Literature DB >> 21515047

3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: design and development to a highly selective lead.

Michael Soth1, Sarah Abbot, Allassan Abubakari, Nidhi Arora, Humberto Arzeno, Roland Billedeau, Nolan Dewdney, Kieran Durkin, Sandra Frauchiger, Manjiri Ghate, David M Goldstein, Ronald J Hill, Andreas Kuglstatter, Fujun Li, Brad Loe, Kristen McCaleb, Joel McIntosh, Eva Papp, Jaehyeon Park, Martin Stahl, Man-Ling Sung, Rebecca Suttman, David C Swinney, Paul Weller, Brian Wong, Hasim Zecic, Tobias Gabriel.   

Abstract

Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21515047     DOI: 10.1016/j.bmcl.2011.03.098

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


  2 in total

1.  Virtual screening using a conformationally flexible target protein: models for ligand binding to p38α MAPK.

Authors:  Natalie B Vinh; Jamie S Simpson; Peter J Scammells; David K Chalmers
Journal:  J Comput Aided Mol Des       Date:  2012-04-20       Impact factor: 3.686

2.  IL-13-induced airway mucus production is attenuated by MAPK13 inhibition.

Authors:  Yael G Alevy; Anand C Patel; Arthur G Romero; Dhara A Patel; Jennifer Tucker; William T Roswit; Chantel A Miller; Richard F Heier; Derek E Byers; Tom J Brett; Michael J Holtzman
Journal:  J Clin Invest       Date:  2012-11-26       Impact factor: 14.808

  2 in total

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