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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: johnson t. 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
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.
Liu H, Kuhn C, Feru F, Jacques SL, Deshmukh GD, Ye P, Rennie GR, Johnson T, Kazmirski S, Low S, Coli R, Ding YH, Cheng AC, Tecle H, English JM, Stanton R, Wu JC. Liu H, et al. Among authors: johnson t. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4885-91. doi: 10.1016/j.bmcl.2010.06.073. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20620059
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: johnson t. 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 a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
Caldwell R, Liu-Bujalski L, Qiu H, Mochalkin I, Jones R, Neagu C, Goutopoulos A, Grenningloh R, Johnson T, Sherer B, Gardberg A, Follis AV, Morandi F, Head J. Caldwell R, et al. Among authors: johnson t. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3419-3424. doi: 10.1016/j.bmcl.2018.09.033. Epub 2018 Sep 27. Bioorg Med Chem Lett. 2018. PMID: 30290988
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: johnson t. ChemMedChem. 2019 Jan 22;14(2):217-223. doi: 10.1002/cmdc.201800714. Epub 2019 Jan 9. ChemMedChem. 2019. PMID: 30521698
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. Among authors: johnson tl. 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
Large-Scale Assessment of Binding Free Energy Calculations in Active Drug Discovery Projects.
Schindler CEM, Baumann H, Blum A, Böse D, Buchstaller HP, Burgdorf L, Cappel D, Chekler E, Czodrowski P, Dorsch D, Eguida MKI, Follows B, Fuchß T, Grädler U, Gunera J, Johnson T, Jorand Lebrun C, Karra S, Klein M, Knehans T, Koetzner L, Krier M, Leiendecker M, Leuthner B, Li L, Mochalkin I, Musil D, Neagu C, Rippmann F, Schiemann K, Schulz R, Steinbrecher T, Tanzer EM, Unzue Lopez A, Viacava Follis A, Wegener A, Kuhn D. Schindler CEM, et al. Among authors: johnson t. J Chem Inf Model. 2020 Nov 23;60(11):5457-5474. doi: 10.1021/acs.jcim.0c00900. Epub 2020 Sep 3. J Chem Inf Model. 2020. PMID: 32813975
6,767 results