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4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth

artículo científico publicado en 2014

A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase

artículo científico publicado en 2008

A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models

artículo científico publicado en 2016

A Platform to Enable the Pharmacological Profiling of Small Molecules in Gel-Based Electrophoretic Mobility Shift Assays

artículo científico publicado en 2016

A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors

artículo científico publicado en 2010

A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ

artículo científico publicado en 2012

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding

artículo científico publicado en 2014

A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

artículo científico publicado en 2012

A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction

artículo científico publicado en 2008

A high throughput screen identifies potent and selective inhibitors to human epithelial 15-lipoxygenase-2

artículo científico publicado en 2014

A high-throughput 1,536-well luminescence assay for glutathione S-transferase activity

artículo científico publicado en 2010

A high-throughput approach for identification of novel general anesthetics

artículo científico publicado en 2009

A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein

artículo científico publicado en 2014

A high-throughput screen for aggregation-based inhibition in a large compound library

artículo científico publicado en 2007

A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

artículo científico publicado en 2010

A homogeneous method for investigation of methylation-dependent protein-protein interactions in epigenetics

artículo científico publicado en 2009

A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation

artículo científico publicado en 2013

A miniaturized screen for inhibitors of Jumonji histone demethylases

artículo científico publicado en 2009

A panel of diverse assays to interrogate the interaction between glucokinase and glucokinase regulatory protein, two vital proteins in human disease

artículo científico publicado en 2014

A potent and selective inhibitor targeting human and murine 12/15-LOX.

artículo científico publicado en 2016

A real-time fluorescence method for enzymatic characterization of specialized human DNA polymerases

artículo científico publicado en 2009

A robotic platform for quantitative high-throughput screening

artículo científico publicado en 2008

A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells

artículo científico publicado en 2013

A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth

artículo científico publicado en 2013

A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase

artículo científico publicado en 2009

Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration

artículo científico publicado en 2014

AlphaScreen-Based Assays: Ultra-High-Throughput Screening for Small-Molecule Inhibitors of Challenging Enzymes and Protein-Protein Interactions

artículo científico publicado en 2016

An Automated High-Throughput Metabolic Stability Assay Using an Integrated High-Resolution Accurate Mass Method and Automated Data Analysis Software

artículo científico publicado en 2016

Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery

scholarly article by Nathan P Coussens et al published 1 September 2018 in Clinical and Translational Science

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays

artículo científico publicado en 2017

Avoiding Fluorescence Assay Interference-The Case for Diaphorase

artículo científico publicado en 2016

Biochemical assays for the discovery of TDP1 inhibitors

artículo científico publicado en 2014

Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1.

artículo científico publicado en 2014

Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space

Cell Lysate-Based AlphaLISA Deubiquitinase Assay Platform for Identification of Small Molecule Inhibitors

artículo científico publicado en 2017

Cell-based assays to support the profiling of small molecules with histone methyltransferase and demethylase modulatory activity

artículo científico publicado en 2015

Characterization of chemical libraries for luciferase inhibitory activity

artículo científico publicado en 2008

Comment on "On the Utility of ToxCast™ and ToxPi as Methods for Identifying New Obesogens".

artículo científico publicado en 2017

Complementarity Between a Docking and a High-Throughput Screen in Discovering New Cruzain Inhibitors

artículo científico publicado en 2010

Complementary non-radioactive assays for investigation of human flap endonuclease 1 activity ⬇️

artículo científico publicado el 9 de noviembre de 2010

Compound Management for Quantitative High-Throughput Screening

artículo científico publicado en 2008

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

artículo científico publicado en 2008

Concise review: modeling central nervous system diseases using induced pluripotent stem cells

artículo científico publicado en 2014

Controversies in ASSAY and Drug Development Technologies: A Focus on Assessing Irreproducibility

artículo científico publicado en 2014

Correction: A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity.

artículo científico publicado en 2018

Correction: A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models

artículo científico publicado en 2016

Covalent small molecule inhibitors of Ca(2+)-bound S100B.

artículo científico publicado en 2014

Current approaches for the discovery of drugs that deter substance and drug abuse

artículo científico publicado en 2014

Diaphorase Coupling Protocols for Red-Shifting Dehydrogenase Assays

artículo científico publicado en 2016

Differential scanning fluorometry signatures as indicators of enzyme inhibitor mode of action: case study of glutathione S-transferase ⬇️

artículo científico publicado el 30 de abril de 2012

Discovery and optimization of piperazine-1-thiourea-based human phosphoglycerate dehydrogenase inhibitors

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1)

artículo científico publicado en 2015

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

artículo científico publicado en 2009

Discovery of a novel dual fungal CYP51/human 5-lipoxygenase inhibitor: implications for anti-fungal therapy

artículo científico publicado en 2013

Discovery of a novel general anesthetic chemotype using high-throughput screening

artículo científico publicado en 2015

Discovery of a novel noniminosugar acid α glucosidase chaperone series

artículo científico publicado en 2012

Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase

artículo científico publicado en 2011

Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

artículo científico publicado en 2010

Disrupting malaria parasite AMA1-RON2 interaction with a small molecule prevents erythrocyte invasion

artículo científico publicado en 2013

Diverse small molecule inhibitors of human apurinic/apyrimidinic endonuclease APE1 identified from a screen of a large public collection

artículo científico publicado en 2012

Donated chemical probes for open science

artículo científico publicado en 2018

Drug discovery and development for rare genetic disorders

article

Drug repurposing screens and synergistic drug-combinations for infectious diseases

artículo científico

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction

artículo científico publicado en 2007

Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities

artículo científico publicado en 2017

Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibiting viral replication and decreasing viral entry.

artículo científico publicado en 2018

Enzyme assays by fluorescence polarization in the presence of polyarginine: study of kinase, phosphatase, and protease reactions

artículo científico publicado en 2002

Erratum: A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth

scientific article published in Nature Communications

Erratum: Prediction of human population responses to toxic compounds by a collaborative competition

article

Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification

artículo científico publicado en 2007

Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity

artículo científico publicado en 2011

Expanding biological space coverage enhances the prediction of drug adverse effects in human using in vitro activity profiles

artículo científico publicado en 2018

Exploratory analysis of kinetic solubility measurements of a small molecule library

artículo científico publicado en 2011

Firefly Luciferase in Chemical Biology: A Compendium of Inhibitors, Mechanistic Evaluation of Chemotypes, and Suggested Use As a Reporter

artículo científico publicado en 2012

First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis

artículo científico

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

artículo científico publicado en 2016

Fluorescence polarization assays in small molecule screening ⬇️

artículo científico publicado el 1 de enero de 2011

Fluorescence spectroscopic profiling of compound libraries

artículo científico publicado en 2008

Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format

artículo científico publicado en 2006

Gene expression analysis identifies global gene dosage sensitivity in cancer.

artículo científico publicado en 2015

High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships

artículo científico publicado en 2010

High-throughput 1,536-well fluorescence polarization assays for α(1)-acid glycoprotein and human serum albumin binding

artículo científico publicado en 2012

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells

artículo científico publicado en 2014

High-throughput fluorescence imaging approaches for drug discovery using in vitro and in vivo three-dimensional models

artículo científico publicado en 2015

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe

artículo científico publicado en 2013

High-throughput screen identifies cyclic nucleotide analogs that inhibit prostatic acid phosphatase

artículo científico publicado en 2012

High-throughput screening assays for the identification of chemical probes

artículo científico publicado en 2007

High-throughput screening for modulators of cellular contractile force

artículo científico publicado en 2015

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

artículo científico publicado en 2010

Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1

artículo científico publicado en 2009

Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase

artículo científico publicado en 2013

Identification of oxadiazoles as new drug leads for the control of schistosomiasis

artículo científico publicado en 2008

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay

artículo científico publicado en 2009

Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening

artículo científico publicado en 2009

Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen

artículo científico publicado en 2016

Identifying environmental chemicals as agonists of the androgen receptor by using a quantitative high-throughput screening platform

artículo científico publicado en 2017

In vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents

artículo científico publicado en 2016

Induced Pluripotent Stem Cell Models to Enable In Vitro Models for Screening in the Central Nervous System

artículo científico publicado en 2015

Inheritance of rare functional GCKR variants and their contribution to triglyceride levels in families

artículo científico publicado en 2014

Inhibition of DNA glycosylases via small molecule purine analogs

artículo científico publicado en 2013

Inhibition of thioredoxin reductase 1 by porphyrins and other small molecules identified by a high-throughput screening assay

artículo científico publicado en 2011

Inhibitors of the apurinic/apyrimidinic endonuclease 1 (APE1)/nucleophosmin (NPM1) interaction that display anti-tumor properties

artículo científico publicado en 2015

Integration of pro-inflammatory cytokines, 12-lipoxygenase and NOX-1 in pancreatic islet beta cell dysfunction

artículo científico publicado en 2012

KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes

artículo científico publicado en 2015

KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance

Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors ⬇️

artículo científico publicado el 10 de julio de 2013

Large-Scale Screening and Identification of Novel Ebola Virus and Marburg Virus Entry Inhibitors

artículo científico publicado en 2016

Literature Search and Review

artículo científico publicado en 2017

Literature Search and Review

article

Literature Search and Review

Literature Search and Review

scholarly article by Doug Auld et al published August 2010 in Assay and Drug Development Technologies

Literature search and review

scientific article published on June 2011

Method for Assaying the Lipid Kinase Phosphatidylinositol-5-phosphate 4-kinase α in Quantitative High-Throughput Screening (qHTS) Bioluminescent Format

artículo científico publicado en 2016

Methods for Activity Analysis of the Proteins that Regulate Histone Methylation ⬇️

artículo científico publicado el 22 de agosto de 2011

Microfluidic Mobility Shift Profiling of Lysine Acetyltransferases Enables Screening and Mechanistic Analysis of Cellular Acetylation Inhibitors.

artículo científico publicado en 2015

Microscale thermophoresis quantifies biomolecular interactions under previously challenging conditions

artículo científico publicado en 2012

Modelling the Tox21 10 K chemical profiles for in vivo toxicity prediction and mechanism characterization

artículo científico publicado en 2016

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

artículo científico publicado en 2010

Non-iminosugar glucocerebrosidase small molecule chaperones

artículo científico publicado en 2011

Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays

artículo científico publicado en 2015

Peroxiredoxin-1 from the Human Hookworm Ancylostoma ceylanicum Forms a Stable Oxidized Decamer and Is Covalently Inhibited by Conoidin A

artículo científico publicado en 2013

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor

scientific article published on 10 June 2013

Platelet 12-LOX is essential for FcγRIIa-mediated platelet activation

artículo científico publicado en 2014

Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies

artículo científico publicado en 2014

Prediction of human population responses to toxic compounds by a collaborative competition

artículo científico publicado en 2015

Preparation of FRET reporters to support chemical probe development

artículo científico publicado en 2010

Profiling of the Tox21 10K compound library for agonists and antagonists of the estrogen receptor alpha signaling pathway

artículo científico publicado en 2014

Profiling of the Tox21 chemical collection for mitochondrial function to identify compounds that acutely decrease mitochondrial membrane potential

artículo científico publicado en 2014

Protein kinase C regulation of 12-lipoxygenase-mediated human platelet activation

artículo científico publicado en 2011

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines

artículo científico publicado en 2010

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

artículo científico publicado en 2010

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

artículo científico publicado en 2010

Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing

artículo científico publicado en 2017

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

artículo científico publicado en 2008

Quantitative high-throughput screening identifies cytoprotective molecules that enhance SUMO conjugation via the inhibition of SUMO-specific protease (SENP)2.

artículo científico publicado en 2017

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries

artículo científico publicado en 2006

Recent developments in the use of differential scanning fluorometry in protein and small molecule discovery and characterization ⬇️

artículo científico publicado el 6 de junio de 2013

Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells

artículo científico publicado en 2011

Selective inhibition of 12-lipoxygenase protects islets and beta cells from inflammatory cytokine-mediated beta cell dysfunction

artículo científico publicado en 2014

Single nucleotide polymorphism genotyping using short, fluorescently labeled locked nucleic acid (LNA) probes and fluorescence polarization detection

artículo científico publicado en 2002

Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models

artículo científico publicado en 2016

Small molecule inhibitors of DNA repair nuclease activities of APE1 ⬇️

artículo científico publicado el 31 de agosto de 2010

Small-Molecule Screens: A Gateway to Cancer Therapeutic Agents with Case Studies of Food and Drug Administration-Approved Drugs

artículo científico publicado en 2017

Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds

artículo científico publicado en 2016

Structural insight into exosite binding and discovery of novel exosite inhibitors of botulinum neurotoxin serotype A through in silico screening

artículo científico publicado en 2014

Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis

artículo científico publicado en 2009

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors

artículo científico publicado en 2013

Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition

artículo científico publicado en 2014

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

artículo científico publicado en 2013

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

artículo científico publicado en 2014

Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer

artículo científico publicado en 2014

Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors

artículo científico publicado en 2012

Targeting iron assimilation to develop new antibacterials

artículo científico publicado en 2012

Targeting the JMJD2 histone demethylases to epigenetically control herpesvirus infection and reactivation from latency

artículo científico publicado en 2013

The NCATS BioPlanet - An Integrated Platform for Exploring the Universe of Cellular Signaling Pathways for Toxicology, Systems Biology, and Chemical Genomics

The Tox21 robotic platform for the assessment of environmental chemicals – from vision to reality ⬇️

artículo científico publicado el 31 de mayo de 2013

The Toxmatrix: Chemo-Genomic Profiling Identifies Interactions That Reveal Mechanisms of Toxicity

artículo científico publicado en 2017

The pilot phase of the NIH Chemical Genomics Center

artículo científico publicado en 2009

Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease

artículo científico publicado en 2007

Tox21Challenge to Build Predictive Models of Nuclear Receptor and Stress Response Pathways as Mediated by Exposure to Environmental Chemicals and Drugs

article

Translating Stem Cell Biology Into Drug Discovery

artículo científico publicado en 2016

Ubiquitin-Specific Proteases as Druggable Targets

artículo científico publicado en 2015

Unexplored therapeutic opportunities in the human genome.

artículo científico publicado en 2018

[none]

artículo científico publicado en 2013

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