Literature DB >> 25716905

Discovery of hydroxyaniline amides as selective Extracellular Regulated Kinase (Erk) inhibitors.

Hugh Y Zhu1, Jagdish Desai1, Yongqi Deng2, Alan Cooper1, James Wang1, Jerry Shipps2, Ahmed Samatar3, Donna Carr3, William Windsor3.   

Abstract

Starting from weak μM hits identified through affinity based Automated Ligand Identification System (ALIS) screenings, double digit nM hydroxyaniline amide Erk inhibitors were discovered. This class of compounds had the unique dual mechanism of inhibiting activated and non-activated forms of Erk. They generally had high degree of selectivity in kinase panel tested.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  ALIS; Erk; Extracellular regulated kinase; MAPK; NeoMorph

Mesh:

Substances:

Year:  2015        PMID: 25716905     DOI: 10.1016/j.bmcl.2015.01.049

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  A high throughput assay to identify substrate-selective inhibitors of the ERK protein kinases.

Authors:  Chad J Miller; Yagmur Muftuoglu; Benjamin E Turk
Journal:  Biochem Pharmacol       Date:  2017-06-21       Impact factor: 5.858

2.  MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Authors:  Sobhana Babu Boga; Yongqi Deng; Liang Zhu; Yang Nan; Alan B Cooper; Gerald W Shipps; Ronald Doll; Neng-Yang Shih; Hugh Zhu; Robert Sun; Tong Wang; Sunil Paliwal; Hon-Chung Tsui; Xiaolei Gao; Xin Yao; Jagdish Desai; James Wang; Abdul Basit Alhassan; Joseph Kelly; Mehul Patel; Kiran Muppalla; Subrahmanyam Gudipati; Li-Kang Zhang; Alexei Buevich; David Hesk; Donna Carr; Priya Dayananth; Stuart Black; Hong Mei; Kathleen Cox; Bradley Sherborne; Alan W Hruza; Li Xiao; Weihong Jin; Brian Long; Gongjie Liu; Stacey A Taylor; Paul Kirschmeier; William T Windsor; Robert Bishop; Ahmed A Samatar
Journal:  ACS Med Chem Lett       Date:  2018-06-14       Impact factor: 4.345

3.  Importance of protein flexibility in ranking ERK2 Type I1/2 inhibitor affinities: a computational study.

Authors:  Yuzhen Niu; Xiaojun Yao; Hongfang Ji
Journal:  RSC Adv       Date:  2019-04-23       Impact factor: 4.036

  3 in total

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