Published in Anal Biochem on February 15, 2003
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol Pharmacol (2010) 1.93
Small molecule activators of TRPML3. Chem Biol (2010) 1.37
Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening. Mol Pharmacol (2008) 1.12
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate. Bioorg Med Chem (2008) 1.03
Inhibitors of VIM-2 by screening pharmacologically active and click-chemistry compound libraries. Bioorg Med Chem (2009) 1.02
Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening. Mol Pharmacol (2009) 0.98
Identification of small-molecule inhibitors of the colorectal cancer oncogene Krüppel-like factor 5 expression by ultrahigh-throughput screening. Mol Cancer Ther (2011) 0.94
Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol Cancer Ther (2013) 0.92
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4). J Biomol Screen (2015) 0.92
Screening of potential a disintegrin and metalloproteinase with thrombospondin motifs-4 inhibitors using a collagen model fluorescence resonance energy transfer substrate. Anal Biochem (2007) 0.88
An ultra-high throughput cell-based screen for wee1 degradation inhibitors. J Biomol Screen (2010) 0.87
High-throughput screen for pharmacoperones of the vasopressin type 2 receptor. J Biomol Screen (2013) 0.81
A FluoPol-ABPP PAD2 high-throughput screen identifies the first calcium site inhibitor targeting the PADs. ACS Chem Biol (2014) 0.81
Development of an HTS-compatible assay for the discovery of ASK1 signalosome inhibitors using alphascreen technology. Assay Drug Dev Technol (2014) 0.80
Small-molecule inhibitors of bacterial AddAB and RecBCD helicase-nuclease DNA repair enzymes. ACS Chem Biol (2012) 0.78
An altered zinc-binding site confers resistance to a covalent inactivator of New Delhi metallo-beta-lactamase-1 (NDM-1) discovered by high-throughput screening. Bioorg Med Chem (2013) 0.78
Multiplexed random peptide library and phospho-specific antibodies facilitate human polo-like kinase 1 inhibitor screen. Assay Drug Dev Technol (2010) 0.77
Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β. Biopolymers (2014) 0.77
Genome-scale RNAi screen for host factors required for HIV replication. Cell Host Microbe (2008) 6.24
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol (2012) 3.40
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. Science (2011) 3.30
Compound cytotoxicity profiling using quantitative high-throughput screening. Environ Health Perspect (2008) 3.11
A high-throughput screen for aggregation-based inhibition in a large compound library. J Med Chem (2007) 2.97
Identification of oxadiazoles as new drug leads for the control of schistosomiasis. Nat Med (2008) 2.90
Application of real-time cell electronic sensing (RT-CES) technology to cell-based assays. Assay Drug Dev Technol (2004) 2.74
Induced pluripotent stem cells--opportunities for disease modelling and drug discovery. Nat Rev Drug Discov (2011) 2.58
Fluorescence spectroscopic profiling of compound libraries. J Med Chem (2008) 2.53
Characterization of chemical libraries for luciferase inhibitory activity. J Med Chem (2008) 2.53
Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression. Proc Natl Acad Sci U S A (2009) 2.18
Median absolute deviation to improve hit selection for genome-scale RNAi screens. J Biomol Screen (2008) 2.12
Compound Management for Quantitative High-Throughput Screening. JALA Charlottesv Va (2008) 2.11
A specific mechanism for nonspecific activation in reporter-gene assays. ACS Chem Biol (2008) 2.08
Small interfering RNA screens reveal enhanced cisplatin cytotoxicity in tumor cells having both BRCA network and TP53 disruptions. Mol Cell Biol (2006) 1.97
Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers. Synapse (2005) 1.90
A robotic platform for quantitative high-throughput screening. Assay Drug Dev Technol (2008) 1.90
Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology. Chem Biol (2010) 1.83
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase. J Med Chem (2008) 1.81
Small molecules can selectively inhibit ephrin binding to the EphA4 and EphA2 receptors. J Biol Chem (2008) 1.80
Apparent activity in high-throughput screening: origins of compound-dependent assay interference. Curr Opin Chem Biol (2010) 1.76
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. Proc Natl Acad Sci U S A (2007) 1.70
The use of strictly standardized mean difference for hit selection in primary RNA interference high-throughput screening experiments. J Biomol Screen (2007) 1.65
Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124. Proc Natl Acad Sci U S A (2010) 1.64
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem (2010) 1.61
Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice. Proc Natl Acad Sci U S A (2009) 1.61
Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade. PLoS Negl Trop Dis (2008) 1.58
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Nat Chem Biol (2009) 1.52
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
Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease. J Med Chem (2010) 1.45
HTS identifies novel and specific uncompetitive inhibitors of the two-component NS2B-NS3 proteinase of West Nile virus. Assay Drug Dev Technol (2007) 1.40
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett (2010) 1.37
Functional genomic screening identifies dual leucine zipper kinase as a key mediator of retinal ganglion cell death. Proc Natl Acad Sci U S A (2013) 1.36
Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells. Chem Biol (2011) 1.35
A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution. J Med Chem (2009) 1.34
In vivo receptor occupancy of mGlu5 receptor antagonists using the novel radioligand [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine). Eur J Pharmacol (2003) 1.33
Chemical biology investigation of cell death pathways activated by endoplasmic reticulum stress reveals cytoprotective modulators of ASK1. J Biol Chem (2008) 1.33
Molecular determinants of voltage-dependent human ether-a-go-go related gene (HERG) K+ channel block. J Biol Chem (2002) 1.33
Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Nat Biotechnol (2009) 1.30
Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Biochemistry (2009) 1.28
Differential distribution of voltage-gated calcium channel alpha-2 delta (alpha2delta) subunit mRNA-containing cells in the rat central nervous system and the dorsal root ganglia. J Comp Neurol (2005) 1.27
Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays. PLoS One (2013) 1.27
Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor. J Biomol Screen (2008) 1.25
Dissecting the effects of DNA polymerase and ribonuclease H inhibitor combinations on HIV-1 reverse-transcriptase activities. Biochemistry (2005) 1.25
Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screening. Chem Res Toxicol (2008) 1.25
A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarker. Toxicol In Vitro (2008) 1.24
The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats. Neuropsychopharmacology (2010) 1.23
The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) in rodent models of anxiety. Neuropsychopharmacology (2004) 1.23
A dual-fluorescence high-throughput cell line system for probing multidrug resistance. Assay Drug Dev Technol (2009) 1.22
Integrating experimental and analytic approaches to improve data quality in genome-wide RNAi screens. J Biomol Screen (2008) 1.22
Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening. Assay Drug Dev Technol (2009) 1.20
Preclinical studies of celastrol and acetyl isogambogic acid in melanoma. Clin Cancer Res (2007) 1.20
Phosphomannose isomerase inhibitors improve N-glycosylation in selected phosphomannomutase-deficient fibroblasts. J Biol Chem (2011) 1.19
Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction. Anal Biochem (2007) 1.18
Identification of chemical compounds that induce HIF-1alpha activity. Toxicol Sci (2009) 1.14
Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter. Chem Biol (2012) 1.14
Molecular determinants of KCNQ1 channel block by a benzodiazepine. Mol Pharmacol (2003) 1.14
Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). J Med Chem (2009) 1.13
Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory. Proc Natl Acad Sci U S A (2009) 1.13
Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J Pharmacol Exp Ther (2004) 1.13
Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Bioorg Med Chem Lett (2008) 1.11
Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay. Mol Cancer Ther (2009) 1.11
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. Bioorg Med Chem Lett (2004) 1.10
A coincidence reporter-gene system for high-throughput screening. Nat Methods (2012) 1.10
A cell-based beta-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication. Anal Biochem (2004) 1.08
Hit selection with false discovery rate control in genome-scale RNAi screens. Nucleic Acids Res (2008) 1.07
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk). Bioorg Med Chem Lett (2009) 1.06
Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis. J Med Chem (2009) 1.05
A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme A production. Assay Drug Dev Technol (2008) 1.05
Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features. Toxicol Sci (2009) 1.05
A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression. Anal Biochem (2007) 1.05
Comparison of bioluminescent kinase assays using substrate depletion and product formation. Assay Drug Dev Technol (2009) 1.04
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem (2010) 1.04
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorg Med Chem Lett (2012) 1.03
Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening. Anal Biochem (2003) 1.02
[3H]Methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine binding to metabotropic glutamate receptor subtype 5 in rodent brain: in vitro and in vivo characterization. J Pharmacol Exp Ther (2002) 1.02
A disalicylic acid-furanyl derivative inhibits ephrin binding to a subset of Eph receptors. Chem Biol Drug Des (2011) 1.01
A cell-based assay for IkappaBalpha stabilization using a two-color dual luciferase-based sensor. Assay Drug Dev Technol (2007) 1.01
A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists. J Med Chem (2004) 1.00
A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase. Mol Biosyst (2009) 1.00
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. J Med Chem (2004) 1.00
Differentiating Alzheimer disease-associated aggregates with small molecules. Neurobiol Dis (2007) 1.00
Comparison on functional assays for Gq-coupled GPCRs by measuring inositol monophospate-1 and intracellular calcium in 1536-well plate format. Curr Chem Genomics (2008) 0.99
Discovery of new antimalarial chemotypes through chemical methodology and library development. Proc Natl Acad Sci U S A (2011) 0.99
Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format. Methods Enzymol (2006) 0.99
Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening. Comb Chem High Throughput Screen (2008) 0.99
Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology (2004) 0.99
Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles. Org Lett (2010) 0.98
Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators. ACS Chem Neurosci (2011) 0.97
A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction. Comb Chem High Throughput Screen (2008) 0.96
Monitoring compound integrity with cytochrome P450 assays and qHTS. J Biomol Screen (2009) 0.95
Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death. Bioorg Med Chem (2009) 0.95
The pilot phase of the NIH Chemical Genomics Center. Curr Top Med Chem (2009) 0.94
A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase. Assay Drug Dev Technol (2008) 0.93
Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone. J Biol Chem (2011) 0.93
An efficient and fully automated high-throughput transfection method for genome-scale siRNA screens. J Biomol Screen (2008) 0.92