We tested the interaction of 72 kinase inhibitors with 442 kinases covering> 80% of the
human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more …

Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets,.
The biological consequences of multi-kinase activity are poorly defined, and an important …

Protein kinases have emerged as one of the most successful families of drug targets. To
date, most selective kinase inhibitors have been discovered serendipitously either through …

Small-molecule protein kinase inhibitors are widely used to elucidate cellular signaling
pathways and are promising therapeutic agents. Owing to evolutionary conservation of the …

Protein kinases are important targets in drug discovery programs aimed at treating many
devastating diseases, including cancer, autoimmune disorders, diabetes, and neurological …

Publicly available kinase inhibitors have been analyzed in detail. Nearly 19000 inhibitors
have been identified with activity against 266 different kinases. Thus, about half of the …

Despite the success of protein kinase inhibitors as approved therapeutics, drug discovery
has focused on a small subset of kinase targets. Here we provide a thorough …

A kinome-wide selectivity screen of> 20000 compounds with a rich representation of many
structural classes has been completed. Analysis of the selectivity patterns for each class …

Protein kinase inhibitors are a well-established class of clinically useful drugs, particularly
for the treatment of cancer. Achieving inhibitor selectivity for particular protein kinases often …

Protein kinases continue to hold tremendous promise for therapeutic intervention, and the
search for novel, safe and efficacious kinase inhibitors has intensified over the past decade …