1
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Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury.
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Nat Chem Biol
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2005
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11.63
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2
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Identification of RIP1 kinase as a specific cellular target of necrostatins.
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Nat Chem Biol
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2008
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9.24
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3
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BMP type I receptor inhibition reduces heterotopic [corrected] ossification.
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Nat Med
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2008
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4.20
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4
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Pharmacologic inhibition of the anaphase-promoting complex induces a spindle checkpoint-dependent mitotic arrest in the absence of spindle damage.
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Cancer Cell
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2010
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2.08
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5
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Necrostatin-1 reduces histopathology and improves functional outcome after controlled cortical impact in mice.
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J Cereb Blood Flow Metab
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2008
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2.06
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6
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Necroptosis, a novel form of caspase-independent cell death, contributes to neuronal damage in a retinal ischemia-reperfusion injury model.
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J Neurosci Res
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2010
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1.89
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7
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Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell line.
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Chem Biol
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2003
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1.85
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8
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Structure-activity relationship study of novel necroptosis inhibitors.
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Bioorg Med Chem Lett
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2005
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1.72
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9
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Inhibition of bone morphogenetic protein signaling attenuates anemia associated with inflammation.
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Blood
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2011
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1.61
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10
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Structure-activity relationship study of novel tissue transglutaminase inhibitors.
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Bioorg Med Chem Lett
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2005
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1.38
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11
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A new class of small molecule inhibitor of BMP signaling.
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PLoS One
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2013
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1.36
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12
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The structural basis of Cryptosporidium -specific IMP dehydrogenase inhibitor selectivity.
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J Am Chem Soc
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2010
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1.35
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13
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Designed inhibitors of insulin-degrading enzyme regulate the catabolism and activity of insulin.
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PLoS One
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2010
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1.35
|
14
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Triazole inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.
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J Med Chem
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2009
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1.33
|
15
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Structure-activity relationship study of tricyclic necroptosis inhibitors.
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J Med Chem
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2007
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1.27
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16
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Carboetomidate: a pyrrole analog of etomidate designed not to suppress adrenocortical function.
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Anesthesiology
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2010
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1.27
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17
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Identification of translational activators of glial glutamate transporter EAAT2 through cell-based high-throughput screening: an approach to prevent excitotoxicity.
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J Biomol Screen
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2010
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1.14
|
18
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Identification of small molecule inhibitors of the mitotic kinase haspin by high-throughput screening using a homogeneous time-resolved fluorescence resonance energy transfer assay.
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J Biomol Screen
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2008
|
1.13
|
19
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Small molecules that enhance the catalytic efficiency of HLA-DM.
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J Immunol
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2006
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1.10
|
20
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Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1.
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Cell Rep
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2015
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1.09
|
21
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Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.
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J Med Chem
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2013
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1.09
|
22
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Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection.
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J Clin Invest
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2014
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1.06
|
23
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Small-molecule activators of insulin-degrading enzyme discovered through high-throughput compound screening.
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PLoS One
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2009
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1.03
|
24
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Validation of IMP dehydrogenase inhibitors in a mouse model of cryptosporidiosis.
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Antimicrob Agents Chemother
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2013
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1.03
|
25
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In vivo and in vitro pharmacological studies of methoxycarbonyl-carboetomidate.
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Anesth Analg
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2011
|
1.01
|
26
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Selective and potent urea inhibitors of cryptosporidium parvum inosine 5'-monophosphate dehydrogenase.
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J Med Chem
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2012
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1.01
|
27
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Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.
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Bioorg Med Chem Lett
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2012
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1.00
|
28
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Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.
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Mol Cancer Ther
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2013
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0.99
|
29
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Kinetic studies of Cdk5/p25 kinase: phosphorylation of tau and complex inhibition by two prototype inhibitors.
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Biochemistry
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2008
|
0.99
|
30
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Development of an ALK2-biased BMP type I receptor kinase inhibitor.
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ACS Chem Biol
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2013
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0.99
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31
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Defining Cdk5 ligand chemical space with small molecule inhibitors of tau phosphorylation.
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Chem Biol
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2005
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0.98
|
32
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Biological properties of novel antistaphylococcal quinoline-indole agents.
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Antimicrob Agents Chemother
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2003
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0.97
|
33
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Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus.
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Bioorg Med Chem Lett
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2010
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0.97
|
34
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Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors.
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Bioorg Med Chem Lett
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2007
|
0.96
|
35
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Identification of novel small molecules that elevate Klotho expression.
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Biochem J
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2012
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0.95
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36
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Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators.
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Bioorg Med Chem Lett
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2011
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0.95
|
37
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Genetic ablation or chemical inhibition of phosphatidylcholine transfer protein attenuates diet-induced hepatic glucose production.
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Hepatology
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2011
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0.94
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38
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Phthalazinone inhibitors of inosine-5'-monophosphate dehydrogenase from Cryptosporidium parvum.
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Bioorg Med Chem Lett
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2012
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0.94
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39
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In vivo enhancement of peptide display by MHC class II molecules with small molecule catalysts of peptide exchange.
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J Immunol
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2009
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0.93
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40
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FDA-preapproved drugs targeted to the translational regulation and processing of the amyloid precursor protein.
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J Mol Neurosci
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2004
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0.92
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41
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Synthesis, in vitro evaluation and cocrystal structure of 4-oxo-[1]benzopyrano[4,3-c]pyrazole Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase (CpIMPDH) inhibitors.
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J Med Chem
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2014
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0.91
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42
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Small-molecule Klotho enhancers as novel treatment of neurodegeneration.
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Future Med Chem
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2012
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0.89
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43
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RNA therapeutics directed to the non coding regions of APP mRNA, in vivo anti-amyloid efficacy of paroxetine, erythromycin, and N-acetyl cysteine.
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Curr Alzheimer Res
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2006
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0.88
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44
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Akt Regulates TNFα synthesis downstream of RIP1 kinase activation during necroptosis.
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PLoS One
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2013
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0.88
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45
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Small-molecule inhibitors of phosphatidylcholine transfer protein/StarD2 identified by high-throughput screening.
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Anal Biochem
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2008
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0.87
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46
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Lowering of amyloid beta peptide production with a small molecule inhibitor of amyloid-β precursor protein dimerization.
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Am J Neurodegener Dis
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2012
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0.87
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47
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Identification of novel compounds that increase SMN protein levels using an improved SMN2 reporter cell assay.
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J Biomol Screen
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2012
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0.86
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48
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Development of a mechanism-based high-throughput screen assay for leucine-rich repeat kinase 2--discovery of LRRK2 inhibitors.
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Anal Biochem
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2010
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0.86
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49
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Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors.
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Bioorg Med Chem Lett
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2007
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0.86
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50
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One-pot synthesis of alpha-carbolines via sequential palladium-catalyzed aryl amination and intramolecular arylation.
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J Org Chem
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2009
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0.85
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51
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Kinetic, mechanistic, and structural modeling studies of truncated wild-type leucine-rich repeat kinase 2 and the G2019S mutant.
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Biochemistry
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2011
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0.85
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52
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Enhancement of SMN protein levels in a mouse model of spinal muscular atrophy using novel drug-like compounds.
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EMBO Mol Med
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2013
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0.84
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53
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Glutamate transporter EAAT2: a new target for the treatment of neurodegenerative diseases.
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Future Med Chem
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2012
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0.84
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54
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Syntheses of aporphine and homoaporphine alkaloids by intramolecular ortho-arylation of phenols with aryl halides via SRN1 reactions in liquid ammonia.
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J Org Chem
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2006
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0.83
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55
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Improving binding specificity of pharmacological chaperones that target mutant superoxide dismutase-1 linked to familial amyotrophic lateral sclerosis using computational methods.
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J Med Chem
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2010
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0.83
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56
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New approaches to the discovery of cdk5 inhibitors.
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Curr Alzheimer Res
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2007
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0.83
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57
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Effects of a verbenachalcone derivative on neurite outgrowth, inhibition of caspase induction and gene expression.
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Bioorg Med Chem Lett
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2005
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0.83
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58
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Diaminothiazoles modify Tau phosphorylation and improve the tauopathy in mouse models.
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J Biol Chem
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2013
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0.83
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59
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Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors.
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Bioorg Med Chem Lett
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2008
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0.82
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60
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Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.
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Bioorg Med Chem Lett
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2009
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0.82
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61
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Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.
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Bioorg Med Chem Lett
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2011
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0.82
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62
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A high-throughput screen to identify inhibitors of SOD1 transcription.
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Front Biosci (Elite Ed)
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2012
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0.80
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63
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Expression and purification of active receptor interacting protein 1 kinase using a baculovirus system.
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Protein Expr Purif
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2013
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0.80
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64
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Synthesis of carbolines by photostimulated cyclization of anilinohalopyridines.
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J Org Chem
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2011
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0.79
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65
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Optimization of tricyclic Nec-3 necroptosis inhibitors for in vitro liver microsomal stability.
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Bioorg Med Chem Lett
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2012
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0.79
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66
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Type II kinase inhibitors show an unexpected inhibition mode against Parkinson's disease-linked LRRK2 mutant G2019S.
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Biochemistry
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2013
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0.79
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67
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Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1.
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Anal Biochem
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2012
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0.78
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68
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Intramolecular Aldol reaction of N-acylated (2-aminophenyl)-alpha-oxoacetic acids: rapid access to tri- and tetracyclic 1,2-dihydroquinolin-2(1H)-ones.
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J Org Chem
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2010
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0.78
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69
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Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
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J Med Chem
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2014
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0.78
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70
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Kinetic-based high-throughput screening assay to discover novel classes of macrophage migration inhibitory factor inhibitors.
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J Biomol Screen
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2010
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0.77
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71
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A mild, one-pot Stadler-Ziegler synthesis of arylsulfides facilitated by photoredox catalysis in batch and continuous-flow.
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Angew Chem Int Ed Engl
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2013
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0.77
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72
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Synthesis of hydantoins from enantiomerically pure alpha-amino amides without epimerization.
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J Org Chem
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2006
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0.77
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73
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Synthesis, receptor binding and functional studies of mesoridazine stereoisomers.
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Bioorg Med Chem Lett
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2004
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0.75
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74
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Synthesis of fused imidazoles, pyrroles, and indoles with a defined stereocenter α to nitrogen utilizing Mitsunobu alkylation followed by palladium-catalyzed cyclization.
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J Org Chem
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2011
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0.75
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75
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Synthesis of tetracyclic indoles via intramolecular α-arylation of ketones.
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J Org Chem
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2012
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0.75
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76
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Synthesis of the indolizino[7,6-c]quinoline alkaloid isaindigotidione.
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Org Lett
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2010
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0.75
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77
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Synthetic studies of 7-oxygenated aporphine alkaloids: preparation of (-)-oliveroline, (-)-nornuciferidine, and derivatives.
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Org Lett
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2015
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0.75
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78
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Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)tetrahydroquinoline derivatives.
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Bioorg Med Chem Lett
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2002
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0.75
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