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

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Rawson DJ, Dack KN, Dickinson RP, James K

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

Bioorg Med Chem Lett. 2002 Jan 21;12(2):125-8.

PubMed ID

11755336 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Darusentan	Endothelin-1 receptor	IC 50 (nM)	0.8	N/A	N/A	Details