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Pyrazole CCK(1) receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free-Wilson additivity
Authors:Sehon Clark  McClure Kelly  Hack Michael  Morton Magda  Gomez Laurent  Li Lina  Barrett Terrance D  Shankley Nigel  Breitenbucher J Guy
Institution:Johnson and Johnson Pharmaceutical Research and Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
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.
Keywords:
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