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Page 1
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X. Aronov AM, et al. Among authors: namchuk mn. J Med Chem. 2007 Mar 22;50(6):1280-7. doi: 10.1021/jm061381f. Epub 2007 Feb 15. J Med Chem. 2007. PMID: 17300186
(S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18.
Wannamaker W, Davies R, Namchuk M, Pollard J, Ford P, Ku G, Decker C, Charifson P, Weber P, Germann UA, Kuida K, Randle JC. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16. doi: 10.1124/jpet.106.111344. Epub 2007 Feb 8. J Pharmacol Exp Ther. 2007. PMID: 17289835
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Markland W, Namchuk MN, Nanthakumar S, Poondru S, Straub J, ter Haar E, Xie X. Aronov AM, et al. Among authors: namchuk mn. J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q. J Med Chem. 2009. PMID: 19827834
In vitro and in vivo isotope effects with hepatitis C protease inhibitors: enhanced plasma exposure of deuterated telaprevir versus telaprevir in rats.
Maltais F, Jung YC, Chen M, Tanoury J, Perni RB, Mani N, Laitinen L, Huang H, Liao S, Gao H, Tsao H, Block E, Ma C, Shawgo RS, Town C, Brummel CL, Howe D, Pazhanisamy S, Raybuck S, Namchuk M, Bennani YL. Maltais F, et al. J Med Chem. 2009 Dec 24;52(24):7993-8001. doi: 10.1021/jm901023f. J Med Chem. 2009. PMID: 19894743
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Wang T, Duffy JP, Wang J, Halas S, Salituro FG, Pierce AC, Zuccola HJ, Black JR, Hogan JK, Jepson S, Shlyakter D, Mahajan S, Gu Y, Hoock T, Wood M, Furey BF, Frantz JD, Dauffenbach LM, Germann UA, Fan B, Namchuk M, Bennani YL, Ledeboer MW. Wang T, et al. J Med Chem. 2009 Dec 24;52(24):7938-41. doi: 10.1021/jm901383u. J Med Chem. 2009. PMID: 20014869
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Davies RJ, Pierce AC, Forster C, Grey R, Xu J, Arnost M, Choquette D, Galullo V, Tian SK, Henkel G, Chen G, Heidary DK, Ma J, Stuver-Moody C, Namchuk M. Davies RJ, et al. J Med Chem. 2011 Oct 27;54(20):7184-92. doi: 10.1021/jm200712h. Epub 2011 Oct 4. J Med Chem. 2011. PMID: 21970471
Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors.
Giroux S, Xu J, Reddy TJ, Morris M, Cottrell KM, Cadilhac C, Henderson JA, Nicolas O, Bilimoria D, Denis F, Mani N, Ewing N, Shawgo R, L'Heureux L, Selliah S, Chan L, Chauret N, Berlioz-Seux F, Namchuk MN, Grillot AL, Bennani YL, Das SK, Maxwell JP. Giroux S, et al. Among authors: namchuk mn. ACS Med Chem Lett. 2013 Jan 27;5(3):240-3. doi: 10.1021/ml300461f. eCollection 2014 Mar 13. ACS Med Chem Lett. 2013. PMID: 24900811 Free PMC article.
Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.
Farmer LJ, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran JE, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Penney MS, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ. Farmer LJ, et al. J Med Chem. 2015 Sep 24;58(18):7195-216. doi: 10.1021/acs.jmedchem.5b00301. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26230873
Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib).
Germann UA, Furey BF, Markland W, Hoover RR, Aronov AM, Roix JJ, Hale M, Boucher DM, Sorrell DA, Martinez-Botella G, Fitzgibbon M, Shapiro P, Wick MJ, Samadani R, Meshaw K, Groover A, DeCrescenzo G, Namchuk M, Emery CM, Saha S, Welsch DJ. Germann UA, et al. Mol Cancer Ther. 2017 Nov;16(11):2351-2363. doi: 10.1158/1535-7163.MCT-17-0456. Epub 2017 Sep 22. Mol Cancer Ther. 2017. PMID: 28939558
c-Jun N-terminal kinases mediate reactivation of Akt and cardiomyocyte survival after hypoxic injury in vitro and in vivo.
Shao Z, Bhattacharya K, Hsich E, Park L, Walters B, Germann U, Wang YM, Kyriakis J, Mohanlal R, Kuida K, Namchuk M, Salituro F, Yao YM, Hou WM, Chen X, Aronovitz M, Tsichlis PN, Bhattacharya S, Force T, Kilter H. Shao Z, et al. Circ Res. 2006 Jan 6;98(1):111-8. doi: 10.1161/01.RES.0000197781.20524.b9. Epub 2005 Nov 23. Circ Res. 2006. PMID: 16306447
28 results