Published in J Med Chem on October 11, 2007
Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine. CNS Drugs (2010) 1.48
Inhibition of calcitonin gene-related peptide function: a promising strategy for treating migraine. Headache (2008) 0.99
Control of olefin geometry in macrocyclic ring-closing metathesis using a removable silyl group. J Am Chem Soc (2011) 0.98
Calcitonin gene-related peptide: physiology and pathophysiology. Physiol Rev (2014) 0.96
Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system. J Headache Pain (2008) 0.92
Research resource: Haploinsufficiency of receptor activity-modifying protein-2 (RAMP2) causes reduced fertility, hyperprolactinemia, skeletal abnormalities, and endocrine dysfunction in mice. Mol Endocrinol (2011) 0.89
Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine. Br J Pharmacol (2012) 0.89
Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974). Br J Clin Pharmacol (2010) 0.88
Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist. ACS Med Chem Lett (2010) 0.80
Analysis of the proteolysis of bioactive peptides using a peptidomics approach. Nat Protoc (2013) 0.78
Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine. ACS Med Chem Lett (2012) 0.77
Asymmetric organocatalysis at the service of medicinal chemistry. ISRN Org Chem (2014) 0.76
The Dose Proportionality of Telcagepant after Administration of Single Oral and Intravenous Doses in Healthy Adult Subjects. Arch Drug Inf (2010) 0.76
Endosomal proteolysis regulates calcitonin gene-related peptide responses in mesenteric arteries. Br J Pharmacol (2012) 0.76
Quinoline derivatives: candidate drugs for a class B G-protein coupled receptor, the calcitonin gene-related peptide receptor, a cause of migraines. CNS Neurol Disord Drug Targets (2014) 0.75
ACS chemical neuroscience molecule spotlight on Telcagepant (MK-0974). ACS Chem Neurosci (2011) 0.75
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor. ACS Med Chem Lett (2013) 0.75
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc Natl Acad Sci U S A (2004) 2.55
HC-030031, a TRPA1 selective antagonist, attenuates inflammatory- and neuropathy-induced mechanical hypersensitivity. Mol Pain (2008) 2.32
Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques. Science (2004) 2.12
Identification and biological characterization of heterocyclic inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem (2002) 1.89
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1). J Med Chem (2004) 1.87
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother (2009) 1.80
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells. J Med Chem (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
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother (2012) 1.48
Resistance profile of a hepatitis C virus RNA-dependent RNA polymerase benzothiadiazine inhibitor. Antimicrob Agents Chemother (2003) 1.40
Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists. J Biol Chem (2002) 1.30
Functional and pharmacological properties of canine ERG potassium channels. Am J Physiol Heart Circ Physiol (2002) 1.28
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist. J Med Chem (2008) 1.28
Copper-facilitated Suzuki reactions: application to 2-heterocyclic boronates. Org Lett (2009) 1.24
Uncovering the genetic landscape for multiple sleep-wake traits. PLoS One (2009) 1.21
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor. J Med Chem (2010) 1.19
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates. J Pharmacol Exp Ther (2008) 1.16
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group. Bioorg Med Chem Lett (2004) 1.15
Arresting initiation of hepatitis C virus RNA synthesis using heterocyclic derivatives. J Biol Chem (2003) 1.15
Discovery of MK-8742: an HCV NS5A inhibitor with broad genotype activity. ChemMedChem (2013) 1.13
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother (2009) 1.13
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease. J Am Chem Soc (2008) 1.11
A potent and orally active HIV-1 integrase inhibitor. Bioorg Med Chem Lett (2006) 1.10
Web-based vs. traditional classroom instruction in gerontology: a pilot study. J Dent Hyg (2005) 1.09
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase. J Med Chem (2006) 1.09
Progress toward a practical BACE-1 inhibitor. Curr Opin Drug Discov Devel (2007) 1.07
Differential effects of the mGluR5 positive allosteric modulator CDPPB in the cortex and striatum following repeated administration. Neuropharmacology (2010) 1.07
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold. Bioorg Med Chem Lett (2010) 1.06
Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium. Ann N Y Acad Sci (2011) 1.06
Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother (2010) 1.04
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. J Med Chem (2008) 1.03
In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice. J Pharmacol Exp Ther (2010) 1.02
Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells. Eur J Pharmacol (2002) 1.01
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases. J Med Chem (2004) 1.00
Refined anatomical isolation of functional sleep circuits exhibits distinctive regional and circadian gene transcriptional profiles. Brain Res (2009) 0.98
Sub-chronic administration of zolpidem affects modifications to rat sleep architecture. Brain Res (2004) 0.98
High throughput ion-channel pharmacology: planar-array-based voltage clamp. Assay Drug Dev Technol (2003) 0.98
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine. Bioorg Med Chem Lett (2006) 0.96
Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice. J Clin Invest (2009) 0.96
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1). J Med Chem (2006) 0.95
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines. J Med Chem (2003) 0.95
Unraveling the aflatoxin-FAPY conundrum: structural basis for differential replicative processing of isomeric forms of the formamidopyrimidine-type DNA adduct of aflatoxin B1. J Am Chem Soc (2006) 0.95
Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure. Neuropharmacology (2009) 0.94
Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther (2002) 0.94
Enzymatic activities of the GB virus-B RNA-dependent RNA polymerase. Virology (2003) 0.93
Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys (2009) 0.93
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist. J Med Chem (2007) 0.92
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther (2010) 0.92
Protease inhibitors as potential disease-modifying therapeutics for Alzheimer's disease. Expert Opin Investig Drugs (2005) 0.92
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors. Bioorg Med Chem Lett (2007) 0.92
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3). Bioorg Med Chem Lett (2009) 0.91
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells. Bioorg Med Chem Lett (2005) 0.91
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors. J Med Chem (2004) 0.91
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model. J Med Chem (2006) 0.90
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats. ChemMedChem (2009) 0.90
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs). Bioorg Med Chem Lett (2007) 0.90
Biochemical and cell-based assays for characterization of BACE-1 inhibitors. Anal Biochem (2005) 0.90
In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232. J Pharmacol Exp Ther (2013) 0.90
Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine. Br J Pharmacol (2012) 0.89
Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett (2008) 0.89
Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974). Br J Clin Pharmacol (2010) 0.88
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation. J Med Chem (2006) 0.88
Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability. Bioorg Med Chem (2006) 0.88
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1. Bioorg Med Chem Lett (2009) 0.87