Published in Bioorg Med Chem Lett on June 30, 2006
The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery. Nat Rev Drug Discov (2010) 1.94
Oral administration of a small molecule targeted to block proNGF binding to p75 promotes myelin sparing and functional recovery after spinal cord injury. J Neurosci (2013) 0.98
Recent advances in the medicinal chemistry of the metabotropic glutamate receptor 1 (mGlu₁). ACS Chem Neurosci (2011) 0.92
Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1. Bioorg Med Chem Lett (2013) 0.84
N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett (2013) 0.80
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents. Bioorg Med Chem Lett (2016) 0.75
ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res (2008) 9.65
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med (2013) 8.89
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res (2007) 5.75
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A (2007) 2.60
A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A (2002) 2.24
The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J Neurosci (2007) 2.07
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem (2008) 1.85
Influence of genotype, dose and sex on pruritogen-induced scratching behavior in the mouse. Pain (2006) 1.83
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer. J Med Chem (2009) 1.68
Involvement of the TTX-resistant sodium channel Nav 1.8 in inflammatory and neuropathic, but not post-operative, pain states. Pain (2006) 1.55
Fatty acid amide hydrolase inhibitors display broad selectivity and inhibit multiple carboxylesterases as off-targets. Neuropharmacology (2007) 1.53
Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain (2005) 1.46
Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-RS. Proc Natl Acad Sci U S A (2007) 1.45
Molecular determinants of species-specific activation or blockade of TRPA1 channels. J Neurosci (2008) 1.42
Effects of A-317491, a novel and selective P2X3/P2X2/3 receptor antagonist, on neuropathic, inflammatory and chemogenic nociception following intrathecal and intraplantar administration. Br J Pharmacol (2003) 1.42
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. J Med Chem (2006) 1.36
Painful purinergic receptors. J Pharmacol Exp Ther (2007) 1.33
Variable sensitivity to noxious heat is mediated by differential expression of the CGRP gene. Proc Natl Acad Sci U S A (2005) 1.33
Thrombospondin-1 mimetic peptide inhibitors of angiogenesis and tumor growth: design, synthesis, and optimization of pharmacokinetics and biological activities. J Med Chem (2005) 1.31
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J Med Chem (2008) 1.30
A-366833: a novel nicotinonitrile-substituted 3,6-diazabicyclo[3.2.0]-heptane alpha4beta2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in animal models. Biochem Pharmacol (2007) 1.27
Synthesis of 4,5-diaryl-1H-pyrazole-3-ol derivatives as potential COX-2 inhibitors. J Org Chem (2004) 1.27
Localization of histamine H4 receptors in the central nervous system of human and rat. Brain Res (2008) 1.24
Transient receptor potential A1 mediates an osmotically activated ion channel. Eur J Neurosci (2008) 1.23
Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents. J Neurosci (2014) 1.21
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther (2007) 1.20
Central and peripheral sites of action for CB₂ receptor mediated analgesic activity in chronic inflammatory and neuropathic pain models in rats. Br J Pharmacol (2011) 1.20
Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans. Pharm Res (2004) 1.19
Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities. Eur J Pharmacol (2004) 1.18
Attenuation of mechanical allodynia by clinically utilized drugs in a rat chemotherapy-induced neuropathic pain model. Pain (2004) 1.12
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. J Med Chem (2007) 1.11
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management. J Med Chem (2008) 1.10
Efficacy of systemic morphine suggests a fundamental difference in the mechanisms that generate bone cancer vs inflammatory pain. Pain (2002) 1.09
History as narrative: the nature and quality of historical understanding for students with LD. J Learn Disabil (2007) 1.09
Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem (2007) 1.06
Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond) (2002) 1.06
TRPV1b overexpression negatively regulates TRPV1 responsiveness to capsaicin, heat and low pH in HEK293 cells. J Neurochem (2006) 1.05
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. J Med Chem (2005) 1.04
Default-mode-like network activation in awake rodents. PLoS One (2011) 1.04
Comparative effects of levosimendan, OR-1896, OR-1855, dobutamine, and milrinone on vascular resistance, indexes of cardiac function, and O2 consumption in dogs. Am J Physiol Heart Circ Physiol (2007) 1.04
Differential action potentials and firing patterns in injured and uninjured small dorsal root ganglion neurons after nerve injury. Brain Res (2004) 1.02
H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats. Pharmacol Biochem Behav (2009) 1.01
Alteration of dorsal root ganglion P2X3 receptor expression and function following spinal nerve ligation in the rat. Exp Brain Res (2002) 1.01
Spinal nerve ligation in mouse upregulates TRPV1 heat function in injured IB4-positive nociceptors. J Pain (2009) 1.00
α4β2 neuronal nicotinic receptor positive allosteric modulation: an approach for improving the therapeutic index of α4β2 nAChR agonists in pain. Biochem Pharmacol (2011) 1.00
A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid. J Pharmacol Exp Ther (2005) 0.99
Pharmacological modulation of movement-evoked pain in a rat model of osteoarthritis. Eur J Pharmacol (2009) 0.99
In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease. J Pharmacol Exp Ther (2010) 0.98
Gamma interferon release assay for monitoring of treatment response for active tuberculosis: an explosion in the spaghetti factory. J Clin Microbiol (2012) 0.98
Comparison of mechanical allodynia and the affective component of inflammatory pain in rats. Neuropharmacology (2009) 0.97
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. J Med Chem (2009) 0.96
Role of central and peripheral mGluR5 receptors in post-operative pain in rats. Pain (2005) 0.96
Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties. CNS Neurosci Ther (2008) 0.96
Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain. Pain (2010) 0.96
Contributions of central and peripheral TRPV1 receptors to mechanically evoked and spontaneous firing of spinal neurons in inflamed rats. J Neurophysiol (2008) 0.96
Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A (2004) 0.96
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors. J Med Chem (2009) 0.95
Reconstitution of human corpus cavernosum smooth muscle in vitro and in vivo. Tissue Eng (2002) 0.95
Kiwifruit promotes laxation in the elderly. Asia Pac J Clin Nutr (2002) 0.95
Copper and human health: biochemistry, genetics, and strategies for modeling dose-response relationships. J Toxicol Environ Health B Crit Rev (2007) 0.95
Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol Pain (2012) 0.94
Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1. J Med Chem (2012) 0.94
Purifying selection and birth-and-death evolution in the class II hydrophobin gene families of the ascomycete Trichoderma/Hypocrea. BMC Evol Biol (2008) 0.94
The novel calpain inhibitor A-705253 potently inhibits oligomeric beta-amyloid-induced dynamin 1 and tau cleavage in hippocampal neurons. Neurochem Int (2008) 0.93
Ritonavir-PEG 8000 amorphous solid dispersions: in vitro and in vivo evaluations. J Pharm Sci (2004) 0.93
Capsaicin causes protein synthesis inhibition and microtubule disassembly through TRPV1 activities both on the plasma membrane and intracellular membranes. Biochem Pharmacol (2007) 0.93
Activation of TRPA1 channels by the fatty acid amide hydrolase inhibitor 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate (URB597). Mol Pharmacol (2007) 0.93
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem (2008) 0.92
A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats. Pharmacol Biochem Behav (2005) 0.92
Discovery of 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a dopaminergic agent with a novel mode of action for the potential treatment of erectile dysfunction. J Med Chem (2004) 0.92