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Page 1
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. Xue CB, et al. ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. doi: 10.1021/ml1001536. eCollection 2010 Dec 9. ACS Med Chem Lett. 2010. PMID: 24900235 Free PMC article.
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B. Xue CB, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036044
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Baribaud F, Shin N, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B, Xue CB. Zheng C, et al. Among authors: xue cb. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295478
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. Xue CB, et al. ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900280 Free PMC article.
Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
Xue CB, Feng H, Cao G, Huang T, Glenn J, Anand R, Meloni D, Zhang K, Kong L, Wang A, Zhang Y, Zheng C, Xia M, Chen L, Tanaka H, Han Q, Robinson DJ, Modi D, Storace L, Shao L, Sharief V, Li M, Galya LG, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B. Xue CB, et al. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. doi: 10.1021/ml200030q. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900329 Free PMC article.
Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K. Brodmerkel CM, et al. Among authors: xue cb. J Immunol. 2005 Oct 15;175(8):5370-8. doi: 10.4049/jimmunol.175.8.5370. J Immunol. 2005. PMID: 16210643
Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.
Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R. Shin N, et al. Among authors: xue cb. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1. J Pharmacol Exp Ther. 2011. PMID: 21459966
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Yue EW, Li YL, Douty B, He C, Mei S, Wayland B, Maduskuie T, Falahatpisheh N, Sparks RB, Polam P, Zhu W, Glenn J, Feng H, Zhang K, Li Y, He X, Katiyar K, Covington M, Feldman P, Shin N, Wang KH, Diamond S, Li Y, Koblish HK, Hall L, Scherle P, Yeleswaram S, Xue CB, Metcalf B, Combs AP, Yao W. Yue EW, et al. Among authors: xue cb. ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560. doi: 10.1021/acsmedchemlett.9b00334. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749910 Free PMC article.
Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.
Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA. Shin N, et al. Among authors: xue cb. Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5. doi: 10.1016/j.bbrc.2009.06.135. Epub 2009 Jul 1. Biochem Biophys Res Commun. 2009. PMID: 19576173
Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.
Hughes RO, Rogier DJ, Devraj R, Zheng C, Cao G, Feng H, Xia M, Anand R, Xing L, Glenn J, Zhang K, Covington M, Morton PA, Hutzler JM, Davis JW 2nd, Scherle P, Baribaud F, Bahinski A, Mo ZL, Newton R, Metcalf B, Xue CB. Hughes RO, et al. Among authors: xue cb. Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30. doi: 10.1016/j.bmcl.2011.01.034. Epub 2011 Jan 15. Bioorg Med Chem Lett. 2011. PMID: 21315584
81 results