Literature summary for 3.4.24.71 extracted from

Berger, Y.; Dehmlow, H.; Blum-Kaelin, D.; Kitas, E.A.; Loeffler, B.M.; Aebi, J.D.; Juillerat-Jeanneret, L.
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells (2005), J. Med. Chem., 48, 483-498.

Search for more literature for 3.4.24.71

Inhibitors

Inhibitors	Comment	Organism	Structure
(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester	IC50: 0.00109 mM	Homo sapiens
(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester	IC50: 0.01089 mM	Homo sapiens
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester	IC50: 0.0000765 mM	Homo sapiens
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester	IC50: 0.0000215 mM	Homo sapiens
(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide	IC50: 0.00253 mM	Homo sapiens
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester	IC50: 0.000137 mM	Homo sapiens
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester	IC50: 0.000067 mM	Homo sapiens
(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol	IC50: 0.0000729 mM	Homo sapiens
(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate	IC50: 0.0000198 mM	Homo sapiens
benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester	IC50: 0.0004805 mM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
umbilical vein endothelial cell line	-	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
0.0000198	-	IC50: 0.0000198 mM	Homo sapiens	(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate
0.0000215	-	IC50: 0.0000215 mM	Homo sapiens	(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester
0.000067	-	IC50: 0.000067 mM	Homo sapiens	(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester
0.0000729	-	IC50: 0.0000729 mM	Homo sapiens	(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
0.0000765	-	IC50: 0.0000765 mM	Homo sapiens	(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester
0.000137	-	IC50: 0.000137 mM	Homo sapiens	(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
0.0004805	-	IC50: 0.0004805 mM	Homo sapiens	benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
0.00109	-	IC50: 0.00109 mM	Homo sapiens	(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester
0.00253	-	IC50: 0.00253 mM	Homo sapiens	(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide
0.01089	-	IC50: 0.01089 mM	Homo sapiens	(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)