Douglas S Auld

Author PubWeight™ 66.28‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries. Proc Natl Acad Sci U S A 2006 9.92
2 Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses. Science 2011 5.72
3 High-throughput screening assays for the identification of chemical probes. Nat Chem Biol 2007 4.50
4 Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol 2012 3.40
5 Fluorescence spectroscopic profiling of compound libraries. J Med Chem 2008 2.53
6 COPI complex is a regulator of lipid homeostasis. PLoS Biol 2008 2.47
7 Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology. Chem Biol 2010 1.83
8 Apparent activity in high-throughput screening: origins of compound-dependent assay interference. Curr Opin Chem Biol 2010 1.76
9 Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem 2010 1.61
10 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
11 Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries. Nat Biotechnol 2009 1.30
12 Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Biochemistry 2009 1.28
13 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
14 A dual-fluorescence high-throughput cell line system for probing multidrug resistance. Assay Drug Dev Technol 2009 1.22
15 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
16 Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter. Chem Biol 2012 1.14
17 Identification of clinically used drugs that activate pregnane X receptors. Drug Metab Dispos 2010 1.14
18 Mechanistic studies with potent and selective inducible nitric-oxide synthase dimerization inhibitors. J Biol Chem 2001 1.14
19 Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk). Bioorg Med Chem Lett 2009 1.06
20 Comparison of bioluminescent kinase assays using substrate depletion and product formation. Assay Drug Dev Technol 2009 1.04
21 A cell-based assay for IkappaBalpha stabilization using a two-color dual luciferase-based sensor. Assay Drug Dev Technol 2007 1.01
22 A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One 2013 1.00
23 The trypanocidal drug suramin and other trypan blue mimetics are inhibitors of pyruvate kinases and bind to the adenosine site. J Biol Chem 2011 1.00
24 Monitoring compound integrity with cytochrome P450 assays and qHTS. J Biomol Screen 2009 0.95
25 2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. Bioorg Med Chem Lett 2011 0.94
26 The pilot phase of the NIH Chemical Genomics Center. Curr Top Med Chem 2009 0.94
27 A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety. ChemMedChem 2010 0.91
28 Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors. Biochem Biophys Res Commun 2013 0.89
29 Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). Bioorg Med Chem Lett 2011 0.89
30 Reporter enzyme inhibitor study to aid assembly of orthogonal reporter gene assays. ACS Chem Biol 2013 0.89
31 A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTS. Comb Chem High Throughput Screen 2008 0.88
32 Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors. Chem Biol 2011 0.88
33 Identification of a novel allosteric binding site in the CXCR2 chemokine receptor. Mol Pharmacol 2011 0.84
34 Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists. Bioorg Med Chem Lett 2006 0.84
35 Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation. Bioorg Med Chem Lett 2007 0.83
36 Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett 2013 0.82
37 Research resource: modulators of glucocorticoid receptor activity identified by a new high-throughput screening assay. Mol Endocrinol 2014 0.81
38 Identification of therapeutic candidates for chronic lymphocytic leukemia from a library of approved drugs. PLoS One 2013 0.81
39 Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors. Bioorg Med Chem Lett 2009 0.80
40 Evaluation of compound interference in immobilized metal ion affinity-based fluorescence polarization detection with a four million member compound collection. Assay Drug Dev Technol 2003 0.79
41 A new family of covalent inhibitors block nucleotide binding to the active site of pyruvate kinase. Biochem J 2012 0.77
42 Comparison of compound administration methods in biochemical assays: effects on apparent compound potency using either assay-ready compound plates or pin tool-delivered compounds. J Biomol Screen 2012 0.77
43 Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists. Bioorg Med Chem Lett 2006 0.75
44 Physicochemical characterization of a thermostable alcohol dehydrogenase from Pyrobaculum aerophilum. PLoS One 2013 0.75
45 Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. Bioorg Med Chem Lett 2010 0.75
46 Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. Bioorg Med Chem Lett 2011 0.75
47 Identification and optimization of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V3 (V1b) receptor antagonists. Bioorg Med Chem Lett 2010 0.75