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Publication List
KINOME
scan
has been featured in many peer-reviewed publications
KINOME
scan
Team Publications
Davis, M.
et al
. Comprehensive analysis of kinase inhibitor selectivity
Wodicka, L.
et al
. Activation State-Dependent Binding of Small Molecule Kinase Inhibitors: Structural Insights from Biochemistry.
Chem. Biol.
17, 1241-9 (2010)
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)
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)
KINOME
scan
Customer Citations
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
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)
Blanck, S.
et al
. Organometallic Pyridylnaphthalimide Complexes as Protein Kinase Inhibitors.
Organometallics
. Epub on July 18, 2011; 10.1021/om200366r
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
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
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)
Kim, O.
et a
l
. 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
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
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
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
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
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
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
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
Cheng, H.
et al
. Why do Kinase Inhibitors Cause Cardiotoxicity and What can be Done About It?
Prog. Cardiovasc. Dis
. 53, 114–120 (2010)
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)
Weisberg, E.
et al
. Discovery and Characterization of Novel Mutant FLT3 Kinase Inhibitors.
Mol. Cancer Ther
. 9, 2468-2477 (2010)
Yang, Q.
et al.
Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein.
Cancer Cell
. 18, 258-267 (2010)
Zhou, W.
et al
. A Structure-Guided Approach to Creating Covalent FGFR Inhibitors.
Chem. & Bio.
17, 285-295, (2010)
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
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)
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, 3389-3395 (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)
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)
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)
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