KinomeScan

Publications

Ambit's KINOMEscan™ technology has been featured in several peer-reviewed publications.
A list of recent articles appears below:


Ambit Publications

PDF 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.
PDF Goldstein, D.M. et al. High-throughput kinase profiling as a platform for drug discovery. Nat. Rev. Drug Discovery. 7, 391-397 (2008)
PDF Karaman, M.W. et al. A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132 (2008)
PDF Poster Supplement - A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132 (2008)
PDF 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)
PDF Fabian, M.A. et al. A small molecule-kinase interaction map for clinical kinase inhibitors. Nat. Biotechnol. 23, 329-336 (2005)

KINOMEscan™ Customer Citations

PDF 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)
PDF 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)
PDF 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)
PDF 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)
PDF 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)
PDF 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)
PDF 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)
PDF McDermott, U. et al. Genomic Alterations of Anaplastic Lymphoma Kinase May Sensitize Tumors to Anaplastic Lymphoma Kinase Inhibitors. Cancer Res 9, (2008)
PDF Rhodes, N. et al. Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Res. 7, 2366-2374 (2008)
PDF 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)
PDF 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)
PDF 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)
PDF 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)