. Bioorg Med Chem Lett (2010) 0.76
Aryl-aryl bond formation by the fluoride-free cross-coupling of aryldisiloxanes with aryl bromides. Chemistry (2011) 0.76
Toward an ab initio fragment database for bioisosterism: dependence of QCT properties on level of theory, conformation, and chemical environment. J Comput Chem (2009) 0.76
NIH workshop on clinical translation of molecular imaging probes and technology--meeting report. Mol Imaging Biol (2014) 0.75
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists. Bioorg Med Chem Lett (2009) 0.75
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity. J Med Chem (2007) 0.75
Plasmachemical surface functionalised beads: versatile tailored supports for polymer assisted organic synthesis. Chem Commun (Camb) (2004) 0.75
Silicon analogues of the nonpeptidic GnRH antagonist AG-045572: syntheses, crystal structure analyses, and pharmacological characterization. ChemMedChem (2011) 0.75
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group. Bioorg Med Chem (2011) 0.75
Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity. Bioorg Med Chem Lett (2010) 0.75
In vivo activity of an azole series of CCR2 antagonists. Bioorg Med Chem Lett (2012) 0.75
A practical drug discovery project at the undergraduate level. Drug Discov Today (2013) 0.75
Reaction of 1,1'-divinyl ferrocene with one-electron oxidants: entry into functionalised [4]ferrocenophanes and observation of an isotope-dependent chemoselectivity effect. Chemistry (2010) 0.75
Synthesis of α-substituted vinylsulfonium salts and their application as annulation reagents in the formation of epoxide- and cyclopropane-fused heterocycles. J Org Chem (2014) 0.75
The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings. Bioorg Med Chem (2011) 0.75
Effect of lamotrigine on the activities of monoamine oxidases A and B in vitro and on monoamine disposition in vivo. Eur J Pharmacol (2005) 0.75