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Results: 1 to 20 of 70

1.

Structure of the BRAF-MEK Complex Reveals a Kinase Activity Independent Role for BRAF in MAPK Signaling.

Haling JR, Sudhamsu J, Yen I, Sideris S, Sandoval W, Phung W, Bravo BJ, Giannetti AM, Peck A, Masselot A, Morales T, Smith D, Brandhuber BJ, Hymowitz SG, Malek S.

Cancer Cell. 2014 Aug 20. pii: S1535-6108(14)00299-2. doi: 10.1016/j.ccr.2014.07.007. [Epub ahead of print]

PMID:
25155755
[PubMed - as supplied by publisher]
2.

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP.

ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9.

PMID:
24900776
[PubMed]
3.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29.

PMID:
24813737
[PubMed - in process]
4.

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2477-80. doi: 10.1016/j.bmcl.2014.04.012. Epub 2014 Apr 13.

PMID:
24780121
[PubMed - in process]
5.

Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.

Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1923-7. doi: 10.1016/j.bmcl.2014.03.007. Epub 2014 Mar 13.

PMID:
24675381
[PubMed - in process]
6.

Elucidating the mechanism of cytochrome P450-mediated pyrimidine ring conversion to pyrazole metabolites with the BACE1 inhibitor GNE-892 in rats.

Takahashi R, Ma S, Deese A, Yue Q, Kim-Kang H, Yi Y, Siu M, Hunt KW, Kallan NC, Hop CE, Liu X, Khojasteh SC.

Drug Metab Dispos. 2014 May;42(5):890-8. doi: 10.1124/dmd.114.057141. Epub 2014 Mar 4.

PMID:
24595682
[PubMed - in process]
7.

Characterization of a novel glucokinase activator in rat and mouse models.

Lu M, Li P, Bandyopadhyay G, Lagakos W, Dewolf WE Jr, Alford T, Chicarelli MJ, Williams L, Anderson DA, Baer BR, McVean M, Conn M, Véniant MM, Coward P.

PLoS One. 2014 Feb 12;9(2):e88431. doi: 10.1371/journal.pone.0088431. eCollection 2014.

PMID:
24533087
[PubMed - in process]
Free PMC Article
8.

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.

Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP, Gunawardana IW.

J Med Chem. 2014 Feb 13;57(3):878-902. doi: 10.1021/jm401635n. Epub 2014 Jan 22.

PMID:
24397738
[PubMed - indexed for MEDLINE]
9.

Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase.

Newhouse BJ, Wenglowsky S, Grina J, Laird ER, Voegtli WC, Ren L, Ahrendt K, Buckmelter A, Gloor SL, Klopfenstein N, Rudolph J, Wen Z, Li X, Feng B.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5896-9. doi: 10.1016/j.bmcl.2013.08.086. Epub 2013 Aug 29.

PMID:
24042006
[PubMed - indexed for MEDLINE]
10.

Identification of a new class of glucokinase activators through structure-based design.

Hinklin RJ, Boyd SA, Chicarelli MJ, Condroski KR, DeWolf WE Jr, Lee PA, Lee W, Singh A, Thomas L, Voegtli WC, Williams L, Aicher TD.

J Med Chem. 2013 Oct 10;56(19):7669-78. doi: 10.1021/jm401116k. Epub 2013 Sep 25.

PMID:
24015910
[PubMed - indexed for MEDLINE]
11.

Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.

Jiang Y, Andrews SW, Condroski KR, Buckman B, Serebryany V, Wenglowsky S, Kennedy AL, Madduru MR, Wang B, Lyon M, Doherty GA, Woodard BT, Lemieux C, Geck Do M, Zhang H, Ballard J, Vigers G, Brandhuber BJ, Stengel P, Josey JA, Beigelman L, Blatt L, Seiwert SD.

J Med Chem. 2014 Mar 13;57(5):1753-69. doi: 10.1021/jm400164c. Epub 2013 May 28.

PMID:
23672640
[PubMed - indexed for MEDLINE]
12.

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP.

J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16.

PMID:
23537249
[PubMed - indexed for MEDLINE]
13.

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD, MacIntyre T, Mohr PJ, Omer CA, Sjögren T, Thress K, Wang B, Wang H, Yu D, Zhang HJ.

ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. doi: 10.1021/ml300074j. eCollection 2012 Sep 13.

PMID:
24900538
[PubMed]
Free PMC Article
14.

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.

Wenglowsky S, Moreno D, Laird ER, Gloor SL, Ren L, Risom T, Rudolph J, Sturgis HL, Voegtli WC.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6237-41. doi: 10.1016/j.bmcl.2012.08.007. Epub 2012 Aug 10.

PMID:
22954737
[PubMed - indexed for MEDLINE]
15.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

PMID:
22934575
[PubMed - indexed for MEDLINE]
16.

The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.

Ren L, Ahrendt KA, Grina J, Laird ER, Buckmelter AJ, Hansen JD, Newhouse B, Moreno D, Wenglowsky S, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Risom T, Sturgis HL, Voegtli WC, Mathieu S.

Bioorg Med Chem Lett. 2012 May 15;22(10):3387-91. doi: 10.1016/j.bmcl.2012.04.015. Epub 2012 Apr 10.

PMID:
22534450
[PubMed - indexed for MEDLINE]
17.

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing.

Wenglowsky S, Moreno D, Rudolph J, Ran Y, Ahrendt KA, Arrigo A, Colson B, Gloor SL, Hastings G.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):912-5. doi: 10.1016/j.bmcl.2011.12.030. Epub 2011 Dec 10.

PMID:
22209462
[PubMed - indexed for MEDLINE]
18.

Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.

Ren L, Laird ER, Buckmelter AJ, Dinkel V, Gloor SL, Grina J, Newhouse B, Rasor K, Hastings G, Gradl SN, Rudolph J.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1165-8. doi: 10.1016/j.bmcl.2011.11.092. Epub 2011 Nov 30.

PMID:
22196124
[PubMed - indexed for MEDLINE]
19.

The role of PIM kinases in human and mouse CD4+ T cell activation and inflammatory bowel disease.

Jackson LJ, Pheneger JA, Pheneger TJ, Davis G, Wright AD, Robinson JE, Allen S, Munson MC, Carter LL.

Cell Immunol. 2012;272(2):200-13. doi: 10.1016/j.cellimm.2011.10.011. Epub 2011 Oct 25.

PMID:
22078270
[PubMed - indexed for MEDLINE]
20.

Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo.

Davies KD, Humphries MJ, Sullivan FX, von Carlowitz I, Le Huerou Y, Mohr PJ, Wang B, Blake JF, Lyon MA, Gunawardana I, Chicarelli M, Wallace E, Gross S.

Oncol Res. 2011;19(7):349-63.

PMID:
21936404
[PubMed - indexed for MEDLINE]

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