SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.

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Gomez L, Hack MD, McClure K, Sehon C, Huang L, Morton M, Li L, Barrett TD, Shankley N, Breitenbucher JG

SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6493-8. Epub 2007 Oct 1.

PubMed ID

17933530 [ View in PubMed

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Abstract

A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK(1) receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between the two enantiomers for the CCK(1) receptor and the flexible nature of the linker led to the design of constrained analogs with increased potency.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Lintitript	Cholecystokinin receptor type A	IC 50 (nM)	0.56	N/A	N/A	Details