(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulf onamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.

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Bell MG, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK

(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulf onamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.

J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.

PubMed ID

18038968 [ View in PubMed

]

Abstract

A novel, potent series of indole analogs were recently developed as MR antagonists, culminating in 14. This compound represents the first MR antagonist in this class of molecules, exhibiting picomolar binding affinity and in vivo blood pressure lowering at pharmaceutically relevant doses.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Spironolactone	Androgen receptor	Ki (nM)	39.4	N/A	N/A	Details
Spironolactone	Glucocorticoid receptor	Ki (nM)	32.6	N/A	N/A	Details
Spironolactone	Mineralocorticoid receptor	Ki (nM)	2.323	N/A	N/A	Details
Spironolactone	Progesterone receptor	Ki (nM)	399.7	N/A	N/A	Details