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Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z. Burch JD, et al. Among authors: wang x. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z. Burch JD, et al. Among authors: wang x. J Med Chem. 2015 May 14;58(9):3806-16. doi: 10.1021/jm501998m. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25844760
Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).
MacKinnon CH, Lau K, Burch JD, Chen Y, Dines J, Ding X, Eigenbrot C, Heifetz A, Jaochico A, Johnson A, Kraemer J, Kruger S, Krülle TM, Liimatta M, Ly J, Maghames R, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Shia S, Stein DB, Trani G, Vaidya DG, Wang X, Bromidge SM, Wu LC, Pei Z. MacKinnon CH, et al. Among authors: wang x. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6331-5. doi: 10.1016/j.bmcl.2013.09.069. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24138940
Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).
Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MHA, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CAGN, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z. Trani G, et al. Among authors: wang x. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5818-5823. doi: 10.1016/j.bmcl.2014.10.020. Epub 2014 Oct 12. Bioorg Med Chem Lett. 2014. PMID: 25455497
Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).
Castanedo GM, Blaquiere N, Beresini M, Bravo B, Brightbill H, Chen J, Cui HF, Eigenbrot C, Everett C, Feng J, Godemann R, Gogol E, Hymowitz S, Johnson A, Kayagaki N, Kohli PB, Knüppel K, Kraemer J, Krüger S, Loke P, McEwan P, Montalbetti C, Roberts DA, Smith M, Steinbacher S, Sujatha-Bhaskar S, Takahashi R, Wang X, Wu LC, Zhang Y, Staben ST. Castanedo GM, et al. Among authors: wang x. J Med Chem. 2017 Jan 26;60(2):627-640. doi: 10.1021/acs.jmedchem.6b01363. Epub 2017 Jan 12. J Med Chem. 2017. PMID: 28005357
Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).
Feng JA, Lee P, Alaoui MH, Barrett K, Castanedo G, Godemann R, McEwan P, Wang X, Wu P, Zhang Y, Harris SF, Staben ST. Feng JA, et al. Among authors: wang x. ACS Med Chem Lett. 2019 Jul 24;10(9):1260-1265. doi: 10.1021/acsmedchemlett.8b00658. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531194 Free PMC article.
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