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Items: 8

1.

Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.

Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O'Mahony A, Zimmerli SC, Bruns L, Bender AT, Schroeder P, Grenningloh R.

J Immunol. 2019 May 15;202(10):2888-2906. doi: 10.4049/jimmunol.1800583. Epub 2019 Apr 15.

2.

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.

ChemMedChem. 2019 Jan 22;14(2):217-223. doi: 10.1002/cmdc.201800714. Epub 2019 Jan 9.

PMID:
30521698
3.

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.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3419-3424. doi: 10.1016/j.bmcl.2018.09.033. Epub 2018 Sep 27.

PMID:
30290988
4.

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.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3307-3311. doi: 10.1016/j.bmcl.2018.09.018. Epub 2018 Sep 15.

PMID:
30243592
5.

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.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5.

PMID:
30122225
6.

Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling.

Bender AT, Gardberg A, Pereira A, Johnson T, Wu Y, Grenningloh R, Head J, Morandi F, Haselmayer P, Liu-Bujalski L.

Mol Pharmacol. 2017 Mar;91(3):208-219. doi: 10.1124/mol.116.107037. Epub 2017 Jan 6.

PMID:
28062735
7.

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.

Clin Immunol. 2016 Mar;164:65-77. doi: 10.1016/j.clim.2016.01.012. Epub 2016 Jan 25.

8.

SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors.

Karra S, Xiao Y, Chen X, Liu-Bujalski L, Huck B, Sutton A, Goutopoulos A, Askew B, Josephson K, Jiang X, Shutes A, Shankar V, Noonan T, Garcia-Berrios G, Dong R, Dhanabal M, Tian H, Wang Z, Clark A, Goodstal S.

Bioorg Med Chem Lett. 2013 May 15;23(10):3081-7. doi: 10.1016/j.bmcl.2013.03.008. Epub 2013 Mar 13.

PMID:
23570792

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