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Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL Jr, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA. Carpenter J, et al. Among authors: robl ja. J Med Chem. 2017 Jul 27;60(14):6166-6190. doi: 10.1021/acs.jmedchem.7b00385. Epub 2017 Jul 7. J Med Chem. 2017. PMID: 28635286
Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.
Karanewsky DS, Badia MC, Ciosek CP Jr, Robl JA, Sofia MJ, Simpkins LM, DeLange B, Harrity TW, Biller SA, Gordon EM. Karanewsky DS, et al. Among authors: robl ja. J Med Chem. 1990 Nov;33(11):2952-6. doi: 10.1021/jm00173a007. J Med Chem. 1990. PMID: 2231594 No abstract available.
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.
Magnin DR, Biller SA, Wetterau J, Robl JA, Dickson JK Jr, Taunk P, Harrity TW, Lawrence RM, Sun CQ, Wang T, Logan J, Fryszman O, Connolly F, Jolibois K, Kunselman L. Magnin DR, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1337-40. doi: 10.1016/s0960-894x(03)00116-1. Bioorg Med Chem Lett. 2003. PMID: 12657277
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG. Magnin DR, et al. Among authors: robl ja. J Med Chem. 2004 May 6;47(10):2587-98. doi: 10.1021/jm049924d. J Med Chem. 2004. PMID: 15115400
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L. Sulsky R, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70. doi: 10.1016/j.bmcl.2004.07.069. Bioorg Med Chem Lett. 2004. PMID: 15380200
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Li JJ, Wang H, Qu F, Musial C, Tino JA, Robl JA, Slusarchyk D, Golla R, Seethala R, Dickinson K, Giupponi L, Grover G, Sleph P, Flynn N, Murphy BJ, Gordon D, Kung M, Stoffel R. Li JJ, et al. Among authors: robl ja. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1799-802. doi: 10.1016/j.bmcl.2005.02.040. Bioorg Med Chem Lett. 2005. PMID: 15780609
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: robl ja. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
70 results