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ID: ALA1135360

Journal: Bioorg Med Chem Lett

Title: The design and synthesis of a novel series of indole derived selective ET(A) antagonists.

Authors: Rawson DJ, Dack KN, Dickinson RP, James K.

Abstract: Conformational constraint has been used as the key design element in the identification of a series of potent and selective ET(A) antagonists. The most potent antagonist, 32, (ET(A) IC(50)=0.55nM) is 722-fold selective over the ET(B) receptor, as measured by binding experiments.

CiteXplore: 11755336

DOI: 10.1016/s0960-894x(01)00660-6