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Items: 1 to 20 of 102

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.

2.

Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.

Kong J, Chuddy J, Stock IA, Loria PM, Straub SV, Vage C, Cameron KO, Bhattacharya SK, Lapham K, McClure KF, Zhang Y, Jackson VM.

Br J Pharmacol. 2016 May;173(9):1452-64. doi: 10.1111/bph.13439. Epub 2016 Mar 17.

3.

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
4.

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.

5.

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.

6.

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.

7.

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.

Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2018 Jan 9. doi: 10.1021/acs.jmedchem.7b00982. [Epub ahead of print]

PMID:
29316397
8.

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
9.

Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.

Peukert S, Hughes R, Nunez J, He G, Yan Z, Jain R, Llamas L, Luchansky S, Carlson A, Liang G, Kunjathoor V, Pietropaolo M, Shapiro J, Castellana A, Wu X, Bose A.

ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8. doi: 10.1021/ml500240d. eCollection 2014 Oct 9.

10.

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
11.

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.

12.

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
13.

Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A, Gobbi A, Hawkins J, Johnson AR, La H, Lesch J, Lockey P, Norman M, Ouyang W, Summerhill S, Wong H.

J Med Chem. 2015 Jul 9;58(13):5308-22. doi: 10.1021/acs.jmedchem.5b00597. Epub 2015 Jun 23.

PMID:
26061388
14.

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.

15.

Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.

Hamdouchi C, Maiti P, Warshawsky AM, DeBaillie AC, Otto KA, Wilbur KL, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Cr S, Lineswala JP, Neathery GL, Bouaichi C, Diseroad BA, Campbell AN, Sweetana SA, Adams LA, Cabrera O, Ma X, Yumibe NP, Montrose-Rafizadeh C, Chen Y, Miller AR.

J Med Chem. 2018 Jan 5. doi: 10.1021/acs.jmedchem.7b01411. [Epub ahead of print]

PMID:
29236497
16.

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
17.

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
18.

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
19.

Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist.

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

ACS Med Chem Lett. 2015 Jan 13;6(3):266-70. doi: 10.1021/ml500391n. eCollection 2015 Mar 12.

20.

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.

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