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Page 1
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: strohbach jw. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
Lovering F, Morgan P, Allais C, Aulabaugh A, Brodfuehrer J, Chang J, Coe J, Ding W, Dowty H, Fleming M, Frisbie R, Guzova J, Hepworth D, Jasti J, Kortum S, Kurumbail R, Mohan S, Papaioannou N, Strohbach JW, Vincent F, Lee K, Zapf CW. Lovering F, et al. Among authors: strohbach jw. Eur J Med Chem. 2018 Feb 10;145:606-621. doi: 10.1016/j.ejmech.2017.12.041. Epub 2017 Dec 15. Eur J Med Chem. 2018. PMID: 29348070
Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
Casimiro-Garcia A, Allais C, Brennan A, Choi C, Dower G, Farley KA, Fleming M, Flick A, Frisbie RK, Hall J, Hepworth D, Jones H, Knafels JD, Kortum S, Lovering FE, Mathias JP, Mohan S, Morgan PM, Parng C, Parris K, Pullen N, Schlerman F, Stansfield J, Strohbach JW, Vajdos FF, Vincent F, Wang H, Wang X, Webster R, Wright SW. Casimiro-Garcia A, et al. Among authors: strohbach jw. J Med Chem. 2022 Jan 13;65(1):757-784. doi: 10.1021/acs.jmedchem.1c01849. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967602
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R. Vazquez ML, et al. Among authors: strohbach jw. J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29298069
Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells.
Li J, Wang B, Juba BM, Vazquez M, Kortum SW, Pierce BS, Pacheco M, Roberts L, Strohbach JW, Jones LH, Hett E, Thorarensen A, Telliez JB, Sharei A, Bunnage M, Gilbert JB. Li J, et al. Among authors: strohbach jw. ACS Chem Biol. 2017 Dec 15;12(12):2970-2974. doi: 10.1021/acschembio.7b00683. Epub 2017 Nov 13. ACS Chem Biol. 2017. PMID: 29088528
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. 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
Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity.
Thaisrivongs S, Tomasselli AG, Moon JB, Hui J, McQuade TJ, Turner SR, Strohbach JW, Howe WJ, Tarpley WG, Heinrikson RL. Thaisrivongs S, et al. Among authors: strohbach jw. J Med Chem. 1991 Aug;34(8):2344-56. doi: 10.1021/jm00112a005. J Med Chem. 1991. PMID: 1875334
Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.
Thaisrivongs S, Romero DL, Tommasi RA, Janakiraman MN, Strohbach JW, Turner SR, Biles C, Morge RR, Johnson PD, Aristoff PA, Tomich PK, Lynn JC, Horng MM, Chong KT, Hinshaw RR, Howe WJ, Finzel BC, Watenpaugh KD. Thaisrivongs S, et al. Among authors: strohbach jw. J Med Chem. 1996 Nov 8;39(23):4630-42. doi: 10.1021/jm960228q. J Med Chem. 1996. PMID: 8917652
Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.
Turner SR, Strohbach JW, Tommasi RA, Aristoff PA, Johnson PD, Skulnick HI, Dolak LA, Seest EP, Tomich PK, Bohanon MJ, Horng MM, Lynn JC, Chong KT, Hinshaw RR, Watenpaugh KD, Janakiraman MN, Thaisrivongs S. Turner SR, et al. Among authors: strohbach jw. J Med Chem. 1998 Aug 27;41(18):3467-76. doi: 10.1021/jm9802158. J Med Chem. 1998. PMID: 9719600
Inhibitors of the protease from human immunodeficiency virus: synthesis, enzyme inhibition, and antiviral activity of a series of compounds containing the dihydroxyethylene transition-state isostere.
Thaisrivongs S, Turner SR, Strohbach JW, TenBrink RE, Tarpley WG, McQuade TJ, Heinrikson RL, Tomasselli AG, Hui JO, Howe WJ. Thaisrivongs S, et al. Among authors: strohbach jw. J Med Chem. 1993 Apr 16;36(8):941-52. doi: 10.1021/jm00060a001. J Med Chem. 1993. PMID: 8478908
21 results