Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 2, Pages 123-128Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml200249h
Keywords
affinity selection-mass spectrometry (AS-MS); Automated Ligand Identification System (ALIS); CHK1 protein kinase; structure-based drug design; thiazole-4-carboxamide
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A novel series of CHK1 inhibitors with a distinctive hinge binding mode, exemplified by 2-aryl-N-(2-(piperazin-1-yl)phenyl)thiazole-4-carboxamide, was discovered through high-throughput screening using the affinity selection-mass spectrometry (AS-MS)-based Automated Ligand Identification System (ALIS) platform. Structure-based ligand design and optimization led to significant improvements in potency to the single digit nanomolar range and hundred-fold selectivity against CDK2.
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