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Updated: Jun 14, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors
David K Williams1, Xiao-Tao Chen, Christine Tarby
1Bristol-Myers Squibb Research and Development, PO Box 4000, Princeton, NJ 08543-4000, USA. david.williams@bms.com
Abstract:
Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds demonstrate nanomolar potency in Met kinase biochemical assays and significant activity in the Met-driven GTL-16 human gastric carcinoma cell line. X-ray crystallography revealed that these compounds adopt a bioactive conformation, in the kinase domain, consistent with that previously seen with 2-pyridone-based Met kinase inhibitors. Compound 9b demonstrated potent in vivo antitumor activity in the GTL-16 human tumor xenograft model.
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