Literature summary for 3.4.24.71 extracted from

Trapani, A.J.; Beil, M.E.; Bruseo, C.W.; Savage, P.; Firooznia, F.; Jeng, A.Y.
CGS 35601 and its orally active prodrug CGS 37808 as triple inhibitors of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme (2004), J. Cardiovasc. Pharmacol., 44, S211-S215.

No PubMed abstract available

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Chinese hamster ovary cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
L-tryptophan, N-[[1-[[(2S)-2-(acetylthio)-4-methyl-1 oxopentyl]amino]cyclopentyl]-carbonyl]-methyl ester	CGS 37808, at an oral dose of 10 mgEq per kg, CGS 37808 produced 71% and 67% inhibition of the big ET-1 pressor response at 30 and 120 min, respectively	Homo sapiens
L-tryptophan, N-[[1-[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]-cyclopentyl]carbonyl]	CGS 35601, IC50: 55 nM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Synonyms

Synonyms	Comment	Organism
ECE-1	-	Homo sapiens
endothelin-converting enzyme-1	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000055	-	CGS 35601, IC50: 55 nM	Homo sapiens	L-tryptophan, N-[[1-[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]-cyclopentyl]carbonyl]

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Release 2023.1 (January 2023)