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Page 1
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Liu C, Lin J, Langevine C, Smith D, Li J, Tokarski JS, Khan J, Ruzanov M, Strnad J, Zupa-Fernandez A, Cheng L, Gillooly KM, Shuster D, Zhang Y, Thankappan A, McIntyre KW, Chaudhry C, Elzinga PA, Chiney M, Chimalakonda A, Lombardo LJ, Macor JE, Carter PH, Burke JR, Weinstein DS. Liu C, et al. Among authors: shuster d. J Med Chem. 2021 Jan 14;64(1):677-694. doi: 10.1021/acs.jmedchem.0c01698. Epub 2020 Dec 28. J Med Chem. 2021. PMID: 33370104
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS. Wrobleski ST, et al. Among authors: shuster d, d arienzo c. J Med Chem. 2019 Oct 24;62(20):8973-8995. doi: 10.1021/acs.jmedchem.9b00444. Epub 2019 Jul 18. J Med Chem. 2019. PMID: 31318208
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.
Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Cherney RJ, et al. Among authors: shuster d. ACS Med Chem Lett. 2020 Mar 31;11(6):1221-1227. doi: 10.1021/acsmedchemlett.0c00063. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551004 Free PMC article.
5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Liu C, Wrobleski ST, Lin J, Ahmed G, Metzger A, Wityak J, Gillooly KM, Shuster DJ, McIntyre KW, Pitt S, Shen DR, Zhang RF, Zhang H, Doweyko AM, Diller D, Henderson I, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Liu C, et al. Among authors: shuster dj. J Med Chem. 2005 Oct 6;48(20):6261-70. doi: 10.1021/jm0503594. J Med Chem. 2005. PMID: 16190753
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC. Das J, et al. Among authors: shuster dj. J Med Chem. 2006 Nov 16;49(23):6819-32. doi: 10.1021/jm060727j. J Med Chem. 2006. PMID: 17154512
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K. Hynes J Jr, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. doi: 10.1016/j.bmcl.2008.02.031. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313298
Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, Shuster DJ, Zhang H, Marathe PH, Doweyko AM, Sack JS, Kiefer SE, Kish KF, Newitt JA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K. Liu C, et al. J Med Chem. 2010 Sep 23;53(18):6629-39. doi: 10.1021/jm100540x. J Med Chem. 2010. PMID: 20804198
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.
Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Dyckman AJ, et al. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. doi: 10.1016/j.bmcl.2011.05.091. Epub 2011 May 30. Bioorg Med Chem Lett. 2011. PMID: 21705217
Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.
Liu C, Lin J, Hynes J, Wu H, Wrobleski ST, Lin S, Dhar TG, Vrudhula VM, Sun JH, Chao S, Zhao R, Wang B, Chen BC, Everlof G, Gesenberg C, Zhang H, Marathe PH, McIntyre KW, Taylor TL, Gillooly K, Shuster DJ, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K. Liu C, et al. J Med Chem. 2015 Oct 8;58(19):7775-84. doi: 10.1021/acs.jmedchem.5b00839. Epub 2015 Sep 22. J Med Chem. 2015. PMID: 26359680
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Watterson SH, et al. Among authors: d arienzo c, shuster dj. J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10. J Med Chem. 2016. PMID: 26924461
162 results