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5,081 results

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Page 1
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.
Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Eigenbrot C, Gallion S, Johnson AR, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Wang X, Wong H, Xiong JM, Xu J, Yu C, Zhao Z, Currie KS. Young WB, et al. Among authors: wong h. Bioorg Med Chem Lett. 2016 Jan 15;26(2):575-579. doi: 10.1016/j.bmcl.2015.11.076. Epub 2015 Nov 24. Bioorg Med Chem Lett. 2016. PMID: 26675441
Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor.
Liu L, Halladay JS, Shin Y, Wong S, Coraggio M, La H, Baumgardner M, Le H, Gopaul S, Boggs J, Kuebler P, Davis JC Jr, Liao XC, Lubach JW, Deese A, Sowell CG, Currie KS, Young WB, Khojasteh SC, Hop CE, Wong H. Liu L, et al. Among authors: wong s, wong h. Drug Metab Dispos. 2011 Oct;39(10):1840-9. doi: 10.1124/dmd.111.040840. Epub 2011 Jul 8. Drug Metab Dispos. 2011. PMID: 21742900
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Gallion S, Hymowitz SG, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Maurer B, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Sowell CG, Wang X, Wong H, Xiong JM, Xu J, Zhao Z, Currie KS. Young WB, et al. Among authors: wong h. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333-7. doi: 10.1016/j.bmcl.2015.01.032. Epub 2015 Feb 7. Bioorg Med Chem Lett. 2015. PMID: 25701252
Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.
Erickson RI, Schutt LK, Tarrant JM, McDowell M, Liu L, Johnson AR, Lewin-Koh SC, Hedehus M, Ross J, Carano RA, Staflin K, Zhong F, Crawford JJ, Zhong S, Reif K, Katewa A, Wong H, Young WB, Dambach DM, Misner DL. Erickson RI, et al. Among authors: wong h. J Pharmacol Exp Ther. 2017 Jan;360(1):226-238. doi: 10.1124/jpet.116.236224. Epub 2016 Nov 7. J Pharmacol Exp Ther. 2017. PMID: 27821712
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Wang X, Barbosa J, Blomgren P, Bremer MC, Chen J, Crawford JJ, Deng W, Dong L, Eigenbrot C, Gallion S, Hau J, Hu H, Johnson AR, Katewa A, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, DiPaolo J, Reif K, Scheerens H, Schmitt A, Wong H, Xiong JM, Xu J, Zhao Z, Zhou F, Currie KS, Young WB. Wang X, et al. Among authors: wong h. ACS Med Chem Lett. 2017 May 3;8(6):608-613. doi: 10.1021/acsmedchemlett.7b00103. eCollection 2017 Jun 8. ACS Med Chem Lett. 2017. PMID: 28626519 Free PMC article.
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB. Crawford JJ, et al. Among authors: wong h. J Med Chem. 2018 Mar 22;61(6):2227-2245. doi: 10.1021/acs.jmedchem.7b01712. Epub 2018 Feb 23. J Med Chem. 2018. PMID: 29457982
Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis.
Katewa A, Wang Y, Hackney JA, Huang T, Suto E, Ramamoorthi N, Austin CD, Bremer M, Chen JZ, Crawford JJ, Currie KS, Blomgren P, DeVoss J, DiPaolo JA, Hau J, Johnson A, Lesch J, DeForge LE, Lin Z, Liimatta M, Lubach JW, McVay S, Modrusan Z, Nguyen A, Poon C, Wang J, Liu L, Lee WP, Wong H, Young WB, Townsend MJ, Reif K. Katewa A, et al. Among authors: wong h. JCI Insight. 2017 Apr 6;2(7):e90111. doi: 10.1172/jci.insight.90111. JCI Insight. 2017. PMID: 28405610 Free PMC article.
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
Crawford JJ, Lee W, Johnson AR, Delatorre KJ, Chen J, Eigenbrot C, Heidmann J, Kakiuchi-Kiyota S, Katewa A, Kiefer JR, Liu L, Lubach JW, Misner D, Purkey H, Reif K, Vogt J, Wong H, Yu C, Young WB. Crawford JJ, et al. Among authors: wong h. ACS Med Chem Lett. 2020 Jul 13;11(8):1588-1597. doi: 10.1021/acsmedchemlett.0c00249. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832028 Free PMC article.
Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy.
Liu L, Di Paolo J, Barbosa J, Rong H, Reif K, Wong H. Liu L, et al. Among authors: wong h. J Pharmacol Exp Ther. 2011 Jul;338(1):154-63. doi: 10.1124/jpet.111.181545. Epub 2011 Apr 26. J Pharmacol Exp Ther. 2011. PMID: 21521773
5,081 results