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Page 1
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: cramer jw. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis.
Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, Reinhard MR, Cohen MP, Hellman SL, Getman BG, Wang X, Menezes MM, Maren DL, Falcone JF, Anderson WH, Wright RA, Morin SM, Knopp KL, Adams BL, Rogovoy B, Okun I, Suter TM, Statnick MA, Gehlert DR, Nelson DL, Lucaites VL, Emkey R, DeLapp NW, Wiernicki TR, Cramer JW, Yang CR, Bruns RF. Svensson KA, et al. Among authors: cramer jw. J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. doi: 10.1124/jpet.116.236372. Epub 2016 Nov 3. J Pharmacol Exp Ther. 2017. PMID: 27811173 Free PMC article.
The synthesis and evaluation of triazolopyrimidines as anti-tubercular agents.
Zuniga ES, Korkegian A, Mullen S, Hembre EJ, Ornstein PL, Cortez G, Biswas K, Kumar N, Cramer J, Masquelin T, Hipskind PA, Odingo J, Parish T. Zuniga ES, et al. Bioorg Med Chem. 2017 Aug 1;25(15):3922-3946. doi: 10.1016/j.bmc.2017.05.030. Epub 2017 May 19. Bioorg Med Chem. 2017. PMID: 28576632 Free PMC article.
Synthesis and SAR of novel histamine H3 receptor antagonists.
Jesudason CD, Beavers LS, Cramer JW, Dill J, Finley DR, Lindsley CW, Stevens FC, Gadski RA, Oldham SW, Pickard RT, Siedem CS, Sindelar DK, Singh A, Watson BM, Hipskind PA. Jesudason CD, et al. Among authors: cramer jw. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3415-8. doi: 10.1016/j.bmcl.2006.04.004. Epub 2006 May 3. Bioorg Med Chem Lett. 2006. PMID: 16677814
3-(4-Chloro-2-morpholin-4-yl-thiazol-5-yl)-8-(1-ethylpropyl)-2,6-dimethyl-imidazo[1,2-b]pyridazine: a novel brain-penetrant, orally available corticotropin-releasing factor receptor 1 antagonist with efficacy in animal models of alcoholism.
Gehlert DR, Cippitelli A, Thorsell A, Lê AD, Hipskind PA, Hamdouchi C, Lu J, Hembre EJ, Cramer J, Song M, McKinzie D, Morin M, Ciccocioppo R, Heilig M. Gehlert DR, et al. J Neurosci. 2007 Mar 7;27(10):2718-26. doi: 10.1523/JNEUROSCI.4985-06.2007. J Neurosci. 2007. PMID: 17344409 Free PMC article.
Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.
Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM. Poe MM, et al. Among authors: cramer jw. J Med Chem. 2016 Dec 8;59(23):10800-10806. doi: 10.1021/acs.jmedchem.6b01332. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933953 Free PMC article.
Synthesis and evaluation of the 2,4-diaminoquinazoline series as anti-tubercular agents.
Odingo J, O'Malley T, Kesicki EA, Alling T, Bailey MA, Early J, Ollinger J, Dalai S, Kumar N, Singh RV, Hipskind PA, Cramer JW, Ioerger T, Sacchettini J, Vickers R, Parish T. Odingo J, et al. Among authors: cramer jw. Bioorg Med Chem. 2014 Dec 15;22(24):6965-79. doi: 10.1016/j.bmc.2014.10.007. Epub 2014 Oct 22. Bioorg Med Chem. 2014. PMID: 25456390 Free article.
Identification of Phenoxyalkylbenzimidazoles with Antitubercular Activity.
Chandrasekera NS, Alling T, Bailey MA, Files M, Early JV, Ollinger J, Ovechkina Y, Masquelin T, Desai PV, Cramer JW, Hipskind PA, Odingo JO, Parish T. Chandrasekera NS, et al. Among authors: cramer jw. J Med Chem. 2015 Sep 24;58(18):7273-85. doi: 10.1021/acs.jmedchem.5b00546. Epub 2015 Sep 2. J Med Chem. 2015. PMID: 26295286
Structure-Based Design of Active-Site-Directed, Highly Potent, Selective, and Orally Bioavailable Low-Molecular-Weight Protein Tyrosine Phosphatase Inhibitors.
He R, Wang J, Yu ZH, Moyers JS, Michael MD, Durham TB, Cramer JW, Qian Y, Lin A, Wu L, Noinaj N, Barrett DG, Zhang ZY. He R, et al. Among authors: cramer jw. J Med Chem. 2022 Oct 27;65(20):13892-13909. doi: 10.1021/acs.jmedchem.2c01143. Epub 2022 Oct 5. J Med Chem. 2022. PMID: 36197449 Free PMC article.
Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis.
Martinez-Grau MA, Valcarcel ICG, Early JV, Gessner RK, de Melo CS, de la Nava EMM, Korkegian A, Ovechkina Y, Flint L, Gravelle A, Cramer JW, Desai PV, Street LJ, Odingo J, Masquelin T, Chibale K, Parish T. Martinez-Grau MA, et al. Among authors: cramer jw. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1758-1764. doi: 10.1016/j.bmcl.2018.04.028. Epub 2018 Apr 13. Bioorg Med Chem Lett. 2018. PMID: 29680666 Free PMC article.
54 results