1
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Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma.
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Nature
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2010
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8.78
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2
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Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses.
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Science
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2011
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5.72
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3
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Noncanonical TGFβ signaling contributes to aortic aneurysm progression in Marfan syndrome mice.
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Science
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2011
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3.49
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4
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Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
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Nat Chem Biol
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2012
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3.40
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5
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Identification of oxadiazoles as new drug leads for the control of schistosomiasis.
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Nat Med
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2008
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2.90
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6
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Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550).
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J Immunol
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2011
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2.59
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7
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Fluorescence spectroscopic profiling of compound libraries.
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J Med Chem
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2008
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2.53
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8
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High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells.
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Proc Natl Acad Sci U S A
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2014
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2.50
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9
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Cooperative epigenetic modulation by cancer amplicon genes.
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Cancer Cell
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2010
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2.43
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10
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A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism.
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Endocrinology
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2008
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2.03
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11
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Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants.
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Biochemistry
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2008
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1.82
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12
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Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
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J Med Chem
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2008
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1.81
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CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP.
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Blood
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2010
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1.77
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14
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Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns.
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J Med Chem
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2006
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1.71
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15
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Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124.
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Proc Natl Acad Sci U S A
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2010
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1.64
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16
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Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
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J Med Chem
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2010
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1.61
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17
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Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.
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Proc Natl Acad Sci U S A
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2009
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1.61
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18
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Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade.
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PLoS Negl Trop Dis
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2008
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1.58
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19
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Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
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J Med Chem
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2010
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1.45
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20
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A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR).
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J Biol Chem
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2006
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1.38
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Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
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Bioorg Med Chem Lett
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2010
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1.37
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22
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A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.
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J Med Chem
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2009
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1.34
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23
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Tuning the optical properties of fluorinated indolylfulgimides.
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J Org Chem
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2003
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1.29
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24
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Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition.
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J Med Chem
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2007
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1.26
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25
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Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor.
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J Biomol Screen
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2008
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1.25
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Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H.
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J Med Chem
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2011
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1.24
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27
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"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
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J Med Chem
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2005
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1.21
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28
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A virtual screen for diverse ligands: discovery of selective G protein-coupled receptor antagonists.
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J Am Chem Soc
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2008
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1.20
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29
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A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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Endocrinology
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30
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Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008.
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J Comb Chem
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TCR signaling via Tec kinase ITK and interferon regulatory factor 4 (IRF4) regulates CD8+ T-cell differentiation.
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Proc Natl Acad Sci U S A
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2012
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1.13
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32
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Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion.
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Proc Natl Acad Sci U S A
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2010
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1.13
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33
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Neuregulin 1-ErbB4-PI3K signaling in schizophrenia and phosphoinositide 3-kinase-p110δ inhibition as a potential therapeutic strategy.
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Proc Natl Acad Sci U S A
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2012
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Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.
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ACS Med Chem Lett
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2011
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35
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Solid-phase synthesis of bleomycin group antibiotics. Construction of a 108-member deglycobleomycin library.
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J Am Chem Soc
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2003
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36
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Structure-guided design of a high-affinity platelet integrin αIIbβ3 receptor antagonist that disrupts Mg²⁺ binding to the MIDAS.
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Sci Transl Med
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2012
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1.07
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37
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Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
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Bioorg Med Chem Lett
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2009
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1.06
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38
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Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.
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J Med Chem
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2009
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1.05
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39
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Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550).
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J Med Chem
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2008
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1.04
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40
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Distinctive inhibition of O-GlcNAcase isoforms by an alpha-GlcNAc thiolsulfonate.
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J Am Chem Soc
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1.04
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41
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Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
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2010
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1.04
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42
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Comparison of bioluminescent kinase assays using substrate depletion and product formation.
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Assay Drug Dev Technol
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2009
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43
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Selective targeting of ITK blocks multiple steps of HIV replication.
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Proc Natl Acad Sci U S A
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2008
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44
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Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2007.
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J Comb Chem
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45
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Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.
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46
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The inhibition and treatment of breast cancer with poly (ADP-ribose) polymerase (PARP-1) inhibitors.
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Int J Biol Sci
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2006
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An O-GlcNAcase-specific inhibitor and substrate engineered by the extension of the N-acetyl moiety.
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J Am Chem Soc
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2006
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0.98
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Structural properties of a series of photochromic fluorinated indolylfulgides.
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Acta Crystallogr C
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2002
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49
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Genomic and functional characterizations of phosphodiesterase subtype 4D in human cancers.
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Proc Natl Acad Sci U S A
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2013
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0.95
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Proteasome inactivation promotes p38 mitogen-activated protein kinase-dependent phosphatidylinositol 3-kinase activation and increases interleukin-8 production in retinal pigment epithelial cells.
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Mol Biol Cell
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2009
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0.95
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51
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Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.
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Bioorg Med Chem
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2009
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2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
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Bioorg Med Chem Lett
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2011
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CD28 and ITK signals regulate autoreactive T cell trafficking.
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Nat Med
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A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety.
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Insulin-dependent diabetes induced by pancreatic beta cell expression of IL-15 and IL-15Rα.
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Proc Natl Acad Sci U S A
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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 disease.
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Bioorg Med Chem Lett
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Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk).
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Bioorg Med Chem Lett
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2011
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Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters.
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Synthesis of Oxadiazole-2-oxide Analogues as Potential Antischistosomal Agents.
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Tetrahedron Lett
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Integrated phosphoproteomic and metabolomic profiling reveals NPM-ALK-mediated phosphorylation of PKM2 and metabolic reprogramming in anaplastic large cell lymphoma.
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Identification of potent Yes1 kinase inhibitors using a library screening approach.
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Identification of a potent new chemotype for the selective inhibition of PDE4.
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Bioorg Med Chem Lett
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2008
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Inhibition of O-GlcNAcase by PUGNAc is dependent upon the oxime stereochemistry.
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Bioorg Med Chem
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A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants.
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Retrovirology
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Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.
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Bioorg Med Chem Lett
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Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
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A 1536-well quantitative high-throughput screen to identify compounds targeting cancer stem cells.
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Exploring the cellular activity of camptothecin-triple-helix-forming oligonucleotide conjugates.
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Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
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Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
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Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells.
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Exploratory analysis of kinetic solubility measurements of a small molecule library.
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Bioorg Med Chem
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Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality.
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Activation of camptothecin derivatives by conjugation to triple helix-forming oligonucleotides.
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Biochemistry
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Multiplexing high-content flow (HCF) and quantitative high-throughput screening (qHTS) to identify compounds capable of decreasing cell viability, activating caspase 3/7, expressing annexin V, and changing mitochondrial membrane integrity.
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Synthesis of Substituted 2-phenylhistamines via a Microwave Promoted Suzuki Coupling.
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Playing well with others! Initiating and sustaining successful collaborations between industry, academia and government.
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Total synthesis of LL-Z1640-2 utilizing a late-stage intramolecular Nozaki-Hiyama-Kishi reaction.
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1-(Phenyl)isoquinoline carboxamides: a novel class of subtype selective inhibitors of thyrotropin-releasing hormone (TRH) receptors.
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