BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

164 related articles for article (PubMed ID: 30587449)

  • 1. Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.
    Geneste H; Drescher K; Jakob C; Laplanche L; Ochse M; Torrent M
    Bioorg Med Chem Lett; 2019 Feb; 29(3):406-412. PubMed ID: 30587449
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
    Cox CD; Hostetler ED; Flores BA; Evelhoch JL; Fan H; Gantert L; Holahan M; Eng W; Joshi A; McGaughey G; Meng X; Purcell M; Raheem IT; Riffel K; Yan Y; Renger JJ; Smith SM; Coleman PJ
    Bioorg Med Chem Lett; 2015 Nov; 25(21):4893-4898. PubMed ID: 26077491
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.
    Höfgen N; Stange H; Schindler R; Lankau HJ; Grunwald C; Langen B; Egerland U; Tremmel P; Pangalos MN; Marquis KL; Hage T; Harrison BL; Malamas MS; Brandon NJ; Kronbach T
    J Med Chem; 2010 Jun; 53(11):4399-411. PubMed ID: 20450197
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.
    Kawamoto Y; Tomino M; Hiramatsu K; Oyama Y; Hayashi Y
    Bioorg Med Chem Lett; 2019 Jun; 29(11):1419-1422. PubMed ID: 30952590
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
    Hu E; Chen N; Bourbeau MP; Harrington PE; Biswas K; Kunz RK; Andrews KL; Chmait S; Zhao X; Davis C; Ma J; Shi J; Lester-Zeiner D; Danao J; Able J; Cueva M; Talreja S; Kornecook T; Chen H; Porter A; Hungate R; Treanor J; Allen JR
    J Med Chem; 2014 Aug; 57(15):6632-41. PubMed ID: 25062128
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
    Hu E; Kunz RK; Chen N; Rumfelt S; Siegmund A; Andrews K; Chmait S; Zhao S; Davis C; Chen H; Lester-Zeiner D; Ma J; Biorn C; Shi J; Porter A; Treanor J; Allen JR
    J Med Chem; 2013 Nov; 56(21):8781-92. PubMed ID: 24102193
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.
    Chino A; Masuda N; Amano Y; Honbou K; Mihara T; Yamazaki M; Tomishima M
    Bioorg Med Chem; 2014 Jul; 22(13):3515-26. PubMed ID: 24837154
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
    Raheem IT; Schreier JD; Fuerst J; Gantert L; Hostetler ED; Huszar S; Joshi A; Kandebo M; Kim SH; Li J; Ma B; McGaughey G; Sharma S; Shipe WD; Uslaner J; Vandeveer GH; Yan Y; Renger JJ; Smith SM; Coleman PJ; Cox CD
    Bioorg Med Chem Lett; 2016 Jan; 26(1):126-32. PubMed ID: 26602277
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
    Rzasa RM; Frohn MJ; Andrews KL; Chmait S; Chen N; Clarine JG; Davis C; Eastwood HA; Horne DB; Hu E; Jones AD; Kaller MR; Kunz RK; Miller S; Monenschein H; Nguyen T; Pickrell AJ; Porter A; Reichelt A; Zhao X; Treanor JJS; Allen JR
    Bioorg Med Chem; 2014 Dec; 22(23):6570-6585. PubMed ID: 25456383
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3).
    Hu E; Kunz RK; Rumfelt S; Andrews KL; Li C; Hitchcock SA; Lindstrom M; Treanor J
    Bioorg Med Chem Lett; 2012 Nov; 22(22):6938-42. PubMed ID: 23044369
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
    Hostetler ED; Fan H; Joshi AD; Zeng Z; Eng W; Gantert L; Holahan M; Meng X; Miller P; O'Malley S; Purcell M; Riffel K; Salinas C; Williams M; Ma B; Buist N; Smith SM; Coleman PJ; Cox CD; Flores BA; Raheem IT; Cook JJ; Evelhoch JL
    Mol Imaging Biol; 2016 Aug; 18(4):579-87. PubMed ID: 26596571
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition.
    Hamaguchi W; Masuda N; Isomura M; Miyamoto S; Kikuchi S; Amano Y; Honbou K; Mihara T; Watanabe T
    Bioorg Med Chem; 2013 Dec; 21(24):7612-23. PubMed ID: 24238902
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
    Kehler J; Ritzen A; Langgård M; Petersen SL; Farah MM; Bundgaard C; Christoffersen CT; Nielsen J; Kilburn JP
    Bioorg Med Chem Lett; 2011 Jun; 21(12):3738-42. PubMed ID: 21602043
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.
    Rzasa RM; Hu E; Rumfelt S; Chen N; Andrews KL; Chmait S; Falsey JR; Zhong W; Jones AD; Porter A; Louie SW; Zhao X; Treanor JJ; Allen JR
    Bioorg Med Chem Lett; 2012 Dec; 22(24):7371-5. PubMed ID: 23149228
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.
    Dore A; Asproni B; Scampuddu A; Pinna GA; Christoffersen CT; Langgård M; Kehler J
    Eur J Med Chem; 2014 Sep; 84():181-93. PubMed ID: 25016376
    [TBL] [Abstract][Full Text] [Related]  

  • 16. AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.
    Chen H; Lester-Zeiner D; Shi J; Miller S; Glaus C; Hu E; Chen N; Able J; Biorn C; Wong J; Ma J; Michelsen K; Hill Della Puppa G; Kazules T; Dou HH; Talreja S; Zhao X; Chen A; Rumfelt S; Kunz RK; Ye H; Thiel OR; Williamson T; Davis C; Porter A; Immke D; Allen JR; Treanor J
    J Pharmacol Exp Ther; 2015 Feb; 352(2):327-37. PubMed ID: 25502803
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
    Malamas MS; Ni Y; Erdei J; Stange H; Schindler R; Lankau HJ; Grunwald C; Fan KY; Parris K; Langen B; Egerland U; Hage T; Marquis KL; Grauer S; Brennan J; Navarra R; Graf R; Harrison BL; Robichaud A; Kronbach T; Pangalos MN; Hoefgen N; Brandon NJ
    J Med Chem; 2011 Nov; 54(21):7621-38. PubMed ID: 21988093
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
    Varnes JG; Geschwindner S; Holmquist CR; Forst J; Wang X; Dekker N; Scott CW; Tian G; Wood MW; Albert JS
    Bioorg Med Chem Lett; 2016 Jan; 26(1):197-202. PubMed ID: 26597534
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
    Yang H; Murigi FN; Wang Z; Li J; Jin H; Tu Z
    Bioorg Med Chem Lett; 2015 Feb; 25(4):919-24. PubMed ID: 25592707
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
    Malamas MS; Stange H; Schindler R; Lankau HJ; Grunwald C; Langen B; Egerland U; Hage T; Ni Y; Erdei J; Fan KY; Parris K; Marquis KL; Grauer S; Brennan J; Navarra R; Graf R; Harrison BL; Robichaud A; Kronbach T; Pangalos MN; Brandon NJ; Hoefgen N
    Bioorg Med Chem Lett; 2012 Sep; 22(18):5876-84. PubMed ID: 22902656
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 9.