Publications

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

Ambit Publications

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

KINOMEscan™ Customer Citations

	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
	Deng, X. et al. Broad spectrum alkynyl inhibitors of T315I Bcr-Abl. Bioorg. Med. Chem. Lett. 20, 4196-4200 (2010)
	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
	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)
	Kwiatkowski, N. et al. Small-molecule kinase inhibitors provide insight into MPS1 cell cycle function. Nat. Chem. Biol. 6, 359-68 (2010)
	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
	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)
	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. Epub ahead of print May, 2010; J Med Chem.; DOI: 10.1021/jm1000248
	Zhou, W. et al. A Structure-Guided Approach to Creating Covalent FGFR Inhibitors. Chem & Bio 17, 285-295, (2010)
	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)
	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)
	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)
	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)
	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)
	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)
	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)
	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)
	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)
	McDermott, U. et al. Genomic Alterations of Anaplastic Lymphoma Kinase May Sensitize Tumors to Anaplastic Lymphoma Kinase Inhibitors. Cancer Res 9, (2008)
	Rhodes, N. et al. Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Cancer Res. 7, 2366-2374 (2008)
	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)
	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)
	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)
	Pan, Z. et al. Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase. ChemMedChem. 2, 58-61 (2007)
	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)