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Article

Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.

Bioorganic & medicinal chemistry letters - 15 Feb 2017

Keung Walter, Boloor Amogh, Brown Jason, Kiryanov Andre, Gangloff Anthony, Lawson J David, Skene Robert, Hoffman Isaac, Atienza Josephine, Kahana Jason, De Jong Ron, Farrell Pamela, Balakrishna Deepika, Halkowycz Petro

Abstract excerpt

Axl has been a target of interest in the oncology field for several years based on its role in various oncogenic processes. To date, no wild-type Axl crystal structure has been reported. Herein, we describe the structure-based optimization of a novel chemotype of Axl inhibitors, 1H-imidazole-2-carboxamide, using a mutated kinase homolog, Mer(I650M), as a crystallographic surrogate. Iterative optimization of the...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 28082036
DOI: 10.1016/j.bmcl.2016.12.024

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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