| L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor JP Vacca, BD Dorsey, WA Schleif, RB Levin, SL McDaniel, PL Darke, ... Proc. Nat. Acad. Sci. U.S.A. 91, 4096, 1994 | 697 | 1994 |
| L-735,524: The Design of a Potent and Orally Bioavailable HIV Protease Inhibitor. BD Dorsey, RB Levin, SL McDaniel, JP Vacca, JP Guare, PL Darke, ... J. Med. Chem. 37, 3443, 1994 | 546 | 1994 |
| A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase DJ Hazuda, NJ Anthony, RP Gomez, SM Jolly, JS Wai, L Zhuang, ... Proceedings of the National Academy of Sciences 101 (31), 11233-11238, 2004 | 418 | 2004 |
| Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1) SJ Stachel, CA Coburn, TG Steele, KG Jones, EF Loutzenhiser, ... Journal of medicinal chemistry 47 (26), 6447-6450, 2004 | 381 | 2004 |
| 4-Aryl-2, 4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells JS Wai, MS Egbertson, LS Payne, TE Fisher, MW Embrey, LO Tran, ... Journal of medicinal chemistry 43 (26), 4923-4926, 2000 | 322 | 2000 |
| A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site MK Holloway, JM Wai, TA Halgren, PMD Fitzgerald, JP Vacca, BD Dorsey, ... Journal of medicinal chemistry 38 (2), 305-317, 1995 | 309 | 1995 |
| Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design. WJ Thompson, PM Fitzgerald, MK Holloway, EA Emini, PL Darke, ... Journal of medicinal chemistry 35 (10), 1685-1701, 1992 | 218 | 1992 |
| Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor S Harper, JA McCauley, MT Rudd, M Ferrara, M DiFilippo, B Crescenzi, ... ACS medicinal chemistry letters 3 (4), 332-336, 2012 | 199 | 2012 |
| Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor JA McCauley, CJ McIntyre, MT Rudd, KT Nguyen, JJ Romano, ... Journal of medicinal chemistry 53 (6), 2443-2463, 2010 | 199 | 2010 |
| X-ray crystal structure of the HIV protease complex with L-700,417, an inhibitor with pseudo C2 symmetry R Bone, JP Vacca, PS Anderson, MK Holloway Journal of the American Chemical Society 113 (24), 9382-9384, 1991 | 197 | 1991 |
| Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease NJ Liverton, MK Holloway, JA McCauley, MT Rudd, JW Butcher, ... Journal of the American Chemical Society 130 (14), 4607-4609, 2008 | 167 | 2008 |
| Thermodynamics of ligand binding and efficiency CH Reynolds, MK Holloway ACS medicinal chemistry letters 2 (6), 433-437, 2011 | 163 | 2011 |
| Identification of a small molecule nonpeptide active site β-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases CA Coburn, SJ Stachel, YM Li, DM Rush, TG Steele, E Chen-Dodson, ... Journal of medicinal chemistry 47 (25), 6117-6119, 2004 | 159 | 2004 |
| HIV protease inhibitors useful for the treatment of AIDS JP Vacca, BD Dorsey, JP Guare, MK Holloway, RW Hungate, RB Levin US Patent 5,527,799, 1996 | 159 | 1996 |
| MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease NJ Liverton, SS Carroll, J DiMuzio, C Fandozzi, DJ Graham, D Hazuda, ... Antimicrobial Agents and Chemotherapy 54 (1), 305-311, 2010 | 154 | 2010 |
| First demonstration of cerebrospinal fluid and plasma Aβ lowering with oral administration of a β-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates S Sankaranarayanan, MA Holahan, D Colussi, MC Crouthamel, ... Journal of Pharmacology and Experimental Therapeutics 328 (1), 131-140, 2009 | 129 | 2009 |
| Drug-like density: a method of quantifying the “bindability” of a protein target based on a very large set of pockets and drug-like ligands from the Protein Data Bank RP Sheridan, VN Maiorov, MK Holloway, WD Cornell, YD Gao Journal of chemical information and modeling 50 (11), 2029-2040, 2010 | 117 | 2010 |
| Macrocyclic inhibitors of β-secretase: functional activity in an animal model SJ Stachel, CA Coburn, S Sankaranarayanan, EA Price, BL Pietrak, ... Journal of medicinal chemistry 49 (21), 6147-6150, 2006 | 115 | 2006 |
| Conformationally biased P3 amide replacements of β-secretase inhibitors SJ Stachel, CA Coburn, TG Steele, MC Crouthamel, BL Pietrak, MT Lai, ... Bioorganic & medicinal chemistry letters 16 (3), 641-644, 2006 | 108 | 2006 |
| Design and Synthesis of Peptidomimetic Inhibitors of HIV-1 Protease and Renin. Evidence for Improved Transport. AB Smith, R Hirschmann, A Pasternak, R Akaishi, MC Guzman, DR Jones, ... Journal of Medicinal Chemistry 37, 215-218, 1994 | 108 | 1994 |
Arun K. GhoshIan P. Rothwell Distinguished Professor, Department of Chemistry: Department of Medicinal ChemistryVerified email at purdue.edu
