K
Ken A. Brameld
Researcher at Hoffmann-La Roche
Publications - 44
Citations - 3220
Ken A. Brameld is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Bruton's tyrosine kinase & Tyrosine kinase. The author has an hindex of 22, co-authored 43 publications receiving 2993 citations. Previous affiliations of Ken A. Brameld include California Institute of Technology & University of Illinois at Urbana–Champaign.
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PatentDOI
Tyrosine kinase inhibitors
TL;DR: In this article, the imidazo[1,2-a]pyrimidine derivatives are used for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET.
Journal ArticleDOI
Prolonged and tunable residence time using reversible covalent kinase inhibitors
J. Michael Bradshaw,Jesse M. McFarland,Ville O. Paavilainen,Angelina Bisconte,Danny Tam,Vernon T. Phan,Sergei Romanov,David Finkle,Jin Shu,Vaishali Patel,Tony Ton,Xiaoyan Li,David G Loughhead,Philip A. Nunn,Dane Karr,Mary E. Gerritsen,Jens Oliver Funk,Timothy D. Owens,Erik Verner,Ken A. Brameld,Ronald J. Hill,David Michael Goldstein,Jack Taunton +22 more
TL;DR: Progress is demonstrated by targeting a noncatalytic cysteine in Bruton's tyrosine kinase (BTK) with reversible covalent inhibitors to discover potent and selective BTK inhibitors that demonstrate biochemical residence times spanning from minutes to 7 days.
Journal ArticleDOI
Small Molecule Conformational Preferences Derived from Crystal Structure Data. A Medicinal Chemistry Focused Analysis
TL;DR: Based on torsion angle distributions of frequently occurring substructures, conformation preferences of druglike molecules are presented, accompanied by a review of the relevant literature and properties of aryl ring substituents are discussed.
Journal ArticleDOI
The pKBHX Database: Toward a Better Understanding of Hydrogen-Bond Basicity for Medicinal Chemists
TL;DR: This paper reviews hydrogenbond basicity scales in general and introduces the pKBHX scale with a brief thermodynamic discussion on the treatment of polyfunctional compounds and discusses the effects of a medium more polar than the definition solvent CCl4 and changes in the reference HB donor on the p KBHX Scale.
Journal ArticleDOI
The chitinase PfCHT1 from the human malaria parasite Plasmodium falciparum lacks proenzyme and chitin-binding domains and displays unique substrate preferences
Joseph M. Vinetz,Sanat K. Dave,Charles A. Specht,Ken A. Brameld,Bo Xu,Rhian E. Hayward,David A. Fidock +6 more
TL;DR: PgCHT1 may be the ortholog of a second, as yet unidentified, chitinase gene of P. gallinaceum, and may allow us to develop novel strategies of blocking human malaria transmission based on interfering with P. falciparum chitInase.