Published in Bioorg Med Chem on January 25, 2010
A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets. Br J Pharmacol (2012) 0.97
Dinaciclib (SCH727965) inhibits the unfolded protein response through a CDK1- and 5-dependent mechanism. Mol Cancer Ther (2013) 0.94
Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors. Bioorg Med Chem Lett (2011) 0.82
Thamnolia vermicularis extract improves learning ability in APP/PS1 transgenic mice by ameliorating both Aβ and Tau pathologies. Acta Pharmacol Sin (2016) 0.75
Inhibition of CDK5 Alleviates the Cardiac Phenotypes in Timothy Syndrome. Stem Cell Reports (2017) 0.75
Discovery of drug mode of action and drug repositioning from transcriptional responses. Proc Natl Acad Sci U S A (2010) 4.35
Interplay between oncogene-induced DNA damage response and heterochromatin in senescence and cancer. Nat Cell Biol (2011) 2.69
Predictive pharmacokinetic-pharmacodynamic modeling of tumor growth kinetics in xenograft models after administration of anticancer agents. Cancer Res (2004) 2.47
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem (2005) 2.38
A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol (2008) 2.18
CDK inhibitors in cancer therapy: what is next? Trends Pharmacol Sci (2007) 1.95
Crystal structures of anaplastic lymphoma kinase in complex with ATP competitive inhibitors. Biochemistry (2010) 1.94
Through the "gatekeeper door": exploiting the active kinase conformation. J Med Chem (2010) 1.92
PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer. Mol Cancer Ther (2007) 1.67
Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol (2013) 1.65
The experimental uncertainty of heterogeneous public K(i) data. J Med Chem (2012) 1.62
Preclinical evaluation of the tyrosine kinase inhibitor SU11248 as a single agent and in combination with "standard of care" therapeutic agents for the treatment of breast cancer. Mol Cancer Ther (2003) 1.61
PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res (2006) 1.61
Comparability of mixed IC₅₀ data - a statistical analysis. PLoS One (2013) 1.60
Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res (2010) 1.48
Dual modulation of MCL-1 and mTOR determines the response to sunitinib. J Clin Invest (2016) 1.47
Crystal structure of the T315I Abl mutant in complex with the aurora kinases inhibitor PHA-739358. Cancer Res (2007) 1.42
Cross platform microarray analysis for robust identification of differentially expressed genes. BMC Bioinformatics (2007) 1.39
Cdc7 inhibition reveals a p53-dependent replication checkpoint that is defective in cancer cells. Cancer Res (2004) 1.37
Cyclin-dependent kinase 2 functions in normal DNA repair and is a therapeutic target in BRCA1-deficient cancers. Cancer Res (2006) 1.27
Early antiangiogenic activity of SU11248 evaluated in vivo by dynamic contrast-enhanced magnetic resonance imaging in an experimental model of colon carcinoma. Clin Cancer Res (2005) 1.27
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem (2006) 1.22
Total synthesis of spongistatin 1: a synthetic strategy exploiting its latent pseudo-symmetry. Angew Chem Int Ed Engl (2005) 1.18
In vivo assessment of antiangiogenic activity of SU6668 in an experimental colon carcinoma model. Clin Cancer Res (2004) 1.18
PoInTree: a polar and interactive phylogenetic tree. Genomics Proteomics Bioinformatics (2005) 1.18
Pathology tissue-chromatin immunoprecipitation, coupled with high-throughput sequencing, allows the epigenetic profiling of patient samples. Proc Natl Acad Sci U S A (2010) 1.15
3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors. Bioorg Med Chem Lett (2005) 1.15
Cdc7 is an active kinase in human cancer cells undergoing replication stress. J Biol Chem (2006) 1.14
NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther (2012) 1.10
High-throughput NMR-based screening with competition binding experiments. J Am Chem Soc (2002) 1.10
Magnetic resonance imaging and histopathological characterization of prostate tumors in TRAMP mice as model for pre-clinical trials. Prostate (2007) 1.08
Searching for biomarkers of Aurora-A kinase activity: identification of in vitro substrates through a modified KESTREL approach. J Proteome Res (2005) 1.06
Assessment of docking poses: interactions-based accuracy classification (IBAC) versus crystal structure deviations. J Chem Inf Comput Sci (2004) 1.05
Synthesis of the C-1-C-28 ABCD unit of spongistatin 1. Org Lett (2003) 1.04
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors. J Med Chem (2012) 1.03
Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem (2009) 1.03
Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J Med Chem (2013) 1.02
Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships. J Med Chem (2008) 1.01
In vivo imaging of early stage apoptosis by measuring real-time caspase-3/7 activation. Apoptosis (2011) 0.99
A new approach to phosphoserine and phosphothreonine analysis in peptides and proteins: chemical modification, enrichment via solid-phase reversible binding, and analysis by mass spectrometry. Anal Bioanal Chem (2003) 0.97
Crystallographic analysis of bacterial signal peptidase in ternary complex with arylomycin A2 and a beta-sultam inhibitor. Biochemistry (2009) 0.96
Camptothecin poly[n-(2-hydroxypropyl) methacrylamide] copolymers in antitopoisomerase-I tumor therapy: intratumor release and antitumor efficacy. Mol Cancer Ther (2003) 0.95
Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition. Cancer Lett (2010) 0.93
NMR-Based screening with competition water-ligand observed via gradient spectroscopy experiments: detection of high-affinity ligands. J Med Chem (2002) 0.92
Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging. Mol Cancer Ther (2010) 0.92
Preclinical studies in the mdx mouse model of duchenne muscular dystrophy with the histone deacetylase inhibitor givinostat. Mol Med (2013) 0.92
Tautomer preference in PDB complexes and its impact on structure-based drug discovery. J Chem Inf Model (2010) 0.92
Predicting polypharmacology by binding site similarity: from kinases to the protein universe. J Chem Inf Model (2010) 0.92