Published in J Med Chem on March 25, 2004
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Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases. ACS Med Chem Lett (2010) 1.04
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Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br J Pharmacol (2014) 0.90
Molecular-docking-guided 3D-QSAR studies of substituted isoquinoline-1,3-(2H,4H)-diones as cyclin-dependent kinase 4 (CDK4) inhibitors. J Mol Model (2009) 0.89
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Testing of SNS-032 in a Panel of Human Neuroblastoma Cell Lines with Acquired Resistance to a Broad Range of Drugs. Transl Oncol (2013) 0.87
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New potential antitumor pyrazole derivatives: synthesis and cytotoxic evaluation. Int J Mol Sci (2013) 0.79
Molecular markers of prognosis and novel therapeutic strategies for urothelial cell carcinomas. World J Urol (2006) 0.78
The effect of a tightly bound water molecule on scaffold diversity in the computer-aided de novo ligand design of CDK2 inhibitors. J Mol Model (2005) 0.78
Insight into the interactions between novel isoquinolin-1,3-dione derivatives and cyclin-dependent kinase 4 combining QSAR and molecular docking. PLoS One (2014) 0.77
A Versatile Cell Death Screening Assay Using Dye-Stained Cells and Multivariate Image Analysis. Assay Drug Dev Technol (2015) 0.76
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4-(4-Chloro-phen-yl)-N-[(E)-4-(dimethyl-amino)-benzyl-idene]-1,3-thia-zol-2-amine. Acta Crystallogr Sect E Struct Rep Online (2011) 0.75
Structure of the Cul1-Rbx1-Skp1-F boxSkp2 SCF ubiquitin ligase complex. Nature (2002) 10.96
BRCA2 function in DNA binding and recombination from a BRCA2-DSS1-ssDNA structure. Science (2002) 6.32
Mechanism of homologous recombination from the RecA-ssDNA/dsDNA structures. Nature (2008) 5.85
Ubiquitination regulates PTEN nuclear import and tumor suppression. Cell (2007) 5.62
Structure of a beta-TrCP1-Skp1-beta-catenin complex: destruction motif binding and lysine specificity of the SCF(beta-TrCP1) ubiquitin ligase. Mol Cell (2003) 5.31
The BRCA2 homologue Brh2 nucleates RAD51 filament formation at a dsDNA-ssDNA junction. Nature (2005) 4.08
Structure of a Fbw7-Skp1-cyclin E complex: multisite-phosphorylated substrate recognition by SCF ubiquitin ligases. Mol Cell (2007) 3.97
Structure of an HIF-1alpha -pVHL complex: hydroxyproline recognition in signaling. Science (2002) 3.86
The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res (2006) 3.28
Recognition of DNA damage by the Rad4 nucleotide excision repair protein. Nature (2007) 2.97
mTOR kinase structure, mechanism and regulation. Nature (2013) 2.80
Structural basis of the Cks1-dependent recognition of p27(Kip1) by the SCF(Skp2) ubiquitin ligase. Mol Cell (2005) 2.75
Structural basis of UV DNA-damage recognition by the DDB1-DDB2 complex. Cell (2008) 2.47
Structure of the 53BP1 BRCT region bound to p53 and its comparison to the Brca1 BRCT structure. Genes Dev (2002) 2.26
Structure of the SWI2/SNF2 chromatin-remodeling domain of eukaryotic Rad54. Nat Struct Mol Biol (2005) 2.25
Structure of the Rb C-terminal domain bound to E2F1-DP1: a mechanism for phosphorylation-induced E2F release. Cell (2005) 1.90
Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia. Blood (2008) 1.87
In vivo evaluation of ixabepilone (BMS247550), a novel epothilone B derivative, against pediatric cancer models. Clin Cancer Res (2005) 1.83
Crystal structure of the FHA domain of the Chfr mitotic checkpoint protein and its complex with tungstate. Structure (2002) 1.77
Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos (2008) 1.74
The BRCA2-interacting protein DSS1 is vital for DNA repair, recombination, and genome stability in Ustilago maydis. Mol Cell (2003) 1.68
Werner syndrome protein contains three structure-specific DNA binding domains. J Biol Chem (2003) 1.62
Structure of the FANCI-FANCD2 complex: insights into the Fanconi anemia DNA repair pathway. Science (2011) 1.58
Tel2 structure and function in the Hsp90-dependent maturation of mTOR and ATR complexes. Genes Dev (2010) 1.55
Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography. Structure (2002) 1.42
Structure and conformational change of a replication protein A heterotrimer bound to ssDNA. Genes Dev (2012) 1.38
Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders. J Med Chem (2008) 1.35
Preclinical discovery of ixabepilone, a highly active antineoplastic agent. Cancer Chemother Pharmacol (2008) 1.19
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem (2002) 1.18
Structure and activation mechanism of the CHK2 DNA damage checkpoint kinase. Mol Cell (2009) 1.18
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: comparative assessement of prediction methods of human clearance. J Pharm Sci (2011) 1.14
Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. Endocrinology (2006) 1.13
High-level expression and purification of recombinant SCF ubiquitin ligases. Methods Enzymol (2005) 1.11
Features of a Smad3 MH1-DNA complex. Roles of water and zinc in DNA binding. J Biol Chem (2003) 1.11
The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases. Mol Cancer Ther (2010) 1.09
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors. J Med Chem (2007) 1.08
Crystal structure of a human Mob1 protein: toward understanding Mob-regulated cell cycle pathways. Structure (2003) 1.07
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem (2008) 1.07
Structural differences in the DNA binding domains of human p53 and its C. elegans ortholog Cep-1. Structure (2004) 1.06
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem (2006) 1.05
PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 2: comparative assessment of prediction methods of human volume of distribution. J Pharm Sci (2011) 1.04
Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists. J Med Chem (2007) 1.03
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors. Bioorg Med Chem Lett (2006) 1.03
PHRMA CPCDC initiative on predictive models of human pharmacokinetics, part 5: prediction of plasma concentration-time profiles in human by using the physiologically-based pharmacokinetic modeling approach. J Pharm Sci (2011) 1.03
Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer. Cancer Res (2009) 0.99
Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res (2006) 0.99
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. Bioorg Med Chem Lett (2005) 0.98
Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors. Bioorg Med Chem Lett (2006) 0.97
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma. J Med Chem (2009) 0.97
Steady-state pharmacokinetics of a novel extended-release metformin formulation. Clin Pharmacokinet (2005) 0.96
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett (2007) 0.95
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders. J Med Chem (2009) 0.95
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. Bioorg Med Chem Lett (2008) 0.94
Antibacterial activity of substituted dibenzo[a,g]quinolizin-7-ium derivatives. Bioorg Med Chem Lett (2012) 0.93
Effect of organic isothiocyanates on the P-glycoprotein- and MRP1-mediated transport of daunomycin and vinblastine. Pharm Res (2002) 0.90
Synergy between chemotherapeutic agents and CTLA-4 blockade in preclinical tumor models. Cancer Immunol Immunother (2013) 0.90
Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template. J Med Chem (2004) 0.90