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Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase

Bagdanoff, Jeffrey and Jain, Rama and Han, Wooseok and Zhu, Shejin and Madera, Ann Marie and Lee, Patrick and Poon, Daniel (2015) Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase. Bioorganic and Medicinal Chemistry Letters, 25 (18). pp. 3788-3792. ISSN 14643405

Abstract

Abstract A series of structure based drug design hypotheses and focused screening efforts led to the identification of tetrahydropyrrolo-diazepenones with striking potency against ERK2 kinase. The role of fluorination in mitigating microsomal clearance was systematically explored. Ultimately, it was found that fluorination of a cyclopentanol substructure provided significant improvement in both potency and human metabolic stability.

Item Type: Article
Keywords: ATP binding cleft ERK2 kinase Extraction ratio Lower-hinge lysine Structure based drug design
Date Deposited: 25 Nov 2017 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/25620

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