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791 results

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Page 1
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B. Qiu H, et al. Among authors: caldwell r. Bioorg Med Chem. 2021 Jun 15;40:116163. doi: 10.1016/j.bmc.2021.116163. Epub 2021 Apr 20. Bioorg Med Chem. 2021. PMID: 33932711
Btk inhibition treats TLR7/IFN driven murine lupus.
Bender AT, Pereira A, Fu K, Samy E, Wu Y, Liu-Bujalski L, Caldwell R, Chen YY, Tian H, Morandi F, Head J, Koehler U, Genest M, Okitsu SL, Xu D, Grenningloh R. Bender AT, et al. Among authors: caldwell r. Clin Immunol. 2016 Mar;164:65-77. doi: 10.1016/j.clim.2016.01.012. Epub 2016 Jan 25. Clin Immunol. 2016. PMID: 26821304 Free article.
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B. Qiu H, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5. Bioorg Med Chem Lett. 2018. PMID: 30122225
Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.
Qiu H, Liu-Bujalski L, Caldwell RD, Viacava Follis A, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones CCV, Jones R, Mochalkin I, Morandi F, Neagu C, Potnick J, Sherer B. Qiu H, et al. Among authors: caldwell rd. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3307-3311. doi: 10.1016/j.bmcl.2018.09.018. Epub 2018 Sep 15. Bioorg Med Chem Lett. 2018. PMID: 30243592
Discovery of Affinity-Based Probes for Btk Occupancy Assays.
Qiu H, Caldwell R, Liu-Bujalski L, Goutopoulos A, Jones R, Potnick J, Sherer B, Bender A, Grenningloh R, Xu D, Gardberg A, Mochalkin I, Johnson T, Viacava Follis A, Head J, Morandi F. Qiu H, et al. Among authors: caldwell r. ChemMedChem. 2019 Jan 22;14(2):217-223. doi: 10.1002/cmdc.201800714. Epub 2019 Jan 9. ChemMedChem. 2019. PMID: 30521698
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists.
Xiao Y, Karra S, Goutopoulos A, Morse NT, Zhang S, Dhanabal M, Tian H, Seenisamy J, Jayadevan J, Caldwell R, Potnick J, Bleich M, Chekler E, Sherer B, Sriraman V. Xiao Y, et al. Among authors: caldwell r. Bioorg Med Chem Lett. 2019 Jul 1;29(13):1660-1664. doi: 10.1016/j.bmcl.2019.04.033. Epub 2019 Apr 24. Bioorg Med Chem Lett. 2019. PMID: 31031055
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression.
Guler S, DiPoto MC, Crespo A, Caldwell R, Doerfel B, Grossmann N, Ho K, Huck B, Jones CC, Lan R, Musil D, Potnick J, Schilke H, Sherer B, Simon S, Sirrenberg C, Zhang Z, Liu-Bujalski L. Guler S, et al. Among authors: caldwell r. ACS Med Chem Lett. 2023 Apr 7;14(5):566-576. doi: 10.1021/acsmedchemlett.2c00481. eCollection 2023 May 11. ACS Med Chem Lett. 2023. PMID: 37197456 Free PMC article.
791 results