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4-Anilinoquinolines were identified as potent and narrow-spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quinoline substituents produced GAK inhibitors with nanomolar activity, over 50 000-fold selectivity relative to other members of the numb-associated kinase (NAK) subfamily, and a compound (6,7-dimethoxy-N-(3,4,5-trimethoxyphenyl)quinolin-4-amine; 49) with a narrow-spectrum kinome profile. These compounds may be useful tools to explore the therapeutic potential of GAK in prevention of a broad range of infectious and systemic diseases.

Original publication




Journal article



Publication Date





48 - 66


anilinoquinolines, antibacterial agents, chemical probes, cyclin G associated kinase (GAK), Aniline Compounds, Binding Sites, Catalytic Domain, Drug Design, Endocytosis, Humans, Intracellular Signaling Peptides and Proteins, Kinetics, Molecular Docking Simulation, Protein Binding, Protein Kinase Inhibitors, Protein Serine-Threonine Kinases, Quinazolines, Structure-Activity Relationship, Viruses