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SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Among authors: stout t. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
The design, synthesis, and biological evaluation of PIM kinase inhibitors.
Tsuhako AL, Brown DS, Koltun ES, Aay N, Arcalas A, Chan V, Du H, Engst S, Franzini M, Galan A, Huang P, Johnston S, Kane B, Kim MH, Laird AD, Lin R, Mock L, Ngan I, Pack M, Stott G, Stout TJ, Yu P, Zaharia C, Zhang W, Zhou P, Nuss JM, Kearney PC, Xu W. Tsuhako AL, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3732-8. doi: 10.1016/j.bmcl.2012.04.025. Epub 2012 Apr 11. Bioorg Med Chem Lett. 2012. PMID: 22542012
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.
Leahy JW, Buhr CA, Johnson HW, Kim BG, Baik T, Cannoy J, Forsyth TP, Jeong JW, Lee MS, Ma S, Noson K, Wang L, Williams M, Nuss JM, Brooks E, Foster P, Goon L, Heald N, Holst C, Jaeger C, Lam S, Lougheed J, Nguyen L, Plonowski A, Song J, Stout T, Wu X, Yakes MF, Yu P, Zhang W, Lamb P, Raeber O. Leahy JW, et al. Among authors: stout t. J Med Chem. 2012 Jun 14;55(11):5467-82. doi: 10.1021/jm300403a. Epub 2012 May 17. J Med Chem. 2012. PMID: 22548342
Discovery of XL413, a potent and selective CDC7 inhibitor.
Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M, Galan A, Holst CR, Huang P, Kane B, Kim MH, Li J, Markby D, Mohan M, Noson K, Plonowski A, Richards SJ, Robertson S, Shaw K, Stott G, Stout TJ, Young J, Yu P, Zaharia CA, Zhang W, Zhou P, Nuss JM, Xu W, Kearney PC. Koltun ES, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. doi: 10.1016/j.bmcl.2012.04.024. Epub 2012 Apr 16. Bioorg Med Chem Lett. 2012. PMID: 22560567
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR, Le DT, Mac M, Parks JJ, Qian F, Rodriquez M, Stout TJ, Till JH, Won KA, Wu X, Yakes FM, Yu P, Zhang W, Zhao Y, Lamb P, Nuss JM, Xu W. Kim MH, et al. Among authors: stout tj. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. doi: 10.1016/j.bmcl.2012.06.029. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22765894
Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
Kick E, Martin R, Xie Y, Flatt B, Schweiger E, Wang TL, Busch B, Nyman M, Gu XH, Yan G, Wagner B, Nanao M, Nguyen L, Stout T, Plonowski A, Schulman I, Ostrowski J, Kirchgessner T, Wexler R, Mohan R. Kick E, et al. Among authors: stout t. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. doi: 10.1016/j.bmcl.2014.11.029. Epub 2014 Nov 15. Bioorg Med Chem Lett. 2015. PMID: 25435151
Growth-rate model predicts in vivo tumor response from in vitro data.
Diegmiller R, Salphati L, Alicke B, Wilson TR, Stout TJ, Hafner M. Diegmiller R, et al. CPT Pharmacometrics Syst Pharmacol. 2022 Sep;11(9):1183-1193. doi: 10.1002/psp4.12836. Epub 2022 Jul 4. CPT Pharmacometrics Syst Pharmacol. 2022. PMID: 35731938 Free PMC article.
259 results