BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

172 related articles for article (PubMed ID: 20614889)

  • 1. Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
    Ward SE; Harries M; Aldegheri L; Andreotti D; Ballantine S; Bax BD; Harris AJ; Harker AJ; Lund J; Melarange R; Mingardi A; Mookherjee C; Mosley J; Neve M; Oliosi B; Profeta R; Smith KJ; Smith PW; Spada S; Thewlis KM; Yusaf SP
    J Med Chem; 2010 Aug; 53(15):5801-12. PubMed ID: 20614889
    [TBL] [Abstract][Full Text] [Related]  

  • 2. Pharmacological characterization of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2, 3-dihydro-1H-inden-2-yl]-2-propanesulfonamide: a novel, clinical AMPA receptor positive allosteric modulator.
    Ward SE; Beswick P; Calcinaghi N; Dawson LA; Gartlon J; Graziani F; Jones DN; Lacroix L; Selina Mok MH; Oliosi B; Pardoe J; Starr K; Woolley ML; Harries MH
    Br J Pharmacol; 2017 Mar; 174(5):370-385. PubMed ID: 28009436
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
    Ward SE; Harries M; Aldegheri L; Austin NE; Ballantine S; Ballini E; Bradley DM; Bax BD; Clarke BP; Harris AJ; Harrison SA; Melarange RA; Mookherjee C; Mosley J; Dal Negro G; Oliosi B; Smith KJ; Thewlis KM; Woollard PM; Yusaf SP
    J Med Chem; 2011 Jan; 54(1):78-94. PubMed ID: 21128618
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes.
    Kalgutkar AS; Hatch HL; Kosea F; Nguyen HT; Choo EF; McClure KF; Taylor TJ; Henne KR; Kuperman AV; Dombroski MA; Letavic MA
    Biopharm Drug Dispos; 2006 Nov; 27(8):371-86. PubMed ID: 16944451
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Structure based evolution of a novel series of positive modulators of the AMPA receptor.
    Jamieson C; Maclean JK; Brown CI; Campbell RA; Gillen KJ; Gillespie J; Kazemier B; Kiczun M; Lamont Y; Lyons AJ; Moir EM; Morrow JA; Pantling J; Rankovic Z; Smith L
    Bioorg Med Chem Lett; 2011 Jan; 21(2):805-11. PubMed ID: 21190850
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
    Gomtsyan A; Bayburt EK; Schmidt RG; Surowy CS; Honore P; Marsh KC; Hannick SM; McDonald HA; Wetter JM; Sullivan JP; Jarvis MF; Faltynek CR; Lee CH
    J Med Chem; 2008 Feb; 51(3):392-5. PubMed ID: 18183945
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
    Phillips GB; Buckman BO; Davey DD; Eagen KA; Guilford WJ; Hinchman J; Ho E; Koovakkat S; Liang A; Light DR; Mohan R; Ng HP; Post JM; Shaw KJ; Smith D; Subramanyam B; Sullivan ME; Trinh L; Vergona R; Walters J; White K; Whitlow M; Wu S; Xu W; Morrissey MM
    J Med Chem; 1998 Sep; 41(19):3557-62. PubMed ID: 9733480
    [No Abstract]   [Full Text] [Related]  

  • 8. Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
    Li H; Anderes KL; Kraynov EA; Luthin DR; Do QQ; Hong Y; Tompkins E; Sun ET; Rajapakse R; Pathak VP; Christie LC; Feng J; Vazir H; Castillo R; Gregory ML; Castro M; Nared-Hood K; Paderes G; Anderson MB
    J Med Chem; 2006 Jun; 49(11):3362-7. PubMed ID: 16722655
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
    Madar DJ; Kopecka H; Pireh D; Yong H; Pei Z; Li X; Wiedeman PE; Djuric SW; Von Geldern TW; Fickes MG; Bhagavatula L; McDermott T; Wittenberger S; Richards SJ; Longenecker KL; Stewart KD; Lubben TH; Ballaron SJ; Stashko MA; Long MA; Wells H; Zinker BA; Mika AK; Beno DW; Kempf-Grote AJ; Polakowski J; Segreti J; Reinhart GA; Fryer RM; Sham HL; Trevillyan JM
    J Med Chem; 2006 Oct; 49(21):6416-20. PubMed ID: 17034148
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
    Cee VJ; Schenkel LB; Hodous BL; Deak HL; Nguyen HN; Olivieri PR; Romero K; Bak A; Be X; Bellon S; Bush TL; Cheng AC; Chung G; Coats S; Eden PM; Hanestad K; Gallant PL; Gu Y; Huang X; Kendall RL; Lin MH; Morrison MJ; Patel VF; Radinsky R; Rose PE; Ross S; Sun JR; Tang J; Zhao H; Payton M; Geuns-Meyer SD
    J Med Chem; 2010 Sep; 53(17):6368-77. PubMed ID: 20684549
    [TBL] [Abstract][Full Text] [Related]  

  • 11. 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
    Poon SF; Eastman BW; Chapman DF; Chung J; Cramer M; Holtz G; Cosford ND; Smith ND
    Bioorg Med Chem Lett; 2004 Nov; 14(22):5477-80. PubMed ID: 15482907
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
    Yan L; Huo P; Debenham JS; Madsen-Duggan CB; Lao J; Chen RZ; Xiao JC; Shen CP; Stribling DS; Shearman LP; Strack AM; Tsou N; Ball RG; Wang J; Tong X; Bateman TJ; Reddy VB; Fong TM; Hale JJ
    J Med Chem; 2010 May; 53(10):4028-37. PubMed ID: 20423086
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Diastereoisomers of 2-benzyl-2, 3-dihydro-2-(1H-inden-2-yl)-1H-inden-1-ol: potential anti-inflammatory agents.
    Sheridan H; Walsh JJ; Cogan C; Jordan M; McCabe T; Passante E; Frankish NH
    Bioorg Med Chem Lett; 2009 Oct; 19(20):5927-30. PubMed ID: 19740655
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
    Zhang L; Balan G; Barreiro G; Boscoe BP; Chenard LK; Cianfrogna J; Claffey MM; Chen L; Coffman KJ; Drozda SE; Dunetz JR; Fonseca KR; Galatsis P; Grimwood S; Lazzaro JT; Mancuso JY; Miller EL; Reese MR; Rogers BN; Sakurada I; Skaddan M; Smith DL; Stepan AF; Trapa P; Tuttle JB; Verhoest PR; Walker DP; Wright AS; Zaleska MM; Zasadny K; Shaffer CL
    J Med Chem; 2014 Feb; 57(3):861-77. PubMed ID: 24392688
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
    Quan ML; Lam PY; Han Q; Pinto DJ; He MY; Li R; Ellis CD; Clark CG; Teleha CA; Sun JH; Alexander RS; Bai S; Luettgen JM; Knabb RM; Wong PC; Wexler RR
    J Med Chem; 2005 Mar; 48(6):1729-44. PubMed ID: 15771420
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
    Hodous BL; Geuns-Meyer SD; Hughes PE; Albrecht BK; Bellon S; Bready J; Caenepeel S; Cee VJ; Chaffee SC; Coxon A; Emery M; Fretland J; Gallant P; Gu Y; Hoffman D; Johnson RE; Kendall R; Kim JL; Long AM; Morrison M; Olivieri PR; Patel VF; Polverino A; Rose P; Tempest P; Wang L; Whittington DA; Zhao H
    J Med Chem; 2007 Feb; 50(4):611-26. PubMed ID: 17253678
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.
    Curtin ML; Davidsen SK; Heyman HR; Garland RB; Sheppard GS; Florjancic AS; Xu L; Carrera GM; Steinman DH; Trautmann JA; Albert DH; Magoc TJ; Tapang P; Rhein DA; Conway RG; Luo G; Denissen JF; Marsh KC; Morgan DW; Summers JB
    J Med Chem; 1998 Jan; 41(1):74-95. PubMed ID: 9438024
    [TBL] [Abstract][Full Text] [Related]  

  • 18. A novel series of positive modulators of the AMPA receptor: structure-based lead optimization.
    Jamieson C; Campbell RA; Cumming IA; Gillen KJ; Gillespie J; Kazemier B; Kiczun M; Lamont Y; Lyons AJ; Maclean JK; Martin F; Moir EM; Morrow JA; Pantling J; Rankovic Z; Smith L
    Bioorg Med Chem Lett; 2010 Oct; 20(20):6072-5. PubMed ID: 20817521
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
    Zhao H; Serby MD; Xin Z; Szczepankiewicz BG; Liu M; Kosogof C; Liu B; Nelson LT; Johnson EF; Wang S; Pederson T; Gum RJ; Clampit JE; Haasch DL; Abad-Zapatero C; Fry EH; Rondinone C; Trevillyan JM; Sham HL; Liu G
    J Med Chem; 2006 Jul; 49(15):4455-8. PubMed ID: 16854050
    [TBL] [Abstract][Full Text] [Related]  

  • 20. (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
    Bell MG; Gernert DL; Grese TA; Belvo MD; Borromeo PS; Kelley SA; Kennedy JH; Kolis SP; Lander PA; Richey R; Sharp VS; Stephenson GA; Williams JD; Yu H; Zimmerman KM; Steinberg MI; Jadhav PK
    J Med Chem; 2007 Dec; 50(26):6443-5. PubMed ID: 18038968
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 9.