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4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase

artículo científico publicado en 2016

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors

artículo científico publicado en 2013

A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade

artículo científico publicado en 2010

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

artículo científico publicado en 2016

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

artículo científico publicado en 2016

Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.

artículo científico publicado en 2013

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

artículo científico publicado en 2016

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

artículo científico publicado en 2012

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor

artículo científico publicado en 2016

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation

artículo científico publicado en 2014

Discovery of the 1,7-diazacarbazole class of inhibitors of checkpoint kinase 1

artículo científico publicado en 2014

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase

artículo científico publicado en 2013

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase

artículo científico publicado en 2014

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

artículo científico publicado en 2013

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

artículo científico publicado en 2014

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

artículo científico publicado en 2016

Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

artículo científico publicado en 2015

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study

artículo científico publicado en 2015

Noncovalent wild-type-sparing inhibitors of EGFR T790M

artículo científico publicado en 2012

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase

artículo científico publicado en 2015

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors

artículo científico publicado en 2018

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

artículo científico publicado en 2011

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

artículo científico publicado en 2012

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

artículo científico publicado en 2015

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

artículo científico publicado en 2013

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

artículo científico publicado en 2010

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

artículo científico publicado en 2014