There are∼ 4500 genes within the 'druggable genome', the subset of the human genome
that expresses proteins able to bind drug-like molecules, yet existing drugs only target a few …

Given the ubiquity of heterocycles in biologically active molecules, transformations with the
capacity to modify such molecular skeletons with modularity remain highly desirable. Ring …

Abstract Adaptor-Associated Kinase 1 (AAK1), a Ser/Thr protein kinase, responsible for
regulating clathrin-mediated endocytosis, is ubiquitous in the central nervous system (CNS) …

Pathological loss-of-function mutations in cyclin-dependent kinase-like 5 (CDKL5) cause
CDKL5 deficiency disorder (CDD), a rare and severe neurodevelopmental disorder …

Naphthyridine-based inhibitors were synthesized to yield a potent and cell-active inhibitor of
casein kinase 2 (CK2). Compound 2 selectively inhibits CK2α and CK2α′ when profiled …

An iron‐catalysed carbene transfer reaction of diazo compounds to isocyanides has been
developed. The resulting ketenimines are trapped in situ with various bisnucleophiles to …

Tau tubulin kinase 1 and 2 (TTBK1/2) are highly homologous kinases that are expressed
and mediate disease-relevant pathways predominantly in the brain. Distinct roles for TTBK1 …

From a designed library of indolyl pyrimidinamines, we identified a highly potent and cell-
active chemical probe (17) that inhibits phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) …

Binding affinity is an important factor in drug design to improve drug-target selectivity and
specificity. In this study, in silico techniques based on molecular docking followed by …

Modern drug discovery relies on combinatorial screening campaigns to find drug molecules
targeting specific disease-associated proteins. The success of such campaigns often relies …