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Page 1
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: messing d. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, Mohan S, O'Connell TN, Ohren JF, Parikh MD, Schmidt M, Selness SR, Springer JR, Thanabal V, Trujillo JI, Walker DP, Wan ZK, Withka JM, Wittwer AJ, Wood NL, Xing L, Zapf CW, Douhan J 3rd. Schnute ME, et al. Among authors: messing d. ACS Med Chem Lett. 2018 Dec 3;10(1):80-85. doi: 10.1021/acsmedchemlett.8b00461. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655951 Free PMC article.
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis.
Ruminski PG, Massa M, Strohbach J, Hanau CE, Schmidt M, Scholten JA, Fletcher TR, Hamper BC, Carroll JN, Shieh HS, Caspers N, Collins B, Grapperhaus M, Palmquist KE, Collins J, Baldus JE, Hitchcock J, Kleine HP, Rogers MD, McDonald J, Munie GE, Messing DM, Portolan S, Whiteley LO, Sunyer T, Schnute ME. Ruminski PG, et al. Among authors: messing dm. J Med Chem. 2016 Jan 14;59(1):313-27. doi: 10.1021/acs.jmedchem.5b01434. Epub 2015 Dec 24. J Med Chem. 2016. PMID: 26653735
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.
Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Among authors: messing d. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21640588
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Messing D, Yang J, Mao MK, Yalamanchili G, Vonder Embse R, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Among authors: messing d. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4066-71. doi: 10.1016/j.bmcl.2011.04.121. Epub 2011 May 11. Bioorg Med Chem Lett. 2011. PMID: 21641211
Cartilage degradation biomarkers predict efficacy of a novel, highly selective matrix metalloproteinase 13 inhibitor in a dog model of osteoarthritis: confirmation by multivariate analysis that modulation of type II collagen and aggrecan degradation peptides parallels pathologic changes.
Settle S, Vickery L, Nemirovskiy O, Vidmar T, Bendele A, Messing D, Ruminski P, Schnute M, Sunyer T. Settle S, et al. Among authors: messing d. Arthritis Rheum. 2010 Oct;62(10):3006-15. doi: 10.1002/art.27596. Arthritis Rheum. 2010. PMID: 20533541 Free article.
Selective inhibition of BTK prevents murine lupus and antibody-mediated glomerulonephritis.
Rankin AL, Seth N, Keegan S, Andreyeva T, Cook TA, Edmonds J, Mathialagan N, Benson MJ, Syed J, Zhan Y, Benoit SE, Miyashiro JS, Wood N, Mohan S, Peeva E, Ramaiah SK, Messing D, Homer BL, Dunussi-Joannopoulos K, Nickerson-Nutter CL, Schnute ME, Douhan J 3rd. Rankin AL, et al. Among authors: messing d. J Immunol. 2013 Nov 1;191(9):4540-50. doi: 10.4049/jimmunol.1301553. Epub 2013 Sep 25. J Immunol. 2013. PMID: 24068666
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.
Walker JK, Selness SR, Devraj RV, Hepperle ME, Naing W, Shieh H, Kurambail R, Yang S, Flynn DL, Benson AG, Messing DM, Dice T, Kim T, Lindmark RJ, Monahan JB, Portanova J. Walker JK, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8. doi: 10.1016/j.bmcl.2010.02.047. Epub 2010 Feb 14. Bioorg Med Chem Lett. 2010. PMID: 20227876
Modeling the clinical phenotype of BTK inhibition in the mature murine immune system.
Benson MJ, Rodriguez V, von Schack D, Keegan S, Cook TA, Edmonds J, Benoit S, Seth N, Du S, Messing D, Nickerson-Nutter CL, Dunussi-Joannopoulos K, Rankin AL, Ruzek M, Schnute ME, Douhan J 3rd. Benson MJ, et al. Among authors: messing d. J Immunol. 2014 Jul 1;193(1):185-97. doi: 10.4049/jimmunol.1302570. Epub 2014 Jun 4. J Immunol. 2014. PMID: 24899507
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