Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.

Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells. Proc Natl Acad Sci U S A (2010) 1.75

Mechanisms of drug resistance in kinases. Expert Opin Investig Drugs (2011) 1.29

Pocketome: an encyclopedia of small-molecule binding sites in 4D. Nucleic Acids Res (2011) 1.21

Molecular dynamics reveal BCR-ABL1 polymutants as a unique mechanism of resistance to PAN-BCR-ABL1 kinase inhibitor therapy. Proc Natl Acad Sci U S A (2014) 1.16

Ten things you should know about protein kinases: IUPHAR Review 14. Br J Pharmacol (2015) 1.06

NMR reveals the allosteric opening and closing of Abelson tyrosine kinase by ATP-site and myristoyl pocket inhibitors. Proc Natl Acad Sci U S A (2013) 1.03

Role of N-terminal myristylation in the structure and regulation of cAMP-dependent protein kinase. J Mol Biol (2012) 0.98

Reply to: Cisplatin-induced primordial follicle oocyte killing and loss of fertility are not prevented by imatinib. Nat Med (2012) 0.97

C-RAF mutations confer resistance to RAF inhibitors. Cancer Res (2013) 0.91

Curcumin derivative C817 inhibits proliferation of imatinib-resistant chronic myeloid leukemia cells with wild-type or mutant Bcr-Abl in vitro. Acta Pharmacol Sin (2014) 0.85

BCR-ABL signaling: A new STATus in CML. Nat Chem Biol (2012) 0.80

Allosteric BCR-ABL inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia: novel opportunities for drug combinations to overcome resistance. Haematologica (2012) 0.79

Defying c-Abl signaling circuits through small allosteric compounds. Front Genet (2014) 0.79

Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism. BMC Cancer (2012) 0.76

Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2. Sci Rep (2016) 0.75

Abl kinase constructs expressed in bacteria: facilitation of structural and functional studies including segmental labeling by expressed protein ligation. Mol Biosyst (2012) 0.75

Fluorophore labeled kinase detects ligands that bind within the MAPK insert of p38α kinase. PLoS One (2012) 0.75

Allosteric Communication Networks in Proteins Revealed through Pocket Crosstalk Analysis. ACS Cent Sci (2017) 0.75

The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity. Nature (2012) 31.78

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

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

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther (2008) 10.35

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

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell (2005) 7.99

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

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

In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res (2005) 5.98

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

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

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

In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell (2004) 4.29

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

Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia. Nat Genet (2004) 3.96

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

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

Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer (2007) 3.36

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

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

Expansion of Bcr-Abl-positive leukemic stem cells is dependent on Hedgehog pathway activation. Cancer Cell (2008) 3.01

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

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

Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma. Sci Transl Med (2010) 2.86

The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. Structure (2005) 2.78

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

PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease. Cancer Cell (2003) 2.70

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

Essential role of stromally induced hedgehog signaling in B-cell malignancies. Nat Med (2007) 2.62

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

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

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

OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib. Blood (2006) 2.29

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

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

The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. Blood (2005) 2.14

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

Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib. J Biol Chem (2008) 2.09

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

Extended kinase profile and properties of the protein kinase inhibitor nilotinib. Biochim Biophys Acta (2009) 2.04

The evolving war on cancer. Cell (2011) 2.02

Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib. Eur J Pharmacol (2008) 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

Insights into RNA unwinding and ATP hydrolysis by the flavivirus NS3 protein. EMBO J (2008) 1.99

Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107). Blood (2006) 1.95

Perspectives on NMR in drug discovery: a technique comes of age. Nat Rev Drug Discov (2008) 1.95

Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res (2010) 1.94

Structural basis for the exceptional in vivo efficacy of bisphosphonate drugs. ChemMedChem (2006) 1.90

Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem (2011) 1.88

Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study. Blood (2007) 1.85

A public-private partnership to unlock the untargeted kinome. Nat Chem Biol (2013) 1.83

Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood (2006) 1.83

AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res (2004) 1.82

TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia. Cancer Discov (2013) 1.81

The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma. Cancer Cell (2012) 1.81

Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol (2013) 1.81