Publication List

KINOMEscan has been featured in many peer-reviewed publications

KINOMEscan Team Publications

kinomescan publication Davis, M. et al. Comprehensive analysis of kinase inhibitor selectivity
kinomescan publication Wodicka, L. et al. Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry. Chem. Biol. 17, 1241-9 (2010)
kinomescan publication Zarrinkar, P. P. et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. First Edition Paper, prepublished online August 4, 2009; DOI 10.1182/blood-2009-05-222034
kinomescan publication Goldstein, D. M. et al. High-throughput kinase profiling as a platform for drug discovery. Nat. Rev. Drug Discovery. 7, 391-397 (2008)
kinomescan publication Karaman, M. W. et al. A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132 (2008)
kinomescan publication Carter, T. A. et al. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc. Natl. Acad. Sci. USA. 102, 11011-11016 (2005)
kinomescan publication Fabian, M. A. et al. A small molecule-kinase interaction map for clinical kinase inhibitors. Nat. Biotechnol. 23, 329-336 (2005)

KINOMEscan Customer Citations

kinomescan publication Park, H. et al. Identification of Novel BRAF Kinase Inhibitors with Structure-Based Virtual Screening. Bioorg. Med. Chem. Lett. Epub August 8, 2011; Doi:10.1016/j.bmcl.2011.08.010 
kinomescan publication Miduturu, C. V. et al. High-Throughput Kinase Profiling: A More Efficient Approach toward the Discovery of New Kinase Inhibitors. Chem. Biol. 18, 868-79 (2011) 
kinomescan publication Blanck, S. et al. Organometallic Pyridylnaphthalimide Complexes as Protein Kinase Inhibitors. Organometallics. Epub on July 18, 2011; 10.1021/om200366r 
kinomescan publication Holladay, M. W. et al. 4-Quinazolinyloxy-diaryl Ureas as Novel BRAFV600E Inhibitors. Bioorg. Med. Chem. Lett. Epub ahead of print July 14, 2011; DOI:10.1016/j.bmcl.2011.07.019 
kinomescan publication Abraham, S. et al. Novel Series of Pyrrolotriazine Analogs as Highly Potent pan- Aurora Kinase Inhibitors. Bioorg. Med. Chem. Lett. Epub ahead of print July 14, 2011; DOI:10.1016/j.bmcl.2011.07.027 
kinomescan publication Biton, S. et al. NEMO and RIP1 control cell fate in response to extensive DNA damage via TNF-α feedforward signaling. Cell. 145, 92-103 (2011) 
kinomescan publication Kim, O. et al. Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. J. Med. Chem. Epub ahead of print March 9, 2011; DOI: 10.1021/jm101582z 
kinomescan publication Deng, X. et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat. Chem. Bio. Epub ahead of print March 6, 2011; DOI:10.1038/nchembio.538 
kinomescan publication Rosenthal, A.S. et al. Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). Bioorg. Med. Chem. Lett. Epub ahead of print March 4, 2011; doi:10.1016/j.bmcl.2011.02.114 
kinomescan publication Deng, X. et al. Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1. ACS Med. Chem. Lett. Epub ahead of print January 12, 2011; 10.1021/ml100304b
kinomescan publication Posy, S. et al. Trends in Kinase Selectivity: Insights for Target Class-Focused Library Screening. J. Med. Chem. Epub ahead of print December 3, 2010; DOI: 10.1021/jm101195a
kinomescan publication Ott, G. et al. Discovery of a Potent Inhibitor of Anaplastic Lymphoma Kinase with in Vivo Antitumor Activity. ACS Med. Chem. Lett. Epub ahead of print September 1, 2010; DOI: 10.1021/ml100158s
kinomescan publication Peddibhotla, S. et al. Inhibition of Protein Kinase C-Driven Nuclear Factor-ΚB Activation: Synthesis, Structure-Activity Relationship, and Pharmacological Profiling of Pathway Specific Benzimidazole Probe Molecules. J. Med. Chem. Epub ahead of print May 18, 2010; DOI: 10.1021/jm1000248
kinomescan publication Cheng, A. et al. Analysis of Kinase Inhibitor Selectivity using a Thermodynamics-Based Partition Index. J. Med. Chem. Epub ahead of print May 11, 2010; DOI: 10.1021/jm100301x
kinomescan publication Cheng, H. et al. Why do Kinase Inhibitors Cause Cardiotoxicity and What can be Done About It? Prog. Cardiovasc. Dis. 53, 114–120 (2010)
kinomescan publication Deng, X. et al. Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorg. Med. Chem. Lett. 20, 4196-4200 (2010)
kinomescan publication Dong, H. et al. Flavonoids activate pregnane X receptor-mediated CYP3A4 gene expression by inhibiting cyclin-dependent kinases in HepG2 liver carcinoma cells. BMC Biochem. (2010), DOI:10.1186/1471-2091-11-23
kinomescan publication Down, K. et al. The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38α MAP kinase. Bioorg. Med. Chem. Lett. 20, 3936-3940 (2010)
kinomescan publication Kwiatkowski, N. et al. Small-molecule kinase inhibitors provide insight into MPS1 cell cycle function. Nat. Chem. Biol. 6, 359-68 (2010)
kinomescan publication Milkiewicz, K. et al. Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Bioorg. Med. Chem. (2010), DOI:10.1016/j.bmc.2010.04.087
kinomescan publication Murphy, E. et al. Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc. Natl. Acad. Sci. USA. 107, 4299-304 (2010)
kinomescan publication Weisberg, E. et al. Discovery and Characterization of Novel Mutant FLT3 Kinase Inhibitors. Mol. Cancer Ther. 9, 2468-2477 (2010)
kinomescan publication Yang, Q. et al.  Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein. Cancer Cell. 18, 258-267 (2010)
kinomescan publication Zhou, W. et al. A Structure-Guided Approach to Creating Covalent FGFR Inhibitors. Chem. & Bio. 17, 285-295, (2010)
kinomescan publication Cee, V.J. et al. Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11. Angew. Chem. Int. Ed. Engl. Epub ahead of print October 20, 2009; DOI: 10.1002/anie.200904778 
kinomescan publication Daouti, S. et al. Characterization of a Novel Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor with a Unique Mechanism of Action for Cancer Therapy. Cancer Res. 5, 1924-1932 (2009)
kinomescan publication Shomin, C. et al. Staurosporine tethered peptide ligands that target cAMP-dependent protein kinase (PKA): Optimization and selectivity profiling. Bioorg. Med. Chem. 17, 6196-6202 (2009)
kinomescan publication Olaharski, A. et al. Identification of a Kinase Profile that Predicts Chromosome Damage Induced by Small Molecule Kinase Inhibitors. PLoS Comput. Biol. 5, 1-10 (2009)
kinomescan publication Angell, R. et al. Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity. Bioorg. Med. Chem. Lett. 18, 4428–4432 (2008)
kinomescan publication Bamborough, P. et al. Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. J. Med. Chem. 51, 7898–7914 (2008)
kinomescan publication Conway, J. G. et al. Effects of the cFMS kinase inhibitor 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine (GW2580) in normal and arthritic rats. J. Pharmacol. Exp. Ther. 326, 41–50 (2008)
kinomescan publication Hill, R. J. et al. Pamapimod, a Novel p38 Mitogen-Activated Protein Kinase Inhibitor: Preclinical Analysis of Efficacy and Selectivity. J. Pharmacol. Exp. Ther. 327, 610–619 (2008)
kinomescan publication Jiang, J. K. et al. Examining the Chirality, Conformation and Selective Kinase Inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J. Med. Chem. 51, 8012–8018 (2008)
kinomescan publication McDermott, U. et al. Genomic Alterations of Anaplastic Lymphoma Kinase May Sensitize Tumors to Anaplastic Lymphoma Kinase Inhibitors. Cancer Res. 9, 3389-3395 (2008)
kinomescan publication Rhodes, N. et al. Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Res. 7, 2366-2374 (2008)
kinomescan publication Schroder, G. et al. Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily. J. Med. Chem. 52, 1251–1254 (2008)
kinomescan publication Feng, Y. et al. Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors. J. Med. Chem. 51. 6642–6645 (2008)
kinomescan publication Angell, R. et al. N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3. Bioorg. Med. Chem. Lett. 17, 1296–1301 (2007)
kinomescan publication Christopher, J. A. et al. The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. Bioorg. Med. Chem. Lett. 17, 3972–3977 (2007)
kinomescan publication Pan, Z. et al. Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase. ChemMedChem. 2, 58-61 (2007)
kinomescan publication Goldstein, D. M. et al. Pathway to the Clinic: Inhibition of P38 MAP Kinase. A Review of Ten Chemotypes Selected for Development. Curr. Top. Med. Chem. 5, 1017-1029 (2005)