McClure Kelly, Hack Michael, Huang Liming, Sehon Clark, Morton Magda, Li Lina, Barrett Terrance D, Shankley Nigel, Breitenbucher J Guy
Johnson and Johnson Pharmaceutical Research and Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2006 Jan 1;16(1):72-6. doi: 10.1016/j.bmcl.2005.09.048. Epub 2005 Oct 19.
High throughput screening revealed compound 1 as a potent antagonist of the CCK(1) receptor. Evaluation of the CCK(1) SAR in a series of these diarylpyrazole antagonists was conducted in a matrix synthesis format revealing additive (Free-Wilson) and non-additive SAR. This use of additive QSAR modeling in conjunction with combinatorial libraries represents a unique approach to the evaluation of SAR interactions between the variables of any combinatorial matrix.
高通量筛选显示化合物1是一种有效的CCK(1)受体拮抗剂。在一系列这些二芳基吡唑拮抗剂中，以矩阵合成形式对CCK(1)的构效关系进行了评估，揭示了累加性（Free-Wilson）和非累加性构效关系。这种将累加性定量构效关系建模与组合文库相结合的方法，代表了一种评估任何组合矩阵变量之间构效关系相互作用的独特方法。
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