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Results: 1 to 20 of 96

1.

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.

ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8.

PMID:
24900864
[PubMed]
2.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30.

PMID:
23953189
[PubMed - indexed for MEDLINE]
3.

Ghrelin receptor inverse agonists: identification of an active peptide core and its interaction epitopes on the receptor.

Holst B, Lang M, Brandt E, Bach A, Howard A, Frimurer TM, Beck-Sickinger A, Schwartz TW.

Mol Pharmacol. 2006 Sep;70(3):936-46. Epub 2006 Jun 23.

PMID:
16798937
[PubMed - indexed for MEDLINE]
Free Article
4.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B.

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8.

PMID:
24900280
[PubMed]
Free PMC Article
5.

Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.

Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P.

ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. doi: 10.1021/ml200051p. eCollection 2011 May 12.

PMID:
24900321
[PubMed]
Free PMC Article
6.

Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.

Arhancet GB, Walker DP, Metz S, Fobian YM, Heasley SE, Carter JS, Springer JR, Jones DE, Hayes MJ, Shaffer AF, Jerome GM, Baratta MT, Zweifel B, Moore WM, Masferrer JL, Vazquez ML.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. doi: 10.1016/j.bmcl.2012.11.109. Epub 2012 Dec 6.

PMID:
23260349
[PubMed - indexed for MEDLINE]
7.

Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.

Negoro N, Sasaki S, Mikami S, Ito M, Suzuki M, Tsujihata Y, Ito R, Harada A, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Tanaka T, Kogame A, Matsunaga S, Yasuma T, Momose Y.

ACS Med Chem Lett. 2010 Jun 18;1(6):290-4. doi: 10.1021/ml1000855. eCollection 2010 Sep 9.

PMID:
24900210
[PubMed]
Free PMC Article
8.

Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor.

Kung DW, Coffey SB, Jones RM, Cabral S, Jiao W, Fichtner M, Carpino PA, Rose CR, Hank RF, Lopaze MG, Swartz R, Chen HT, Hendsch Z, Posner B, Wielis CF, Manning B, Dubins J, Stock IA, Varma S, Campbell M, DeBartola D, Kosa-Maines R, Steyn SJ, McClure KF.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. doi: 10.1016/j.bmcl.2012.05.024. Epub 2012 May 17.

PMID:
22677316
[PubMed - indexed for MEDLINE]
9.

High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.

Holst B, Cygankiewicz A, Jensen TH, Ankersen M, Schwartz TW.

Mol Endocrinol. 2003 Nov;17(11):2201-10. Epub 2003 Aug 7.

PMID:
12907757
[PubMed - indexed for MEDLINE]
10.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.

ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. doi: 10.1021/ml1001536. eCollection 2010 Dec 9.

PMID:
24900235
[PubMed]
Free PMC Article
11.

GABAA receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement.

Atack JR.

Curr Top Med Chem. 2011;11(9):1203-14. Review.

PMID:
21050171
[PubMed - indexed for MEDLINE]
12.

Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.

Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, Ahn K.

ACS Med Chem Lett. 2011 Feb 10;2(2):91-96.

PMID:
21666860
[PubMed]
Free PMC Article
13.

Unique interaction pattern for a functionally biased ghrelin receptor agonist.

Sivertsen B, Lang M, Frimurer TM, Holliday ND, Bach A, Els S, Engelstoft MS, Petersen PS, Madsen AN, Schwartz TW, Beck-Sickinger AG, Holst B.

J Biol Chem. 2011 Jun 10;286(23):20845-60. doi: 10.1074/jbc.M110.173237. Epub 2011 Mar 14.

PMID:
21402696
[PubMed - indexed for MEDLINE]
Free PMC Article
14.

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.

Guo L, Ye Z, Liu J, He S, Bakshi RK, Sebhat IK, Dobbelaar PH, Hong Q, Jian T, Dellureficio JP, Tsou NN, Ball RG, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Chen HY, Chen AS, Martin WJ, MacIntyre DE, Strack AM, Fong TM, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4895-900. doi: 10.1016/j.bmcl.2010.06.068. Epub 2010 Jun 17.

PMID:
20621473
[PubMed - indexed for MEDLINE]
15.

Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity.

Rudolph J, Esler WP, O'connor S, Coish PD, Wickens PL, Brands M, Bierer DE, Bloomquist BT, Bondar G, Chen L, Chuang CY, Claus TH, Fathi Z, Fu W, Khire UR, Kristie JA, Liu XG, Lowe DB, McClure AC, Michels M, Ortiz AA, Ramsden PD, Schoenleber RW, Shelekhin TE, Vakalopoulos A, Tang W, Wang L, Yi L, Gardell SJ, Livingston JN, Sweet LJ, Bullock WH.

J Med Chem. 2007 Oct 18;50(21):5202-16. Epub 2007 Sep 21.

PMID:
17887659
[PubMed - indexed for MEDLINE]
16.

Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists.

Takano R, Yoshida M, Inoue M, Honda T, Nakashima R, Matsumoto K, Yano T, Ogata T, Watanabe N, Toda N.

Bioorg Med Chem Lett. 2014 Jul 1;24(13):2949-53. doi: 10.1016/j.bmcl.2014.04.065. Epub 2014 Apr 26.

PMID:
24835985
[PubMed - in process]
17.

Design, evaluation, and comparison of ghrelin receptor agonists and inverse agonists as suitable radiotracers for PET imaging.

Chollet C, Bergmann R, Pietzsch J, Beck-Sickinger AG.

Bioconjug Chem. 2012 Apr 18;23(4):771-84. doi: 10.1021/bc2005889. Epub 2012 Mar 20.

PMID:
22372770
[PubMed - indexed for MEDLINE]
18.

Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.

Bell IM, Gallicchio SN, Wood MR, Quigley AG, Stump CA, Zartman CB, Fay JF, Li CC, Lynch JJ, Moore EL, Mosser SD, Prueksaritanont T, Regan CP, Roller S, Salvatore CA, Kane SA, Vacca JP, Selnick HG.

ACS Med Chem Lett. 2010 Jan 12;1(1):24-9. doi: 10.1021/ml900016y. eCollection 2010 Apr 8.

PMID:
24900170
[PubMed]
Free PMC Article
19.
20.

68Ga-Labeled NODAGA-conjugated ghrelin receptor agonists and inverse agonists.

Chopra A.

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Jun 10 [updated 2012 Jul 12].

PMID:
22787690
[PubMed]
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