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Page 1
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: tasker as. J Med Chem. 2010 Apr 8;53(7):2973-85. doi: 10.1021/jm100095x. J Med Chem. 2010. PMID: 20218619
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE. Norman MH, et al. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22897589
Design, synthesis, and biological evaluation of potent c-Met inhibitors.
D'Angelo ND, Bellon SF, Booker SK, Cheng Y, Coxon A, Dominguez C, Fellows I, Hoffman D, Hungate R, Kaplan-Lefko P, Lee MR, Li C, Liu L, Rainbeau E, Reider PJ, Rex K, Siegmund A, Sun Y, Tasker AS, Xi N, Xu S, Yang Y, Zhang Y, Burgess TL, Dussault I, Kim TS. D'Angelo ND, et al. Among authors: tasker as. J Med Chem. 2008 Sep 25;51(18):5766-79. doi: 10.1021/jm8006189. J Med Chem. 2008. PMID: 18763753
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Xu S, Cao GQ, Chakrabarti PP, Rzasa RM, Sham K, Wurz RP, Zhang D, Middleton S, Henkle B, Plant MH, Saris CJ, Sherman L, Wong LM, Powers DA, Tudor Y, Yu V, Lee MR, Syed R, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: tasker as. J Med Chem. 2008 Oct 23;51(20):6280-92. doi: 10.1021/jm8005405. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817364
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Herberich B, Cao GQ, Chakrabarti PP, Falsey JR, Pettus L, Rzasa RM, Reed AB, Reichelt A, Sham K, Thaman M, Wurz RP, Xu S, Zhang D, Hsieh F, Lee MR, Syed R, Li V, Grosfeld D, Plant MH, Henkle B, Sherman L, Middleton S, Wong LM, Tasker AS. Herberich B, et al. Among authors: tasker as. J Med Chem. 2008 Oct 23;51(20):6271-9. doi: 10.1021/jm8005417. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817365
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Xu S, Henkle B, Sherman L, Plant M, Miner K, McBride H, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4724-8. doi: 10.1016/j.bmcl.2009.06.058. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19574047
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Henkle B, Sherman L, Plant M, Miner K, McBride HJ, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1680-4. doi: 10.1016/j.bmcl.2010.01.059. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138761
Identification of triazolopyridazinones as potent p38α inhibitors.
Herberich B, Jackson C, Wurz RP, Pettus LH, Sherman L, Liu Q, Henkle B, Saris CJ, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Herberich B, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1226-9. doi: 10.1016/j.bmcl.2011.11.067. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22196117
52 results