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]
- 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