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86 results

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Page 1
Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP. Hanan EJ, et al. Among authors: ultsch m. J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23061660
Peptide exosite inhibitors of factor VIIa as anticoagulants.
Dennis MS, Eigenbrot C, Skelton NJ, Ultsch MH, Santell L, Dwyer MA, O'Connell MP, Lazarus RA. Dennis MS, et al. Among authors: ultsch mh. Nature. 2000 Mar 30;404(6777):465-70. doi: 10.1038/35006574. Nature. 2000. PMID: 10761907
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Olivero AG, Eigenbrot C, Goldsmith R, Robarge K, Artis DR, Flygare J, Rawson T, Sutherlin DP, Kadkhodayan S, Beresini M, Elliott LO, DeGuzman GG, Banner DW, Ultsch M, Marzec U, Hanson SR, Refino C, Bunting S, Kirchhofer D. Olivero AG, et al. Among authors: ultsch m. J Biol Chem. 2005 Mar 11;280(10):9160-9. doi: 10.1074/jbc.M409068200. Epub 2005 Jan 4. J Biol Chem. 2005. PMID: 15632123 Free article.
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.
Rawson TE, Rüth M, Blackwood E, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Georges GJ, Goller B, Halladay J, Hunsaker T, Kleinheinz T, Krell HW, Li J, Liang J, Limberg A, McNutt A, Moffat J, Phillips G, Ran Y, Safina B, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhou A, Zhu BY, Rüger P, Cochran AG. Rawson TE, et al. Among authors: ultsch m. J Med Chem. 2008 Aug 14;51(15):4465-75. doi: 10.1021/jm800052b. Epub 2008 Jul 17. J Med Chem. 2008. PMID: 18630890
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.
Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ. Folkes AJ, et al. Among authors: ultsch mh. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. J Med Chem. 2008. PMID: 18754654
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E, Liang J, Moffat J, Phillips G, Pulk R, Rawson TE, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhu BY, Cochran AG. Aliagas-Martin I, et al. Among authors: ultsch m. J Med Chem. 2009 May 28;52(10):3300-7. doi: 10.1021/jm9000314. J Med Chem. 2009. PMID: 19402633
Antibodies specific for a segment of human membrane IgE deplete IgE-producing B cells in humanized mice.
Brightbill HD, Jeet S, Lin Z, Yan D, Zhou M, Tan M, Nguyen A, Yeh S, Delarosa D, Leong SR, Wong T, Chen Y, Ultsch M, Luis E, Ramani SR, Jackman J, Gonzalez L, Dennis MS, Chuntharapai A, DeForge L, Meng YG, Xu M, Eigenbrot C, Lee WP, Refino CJ, Balazs M, Wu LC. Brightbill HD, et al. Among authors: ultsch m. J Clin Invest. 2010 Jun;120(6):2218-29. doi: 10.1172/JCI40141. Epub 2010 May 10. J Clin Invest. 2010. PMID: 20458139 Free PMC article.
86 results