Literature DB >> 16236506

Pyrazole CCK(1) receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free-Wilson additivity.

Clark Sehon1, Kelly McClure, Michael Hack, Magda Morton, Laurent Gomez, Lina Li, Terrance D Barrett, Nigel Shankley, J Guy Breitenbucher.   

Abstract

High-throughput screening revealed compound 1 as a potent antagonist of the CCK(1) receptor. Here, we disclose the synthesis of combinatorial libraries by solid-phase synthesis on Kenner 'safety catch' resin. Additive QSAR models were used to determine a lack of consistent additive SAR within the matrix.

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Year:  2005        PMID: 16236506     DOI: 10.1016/j.bmcl.2005.09.041

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


  2 in total

1.  Decision Making in Medicinal Chemistry: The Power of Our Intuition.

Authors:  Laurent Gomez
Journal:  ACS Med Chem Lett       Date:  2018-09-11       Impact factor: 4.345

2.  Nonadditivity in public and inhouse data: implications for drug design.

Authors:  D Gogishvili; E Nittinger; C Margreitter; C Tyrchan
Journal:  J Cheminform       Date:  2021-07-02       Impact factor: 5.514

  2 in total

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