Research Topics
| Christopher P AustinSummaryAffiliation: National Institutes of Health Country: USA Publications
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Detail Information
Publications
The impact of the completed human genome sequence on the development of novel therapeutics for human diseaseChristopher P Austin
National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892, USA
Annu Rev Med 55:1-13. 2004..These improvements will require increased physician understanding of genetic principles applied to common diseases...- NIH Molecular Libraries InitiativeChristopher P Austin
National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Science 306:1138-9. 2004 
The knockout mouse projectChristopher P Austin
National Human Genome Research Institute, National Institutes of Health, Building 31, Room 4B09, 31 Center Drive, Bethesda, Maryland 20892, USA
Nat Genet 36:921-4. 2004..It is time to harness new technologies and efficiencies of production to mount a high-throughput international effort to produce and phenotype knockouts for all mouse genes, and place these resources into the public domain...- The completed human genome: implications for chemical biologyChristopher P Austin
National Human Genome Research Institute, National Institutes of Health Building 31, Room 4B09, 31 Center Drive, Bethesda, MD 20892, USA
Curr Opin Chem Biol 7:511-5. 2003..Small-molecule chemical biology applied on a genomic scale promises to speed this translation to novel therapeutics... - Application of a homogenous membrane potential assay to assess mitochondrial functionSrilatha Sakamuru
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
Physiol Genomics 44:495-503. 2012..Our results demonstrate that this homogenous cell-based Mito-MPS assay can be used to evaluate the ability of large numbers of chemicals to decrease mitochondrial function... - High throughput screening for small molecule therapy for Gaucher disease using patient tissue as the source of mutant glucocerebrosidaseEhud Goldin
Medical Genetics Branch, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America
PLoS ONE 7:e29861. 2012..These results suggest that primary screening assays using enzyme extracted from tissues is an alternative approach to identify high quality, physiologically relevant lead compounds for drug development... - A multiplex calcium assay for identification of GPCR agonists and antagonistsKe Liu
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, USA
Assay Drug Dev Technol 8:367-79. 2010..This multiplexed assay format provides an efficient and cost-effective method for HTS of G(q)-coupled GPCR targets... - A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTSPing Jun Zhu
National Institutes of Health, National Human Genome Research Institute, NIH Chemical Genomics Center, Bethesda, MD 20892 3370, USA
Comb Chem High Throughput Screen 11:545-59. 2008.... - Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinaseJian Kang Jiang
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, USA
Bioorg Med Chem Lett 20:3387-93. 2010..These agents represent the second reported chemotype for activation of PKM2... - Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screeningDaniel J Urban
Medical Genetics Branch, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3708, USA
Comb Chem High Throughput Screen 11:817-24. 2008..These two assays can be used to identify both GC activators and inhibitors with potential therapeutic value... - Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targetsJing Yuan
Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Science 333:724-9. 2011..Drugs whose responses mapped to wild-type or mutant pfcrt alleles were tested in combination in vitro and in vivo, which yielded promising new leads for antimalarial treatments... - Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinaseMatthew B Boxer
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, MSC 3370 Bethesda, Maryland 20850, USA
J Med Chem 53:1048-55. 2010..7 microg/mL), and 58 (AC(50) = 38 nM, maximum response = 82%; solubility = 51.2 microg/mL). The small molecules described here represent first-in-class activators of PKM2... - Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasisGanesha Rai
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, Maryland 20892 3370, USA
J Med Chem 52:6474-83. 2009..The results of these studies verify the utility of oxadiazole-2-oxides as novel inhibitors of TGR and as efficacious antischistosomal agents... - Synthesis and characterization of a new fluorogenic substrate for alpha-galactosidaseZhen Dan Shi
Imaging Probe Development Center, Division of Intramural Research, National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, MD 20892 3708, USA
Anal Bioanal Chem 394:1903-9. 2009..Therefore, this new red fluorogenic substrate and the resulting enzyme assay can be used in high-throughput screening to identify small-molecule chaperones for Fabry disease... - Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activityJuan J Marugan
NIH Chemical Genomic Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, United States
J Med Chem 54:1033-58. 2011.... - Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memoryMenghang Xia
NIH Chemical Genomics Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, MD 20892, USA
Proc Natl Acad Sci U S A 106:2412-7. 2009..qHTS followed by interrogation of pathway targets is an efficient paradigm for lead generation for chemical genomics and drug development... - Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and miceSusanne Neumann
Clinical Endocrinology Branch, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Proc Natl Acad Sci U S A 106:12471-6. 2009..Thus, we discovered a small molecule that activates human TSHR in vitro, is orally active in mice, and could be a lead for development of drugs to use in place of recombinant human TSH in patients with thyroid cancer... - A quantitative high-throughput screen identifies potential epigenetic modulators of gene expressionRonald L Johnson
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892, USA
Anal Biochem 375:237-48. 2008..These results suggest that the identified small molecules act on epigenetic or transcriptional components and validate our approach of using a cell-based imaging assay in conjunction with qHTS... - A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolutionDouglas S Auld
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
J Med Chem 52:1450-8. 2009..This study demonstrates the power of large-scale quantitative analysis of structure-activity relationships (>100K compounds) in addressing important questions such as a target's druggability... - Identification of small molecule compounds that inhibit the HIF-1 signaling pathwayMenghang Xia
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
Mol Cancer 8:117. 2009..To identify small molecule inhibitors of the HIF-1 pathway, we have developed a cell-based reporter gene assay and screened a large compound library by using a quantitative high-throughput screening (qHTS) approach... - The pilot phase of the NIH Chemical Genomics CenterCraig J Thomas
NIH Chemical Genomics Center, NHGRI, National Institutes of Health, 9800 Medical Center Drive, Building B, Room 3005, MSC 3370, Bethesda, MD 20892 3370, USA
Curr Top Med Chem 9:1181-93. 2009.... - Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk)Bryan T Mott
NIH Chemical Genomics Center, National Human Genome Research Institute, Bethesda, MD 20892 3370, USA
Bioorg Med Chem Lett 19:6700-5. 2009..Molecular docking provides further evidence that inhibition is the result of binding at the kinase hinge region. Selected compounds represent novel tools capable of potent and selective inhibition of Clk1, Clk4, and Dyrk1A... - A robotic platform for quantitative high-throughput screeningSam Michael
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20850, USA
Assay Drug Dev Technol 6:637-57. 2008..The combination of this system and qHTS has led to the generation of over 6 million CRCs from > 120 assays in the last 3 years and is a technology that can be widely implemented to increase efficiency of screening and lead generation... - Monitoring compound integrity with cytochrome P450 assays and qHTSRyan MacArthur
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
J Biomol Screen 14:538-46. 2009..Furthermore, the study illustrates the degree and time scale of apparent compound potency changes due to sample storage... - Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activatorsJuan J Marugan
NIH Chemical Genomic Center, National Human Genome Research Institute, National Institutes of Heath, 9800 Medical Center Drive, Rockville, MD, USA
Eur J Med Chem 45:1880-97. 2010..Herein we report our initial findings of a new series of acid alpha-glucosidase activators... - Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screeningRuili Huang
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
Chem Res Toxicol 21:659-67. 2008..The performance of this clustering method is evaluated by comparing the clustering results against literature annotations of compound mechanisms... - Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascadeAnton Simeonov
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America
PLoS Negl Trop Dis 2:e127. 2008.... - Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitorsAmanda P Skoumbourdis
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH 9800 Medical Center Drive, MSC 3370 Bethesda, MD 20892 3370, USA
Bioorg Med Chem Lett 19:3686-92. 2009..Finally, docking studies with selective ligands (including 10 and 18) were undertaken to better understand this chemotypes ability to bind and inhibit PDE4 selectively... 
Characterization of chemical libraries for luciferase inhibitory activityDouglas S Auld
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
J Med Chem 51:2372-86. 2008..pyralis luciferase. We describe the structure-activity relationship of the luciferase inhibitors and discuss the use of this data in the interpretation of HTS results and configuration of luciferase-based assays...- Fluorescence spectroscopic profiling of compound librariesAnton Simeonov
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
J Med Chem 51:2363-71. 2008..Native compound fluorescence, fluorescent impurities, novel fluorescent compounds, and the utilization of fluorescence profiling data are discussed... - Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol proteaseAjit Jadhav
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
J Med Chem 53:37-51. 2010..The distribution of false positives was relatively constant across library sources. The simple step of including detergent in the assay buffer suppressed the nonspecific effect of approximately 93% of the original hits... - Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatBBryan T Mott
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, MSC 3370 Bethesda, Maryland 20892 3370, USA
J Med Chem 53:52-60. 2010..brucei parasites. Selected compounds were screened against a panel of human cysteine and serine proteases to determine selectivity, and a cocrystal was obtained of our most potent analogue bound to cruzain... - Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channelsMenghang Xia
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
Toxicol Appl Pharmacol 252:250-8. 2011..Profiling environmental compound libraries for hERG channel inhibition provides information useful in prioritizing these compounds for cardiotoxicity assessment in vivo... - Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural featuresRuili Huang
Department of Health and Human Services, NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
Toxicol Sci 112:385-93. 2009..The new algorithm has the important advantages of simplicity, power, interpretability, and ease of implementation... - Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput formatMenghang Xia
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Cell Mol Neurobiol 31:901-7. 2011..The qHTS approach we used in this study will be useful in identifying novel inhibitors of morphine induced addiction from a larger scale screening... - The NCGC pharmaceutical collection: a comprehensive resource of clinically approved drugs enabling repurposing and chemical genomicsRuili Huang
National Institutes of Health Chemical Genomics Center, NIH, Bethesda, MD 20892, USA
Sci Transl Med 3:80ps16. 2011..We report here the creation of a definitive, complete, and nonredundant list of all approved molecular entities as a freely available electronic resource and a physical collection of small molecules amenable to high-throughput screening... - A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical librariesRonald L Johnson
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892, USA
Mol Biosyst 5:1039-50. 2009..Small molecules within these series will make useful tool compounds to investigate IL-6 signaling mediated by JAK-STAT activation... - A high-throughput approach for identification of novel general anestheticsWendy A Lea
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, USA
PLoS ONE 4:e7150. 2009..These hits were validated using isothermal titration calorimetry. The success of this initial screen and computational triage provides feasibility to undergo a large scale campaign to discover novel general anesthetics... - High-throughput screening assays for the identification of chemical probesJames Inglese
US National Institutes of Health Chemical Genomics Center, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892 3370, USA
Nat Chem Biol 3:466-79. 2007..We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays... - Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptorSteve Titus
National Institutes of Health Chemical Genomics Center, National Human Genome Research Institute, NIH, Bethesda, MD 20892 3370, USA
J Biomol Screen 13:120-7. 2008..Forty-nine compounds in several structural classes have been confirmed as the small-molecule TSHR agonists that will serve as a starting point for chemical optimization and studies of thyroid physiology in health and disease... - Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical librariesHenrike Veith
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland, USA
Nat Biotechnol 27:1050-5. 2009..We also identified chemical substructures that differentiated between the five isozymes. The pharmacological compendium described here should further the understanding of CYP isozymes... - Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparumJing Yuan
Laboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, Bethesda, Maryland, USA
Nat Chem Biol 5:765-71. 2009..This study identifies new leads for antimalarial drugs and demonstrates the utility of a high-throughput chemical genomic strategy for studying malaria traits... - Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitorsWenwei Huang
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Dr, Rockville, MD 20850, USA
Bioorg Med Chem Lett 21:5239-43. 2011..In this Letter, we describe an efficient one-pot sequential reaction for the synthesis of quinazolin-4-one 1 analogues. The structure-activity relationship (SAR) study led to the 5-fold more potent analogue, 16... - A cell-based PDE4 assay in 1536-well plate format for high-throughput screeningSteven A Titus
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, Bethesda, Maryland 20892 3370, USA
J Biomol Screen 13:609-18. 2008.... - Identification of chemical compounds that induce HIF-1alpha activityMenghang Xia
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892, USA
Toxicol Sci 112:153-63. 2009..Identification of environmental compounds having HIF-1alpha activation activity in cell-based assays may be useful for prioritizing chemicals for further testing as hypoxia-response inducers in vivo... - Compound cytotoxicity profiling using quantitative high-throughput screeningMenghang Xia
NIH Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 3370, USA
Environ Health Perspect 116:284-91. 2008..Such methods can be relatively expensive, low-throughput, and associated with pain suffered by the treated animals. In addition, differences in species biology may confound extrapolation to human health effects... - A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarkerMing Hsuang Cho
NIH Chemical Genomics Center, National Institutes of Health, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
Toxicol In Vitro 22:1099-106. 2008..This cytotoxicity assay, combined with the qHTS platform, allowed us to quickly and efficiently evaluate compound toxicities related to cell membrane integrity... - Identification of known drugs that act as inhibitors of NF-kappaB signaling and their mechanism of actionSusanne C Miller
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Biochem Pharmacol 79:1272-80. 2010..Comprehensive profiling of approved drugs provides insight into their molecular mechanisms, thus providing a basis for drug repurposing... - Identification of clinically used drugs that activate pregnane X receptorsSunita J Shukla
National Institutes of Health Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, USA
Drug Metab Dispos 39:151-9. 2011.... - Profiling environmental chemicals for activity in the antioxidant response element signaling pathway using a high throughput screening approachSunita J Shukla
NIH Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Rockville, Maryland, USA
Environ Health Perspect 120:1150-6. 2012..Thus, assays that detect the up-regulation of this pathway could be useful for identifying chemicals that induce oxidative stress... - High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell deathJennifer T Fox
Genome Instability Section, Genetics and Molecular Biology Branch, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Proc Natl Acad Sci U S A 109:5423-8. 2012..Furthermore, resveratrol and genistein killed multidrug-resistant cancer cells. We therefore propose that resveratrol, genistein, and baicalein are attractive candidates for improved chemotherapeutic agents... - High-throughput Giardia lamblia viability assay using bioluminescent ATP content measurementsCatherine Z Chen
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
Antimicrob Agents Chemother 55:667-75. 2011..The most potent novel compound was fumagillin, which showed 50% inhibitory concentrations of 10 nM against the WB isolate and 2 nM against the GS isolate... - A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2Ronald L Johnson
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD, USA
J Biomol Screen 16:618-27. 2011..Selected compounds were tested as independent samples, and a methylsulfonylnitrobenzoate series inhibited the TRβ-SRC2 interaction with 5 µM IC(50). This series represents a new class of thyroid hormone receptor-coactivator modulators... - A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductaseWendy A Lea
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Assay Drug Dev Technol 6:551-5. 2008..This assay is further applicable to the testing of other redox enzymes that utilize DTNB as a model substrate... - Discovery, synthesis, and biological evaluation of novel SMN protein modulatorsJingbo Xiao
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Rockville, Maryland 20850, USA
J Med Chem 54:6215-33. 2011..We anticipate that a lead candidate chosen from this series may serve as a useful probe for exploring the therapeutic benefits of SMN protein up-regulation in SMA animal models and a starting point for clinical development... - A new resorufin-based alpha-glucosidase assay for high-throughput screeningOmid Motabar
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anal Biochem 390:79-84. 2009..Therefore, this new fluorogenic substrate is a useful tool for the alpha-glucosidase enzyme assay and will facilitate compound screening for the development of new therapies for Pompe disease... - Two high-throughput screening assays for aberrant RNA-protein interactions in myotonic dystrophy type 1Catherine Z Chen
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anal Bioanal Chem 402:1889-98. 2012..These assays are homogenous and successfully miniaturized to 1,536-well plate format. Both assays were validated and show robust signal-to-basal ratios and Z' factors... - Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interactionAnton Simeonov
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anal Biochem 375:60-70. 2008..Faced with a traditionally difficult protein-protein interaction assay, by performing two-fluorophore qHTS, we were able to confidently select a number of actives for further studies... - Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verificationAnton Simeonov
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Assay Drug Dev Technol 5:815-24. 2007..We discuss the benefits of microPLC and its limitations from the standpoint of ease of use and integration into a seamless postscreen workflow... - A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channelSteven A Titus
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anal Biochem 394:30-8. 2009..Our findings indicate that this thallium flux assay can be used as an alternative method to profile large-volume compound libraries for compound activity on the hERG channel... - Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodentsPeixiong Yuan
Biomarker Laboratory, National Institute of Mental Health, Mood and Anxiety Disorders Program, National Institutes of Health, Bethesda, MD 20892, USA
Pharmacol Biochem Behav 98:349-55. 2011..The results suggest that PDE4 may be a plausible contributor to the sexual pleasure-seeking deficits seen in depressed patients; inhibiting PDE4 may restore these deficits... - Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate formatDouglas S Auld
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892, USA
Methods Enzymol 414:566-89. 2006..This chapter illustrates the application of microplate laser cytometry to these assays in a manner that is suitable for screening large compound collections in high throughput... - Chemical genomics profiling of environmental chemical modulation of human nuclear receptorsRuili Huang
National Institutes of Health Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 3370, USA
Environ Health Perspect 119:1142-8. 2011.... - A dual-fluorescence high-throughput cell line system for probing multidrug resistanceKyle R Brimacombe
Laboratory of Cell Biology, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
Assay Drug Dev Technol 7:233-49. 2009.... - N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher diseaseWenwei Huang
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
Bioorg Med Chem Lett 17:5783-9. 2007..Synthesis, structure activity relationships and the selectivity of chosen analogues against related sugar hydrolases enzymes are described... - Comparison on Functional Assays for Gq-Coupled GPCRs by Measuring Inositol Monophospate-1 and Intracellular Calcium in 1536-Well Plate FormatKe Liu
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Curr Chem Genomics 1:70-8. 2008..This IP-One assay offers an alternative method for high throughput screening of Gq-coupled GPCRs without using costly kinetic plate readers... - A real-time fluorescence method for enzymatic characterization of specialized human DNA polymerasesDorjbal Dorjsuren
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Nucleic Acids Res 37:e128. 2009..The fluorogenic method presented here should facilitate mechanistic and inhibitor investigations of these polymerases and is also applicable to the study of highly processive replicative polymerases... - Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screeningSunita J Shukla
NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland, USA
Assay Drug Dev Technol 7:143-69. 2009..The CRC information was also used to define chemotypes associated with PXR ligands. This study demonstrates the feasibility of profiling thousands of compounds against PXR using the TR-FRET assay in a high-throughput format... - A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interactionAdam J Kimple
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Comb Chem High Throughput Screen 11:396-409. 2008..84 and 0.66 for the green- and red-label assays, respectively... - Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical librariesJames Inglese
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Proc Natl Acad Sci U S A 103:11473-8. 2006..qHTS produces rich data sets that can be immediately mined for reliable biological activities, thereby providing a platform for chemical genomics and accelerating the identification of leads for drug discovery... - Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher diseaseWei Zheng
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
Proc Natl Acad Sci U S A 104:13192-7. 2007..These small molecules have potential as leads for chaperone therapy for Gaucher disease, and this paradigm promises to accelerate the development of leads for other rare genetic disorders... - A cell-based assay for IkappaBalpha stabilization using a two-color dual luciferase-based sensorR Eric Davis
Metabolism Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892 3370, USA
Assay Drug Dev Technol 5:85-103. 2007..Known and unexpected inhibitors of NFkappaB signaling were identified from the bioactive collection. We describe here the development and performance of this assay, and discuss the merits of its specific features... - Tetracycline-inducible gene expression in conditionally immortalized mouse podocytesHiroshi Kajiyama
Kidney Disease Section, Kidney Disease Branch, National Institute of Diabetes, Digestive and Kidney Diseases, Bethesda, MD 20892 1268, USA
Am J Nephrol 29:153-63. 2009..Conditionally immortalized podocytes are valuable research tools but are difficult to efficiently transfect and do not provide graded transgene expression... - Identification of a potent new chemotype for the selective inhibition of PDE4Amanda P Skoumbourdis
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
Bioorg Med Chem Lett 18:1297-303. 2008..Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented... - Measure, mine, model, and manipulate: the future for HTS and chemoinformatics?Christian N Parker
Drug Discov Today 11:863-5. 2006 - Molecular characterization of the murine SIGNR1 gene encoding a C-type lectin homologous to human DC-SIGN and DC-SIGNRStephen A Parent
Department of Immunology and Rheumatology, Merck Research Laboratories, PO Box 2000, RY 80Y 225, Rahway, NJ 07065, USA
Gene 293:33-46. 2002..In situ hybridization and immunocytochemistry experiments demonstrate that, like human DC-SIGN, the murine messenger RNAs are expressed in subsets of dendritic cells in the spleen and skin... - A high-throughput screen for aggregation-based inhibition in a large compound libraryBrian Y Feng
Department of Pharmaceutical Chemistry and Graduate Group in Chemistry and Chemical Biology, 1700 4th Street, University of California San Francisco, San Francisco, California 94158 2330, USA
J Med Chem 50:2385-90. 2007..Third, aggregate-based inhibition is correlated with steep dose-response curves, although not absolutely. The results of this screen are being released publicly via the PubChem database... - Identification, localization and receptor characterization of novel mammalian substance P-like peptidesMarc M Kurtz
Department of Immunology Rheumatology, Merck Research Laboratories, Rahway, NJ 07065, USA
Gene 296:205-12. 2002..The results indicate that PPT-C encodes another high affinity ligand of the NK1 receptor which may play an important role in mediating some of the physiological roles previously assigned to the NK1 receptor... - Melanin-concentrating hormone receptor subtypes 1 and 2: species-specific gene expressionCarina P Tan
Department of Obesity and Metabolic Research, Merck Research Laboratories, Rahway, NJ 07065, USA
Genomics 79:785-92. 2002.... - Cloning and characterization of Disc1, the mouse ortholog of DISC1 (Disrupted-in-Schizophrenia 1)Lei Ma
Department of Neuroscience, West Point, Pennsylvania 19486, USA
Genomics 80:662-72. 2002..Identification of Disc1 will facilitate the study of DISC1's function and creation of mouse models of DISC1 disruption... - Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamaseKerim Babaoglu
Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, California 94158 2330, USA
J Med Chem 51:2502-11. 2008..Structure-based methods may prioritize weak-but-novel chemotypes in unbiased library screens... - DISC1 (Disrupted-In-Schizophrenia 1) is a centrosome-associated protein that interacts with MAP1A, MIPT3, ATF4/5 and NUDEL: regulation and loss of interaction with mutationJill A Morris
Department of Neuroscience, Merck Research Laboratories, West Point, PA 19486, USA
Hum Mol Genet 12:1591-608. 2003.... - Identification of oxadiazoles as new drug leads for the control of schistosomiasisAhmed A Sayed
Department of Biological Sciences, Illinois State University, Normal, Illinois 61790, USA
Nat Med 14:407-12. 2008..The compound was active against the three major schistosome species infecting humans. These protective effects exceed benchmark activity criteria set by the World Health Organization for lead compound development for schistosomiasis... - Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activationYuli Xie
Division of Clinical Pharmacology and Experimental Therapeutics, Department of Medicine, Columbia University, 630 West 168th Street, New York, NY 10032, USA
Bioorg Med Chem Lett 18:329-35. 2008..The series exhibited potencies in the cell-based assays at as low as 0.6 microM, and several indications suggest that the targeted activity lies within a common region of the NFkappaB pathway...