Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Text availability

Article attribute

Article type

Publication date

Search Results

32 results

Filters applied: . Clear all
Results are displayed in a computed author sort order. The Results By Year timeline is not available.
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: saiah e. 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
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Gerstenberger BS, Ambler C, Arnold EP, Banker ME, Brown MF, Clark JD, Dermenci A, Dowty ME, Fensome A, Fish S, Hayward MM, Hegen M, Hollingshead BD, Knafels JD, Lin DW, Lin TH, Owen DR, Saiah E, Sharma R, Vajdos FF, Xing L, Yang X, Yang X, Wright SW. Gerstenberger BS, et al. Among authors: saiah e. J Med Chem. 2020 Nov 25;63(22):13561-13577. doi: 10.1021/acs.jmedchem.0c00948. Epub 2020 Aug 25. J Med Chem. 2020. PMID: 32787094
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. Among authors: saiah e. J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31. J Med Chem. 2012. PMID: 22651823
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).
Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L. Fensome A, et al. Among authors: saiah e. J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16. J Med Chem. 2018. PMID: 30113844
Small molecules that target protein misfolding.
Gavrin LK, Denny RA, Saiah E. Gavrin LK, et al. Among authors: saiah e. J Med Chem. 2012 Dec 27;55(24):10823-43. doi: 10.1021/jm301182j. Epub 2012 Nov 1. J Med Chem. 2012. PMID: 23075044
Recent developments in targeting protein misfolding diseases.
Denny RA, Gavrin LK, Saiah E. Denny RA, et al. Among authors: saiah e. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1935-44. doi: 10.1016/j.bmcl.2013.01.089. Epub 2013 Feb 4. Bioorg Med Chem Lett. 2013. PMID: 23454013 Free article. Review.
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Follows B, Leung L, Thomason J, Huang A, Moretto A, Janz K, Lowe M, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. Among authors: saiah e. J Med Chem. 2014 Feb 27;57(4):1299-322. doi: 10.1021/jm401509e. Epub 2014 Feb 10. J Med Chem. 2014. PMID: 24512187
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ. Montalban AG, et al. Among authors: saiah e. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1772-7. doi: 10.1016/j.bmcl.2008.02.033. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18325768
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, Gibbs A, Kahl J, Kessler L, Kucharski J, Lum C, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Urban J, Wang Z, Larson CJ. Montalban AG, et al. Among authors: saiah e. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4819-24. doi: 10.1016/j.bmcl.2010.06.102. Bioorg Med Chem Lett. 2010. PMID: 20663667
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, Vallese S, Raveglia L, Hotchandani R, Fuller N, Bard J, Cunningham K, Fish S, Krykbaev R, Tam S, Goldman SJ, Williams C, Mansour TS, Saiah E, Sypek J, Li W. Wu Y, et al. Among authors: saiah e. Bioorg Med Chem Lett. 2012 Jan 1;22(1):138-43. doi: 10.1016/j.bmcl.2011.11.046. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22153340
32 results