Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem (2013) 0.96

Ethyl 1-phenyl-2-[4-(trifluoro-meth-oxy)phen-yl]-1H-benzimidazole-5-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online (2012) 0.93

Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem (2013) 0.91

Ethyl 1-tert-butyl-2-(4-hydr-oxy-3-methoxy-phen-yl)-1H-benzimidazole-5-carboxyl-ate. Acta Crystallogr Sect E Struct Rep Online (2010) 0.84

Systematic identification of genomic markers of drug sensitivity in cancer cells. Nature (2012) 15.91

The sequence and de novo assembly of the giant panda genome. Nature (2009) 15.76

An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem (2009) 12.73

EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res (2008) 9.29

Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A (2007) 8.23

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature (2009) 7.05

Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature (2008) 6.80

The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling. Science (2011) 6.75

Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res (2008) 6.71

KCNQ1 gain-of-function mutation in familial atrial fibrillation. Science (2003) 6.60

MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A (2009) 6.58

A unifying model for mTORC1-mediated regulation of mRNA translation. Nature (2012) 6.44

DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell (2009) 5.97

The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature (2012) 5.61

The TEAD/TEF family protein Scalloped mediates transcriptional output of the Hippo growth-regulatory pathway. Dev Cell (2008) 5.58

Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science (2010) 5.50

Residual human immunodeficiency virus type 1 viremia in some patients on antiretroviral therapy is dominated by a small number of invariant clones rarely found in circulating CD4+ T cells. J Virol (2006) 5.41

Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol (2006) 5.03

mTORC1-mediated cell proliferation, but not cell growth, controlled by the 4E-BPs. Science (2010) 4.81

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc Natl Acad Sci U S A (2008) 4.80

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer. Cancer Discov (2011) 4.80

Attenuated cold sensitivity in TRPM8 null mice. Neuron (2007) 4.73

Mitogenic influence of human R-spondin1 on the intestinal epithelium. Science (2005) 4.58

Insulin modulates gluconeogenesis by inhibition of the coactivator TORC2. Nature (2007) 4.54

A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. Cancer Res (2011) 4.22

Mesenchymal stem cell-mediated functional tooth regeneration in swine. PLoS One (2006) 3.91

White Collar-1, a circadian blue light photoreceptor, binding to the frequency promoter. Science (2002) 3.85

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A (2006) 3.83

Association between adverse clinical outcome in human disease caused by novel influenza A H7N9 virus and sustained viral shedding and emergence of antiviral resistance. Lancet (2013) 3.83

Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature (2010) 3.39

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem (2013) 3.27

Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med (2010) 3.26

R-Spondin1 regulates Wnt signaling by inhibiting internalization of LRP6. Proc Natl Acad Sci U S A (2007) 3.24

Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer. PLoS One (2011) 3.23

Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol (2008) 3.18

The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers. Cancer Res (2010) 3.16

The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. Nat Chem Biol (2010) 3.15

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science (2011) 3.07

White collar-1, a DNA binding transcription factor and a light sensor. Science (2002) 2.97

Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol (2006) 2.96

Characterization of the apical papilla and its residing stem cells from human immature permanent teeth: a pilot study. J Endod (2008) 2.95

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol (2011) 2.91

Epstein-Barr virus latent membrane protein 1 induces cellular MicroRNA miR-146a, a modulator of lymphocyte signaling pathways. J Virol (2007) 2.88

Practical reconstruction method for bioluminescence tomography. Opt Express (2005) 2.83

RXLR-mediated entry of Phytophthora sojae effector Avr1b into soybean cells does not require pathogen-encoded machinery. Plant Cell (2008) 2.72

mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin. Science (2013) 2.71

In situ kinase profiling reveals functionally relevant properties of native kinases. Chem Biol (2011) 2.69

Identification of a KCNE2 gain-of-function mutation in patients with familial atrial fibrillation. Am J Hum Genet (2004) 2.66

Cryptochrome mediates circadian regulation of cAMP signaling and hepatic gluconeogenesis. Nat Med (2010) 2.65

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A (2007) 2.60

A Kir2.1 gain-of-function mutation underlies familial atrial fibrillation. Biochem Biophys Res Commun (2005) 2.55

An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A (2006) 2.51

Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A (2013) 2.49

Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov (2012) 2.47

MicroRNA-155 is an Epstein-Barr virus-induced gene that modulates Epstein-Barr virus-regulated gene expression pathways. J Virol (2008) 2.45

B-cell receptor activation induces BIC/miR-155 expression through a conserved AP-1 element. J Biol Chem (2007) 2.44

CCL2/CCR2 pathway mediates recruitment of myeloid suppressor cells to cancers. Cancer Lett (2007) 2.43

Antiretroviral therapy to prevent HIV transmission in serodiscordant couples in China (2003-11): a national observational cohort study. Lancet (2012) 2.41

Pure spinal epidural cavernous hemangioma. Acta Neurochir (Wien) (2012) 2.38

Mesenchymal stem cells derived from human gingiva are capable of immunomodulatory functions and ameliorate inflammation-related tissue destruction in experimental colitis. J Immunol (2009) 2.37

Frequent somatic mutations in MAP3K5 and MAP3K9 in metastatic melanoma identified by exome sequencing. Nat Genet (2011) 2.36

Variable fitness impact of HIV-1 escape mutations to cytotoxic T lymphocyte (CTL) response. PLoS Pathog (2009) 2.36

Oct4 pseudogenes are transcribed in cancers. Biochem Biophys Res Commun (2005) 2.34

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms. Nat Med (2011) 2.34

A general strategy for creating "inactive-conformation" abl inhibitors. Chem Biol (2006) 2.27

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol (2010) 2.26

The Drosophila melanogaster transcriptome by paired-end RNA sequencing. Genome Res (2010) 2.25

Diverse pathways generate microRNA-like RNAs and Dicer-independent small interfering RNAs in fungi. Mol Cell (2010) 2.23

Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene. Cancer Res (2010) 2.20

Actin filament dynamics are dominated by rapid growth and severing activity in the Arabidopsis cortical array. J Cell Biol (2009) 2.20

Non-optimal codon usage affects expression, structure and function of clock protein FRQ. Nature (2013) 2.15

Conserved C-terminal motifs required for avirulence and suppression of cell death by Phytophthora sojae effector Avr1b. Plant Cell (2008) 2.15

High-throughput kinase profiling as a platform for drug discovery. Nat Rev Drug Discov (2008) 2.12

Cooperative interactions between CBP and TORC2 confer selectivity to CREB target gene expression. EMBO J (2007) 2.07

Regulation of the Neurospora circadian clock by an RNA helicase. Genes Dev (2004) 2.07

Synthetic small molecules that control stem cell fate. Proc Natl Acad Sci U S A (2003) 2.06

qiRNA is a new type of small interfering RNA induced by DNA damage. Nature (2009) 2.06

The evolving war on cancer. Cell (2011) 2.02

Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One (2012) 2.01

Predictive value of serum HER2 ECD in patients with HER2-positive advanced gastric cancer treated with trastuzumab plus chemotherapy. J Gastroenterol (2015) 2.01

Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem (2010) 2.00

Biocompatible copper(I) catalysts for in vivo imaging of glycans. J Am Chem Soc (2010) 1.98

Phosphorylation of extracellular signal-regulated kinase in primary afferent neurons by noxious stimuli and its involvement in peripheral sensitization. J Neurosci (2002) 1.96

Mutations in NMNAT1 cause Leber congenital amaurosis and identify a new disease pathway for retinal degeneration. Nat Genet (2012) 1.96