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Literature summary for 3.5.3.18 extracted from

  • Kotthaus, J.; Schade, D.; Muschick, N.; Beitz, E.; Clement, B.
    Structure-activity relationship of novel and known inhibitors of human dimethylarginine dimethylaminohydrolase-1: alkenyl-amidines as new leads (2008), Bioorg. Med. Chem., 16, 10205-10209.
    View publication on PubMed
Search for more literature for 3.5.3.18

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli BL21 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N5-(but-3-en-1-ylcarbamimidoyl)-L-ornithine 1 mM, 71% inhibition Homo sapiens
N5-(nitrocarbamimidoyl)-L-ornithine 1 mM, 6% inhibition Homo sapiens
N5-(prop-2-en-1-ylcarbamimidoyl)-L-ornithine 1 mM, 70% inhibition Homo sapiens
N5-(prop-2-yn-1-ylcarbamimidoyl)-L-ornithine 1 mM, 83% inhibition Homo sapiens
N5-(propylcarbamimidoyl)-L-ornithine 1 mM, 60% inhibition Homo sapiens
N5-but-3-enimidoyl-L-ornithine 1 mM, 97% inhibition Homo sapiens
N5-butanimidoyl-L-ornithine 1 mM, 78% inhibition Homo sapiens
N5-ethanimidoyl-L-ornithine 1 mM, 24% inhibition Homo sapiens
N5-propanimidoyl-L-ornithine 1 mM, 65% inhibition Homo sapiens
N5-[(2,2,2-trifluoroethyl)carbamimidoyl]-L-ornithine 1 mM, 41% inhibition Homo sapiens
N5-[(2-methoxyethyl)carbamimidoyl]-L-ornithine 1 mM, 89% inhibition Homo sapiens
N5-[(3-amino-3-oxopropyl)carbamimidoyl]-L-ornithine 1 mM, 43% inhibition Homo sapiens
N5-[(3E)-pent-3-enimidoyl]-L-ornithine 1 mM, 73% inhibition Homo sapiens
N5-[imino(morpholin-4-yl)methyl]-L-ornithine 1 mM, 23% inhibition Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.106
-
 N5-(methylcarbamimidoyl)-L-ornithine 37°C, 30 min, pH 7.4 Homo sapiens
0.13
-
 N5-(methoxycarbamimidoyl)-L-ornithine 37°C, 30 min, pH 7.4 Homo sapiens
0.161
-
 N5-[2,5-dihydro-1H-pyrrol-1-yl(imino)methyl]-L-ornithine 37°C, 30 min, pH 7.4 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N5-(methoxycarbamimidoyl)-L-ornithine + H2O assay at 37°C, 30 min, pH 7.4 Homo sapiens L-citrulline + ?
-
 ?
N5-(methylcarbamimidoyl)-L-ornithine + H2O assay at 37°C, 30 min, pH 7.4 Homo sapiens L-citrulline + ?
-
 ?
N5-[2,5-dihydro-1H-pyrrol-1-yl(imino)methyl]-L-ornithine + H2O assay at 37°C, 30 min, pH 7.4 Homo sapiens L-citrulline + ?
-
 ?

Synonyms

Synonyms Comment Organism
human DDAH-1
-
 Homo sapiens
human dimethylarginine dimethylaminohydrolase-1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.002
-
 N5-but-3-enimidoyl-L-ornithine
-
 Homo sapiens
0.013
-
 N5-[(2-methoxyethyl)carbamimidoyl]-L-ornithine
-
 Homo sapiens
0.017
-
 N5-(prop-2-yn-1-ylcarbamimidoyl)-L-ornithine
-
 Homo sapiens
0.032
-
 N5-butanimidoyl-L-ornithine
-
 Homo sapiens
0.036
-
 N5-[(3E)-pent-3-enimidoyl]-L-ornithine
-
 Homo sapiens
0.057
-
 N5-(but-3-en-1-ylcarbamimidoyl)-L-ornithine
-
 Homo sapiens
0.058
-
 N5-(prop-2-en-1-ylcarbamimidoyl)-L-ornithine
-
 Homo sapiens
0.09
-
 N5-(propylcarbamimidoyl)-L-ornithine
-
 Homo sapiens
0.145
-
 N5-propanimidoyl-L-ornithine
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.013
-
-
 Homo sapiens N5-but-3-enimidoyl-L-ornithine
0.029
-
-
 Homo sapiens N5-[(2-methoxyethyl)carbamimidoyl]-L-ornithine
0.055
-
-
 Homo sapiens N5-(prop-2-yn-1-ylcarbamimidoyl)-L-ornithine
0.07
-
-
 Homo sapiens N5-butanimidoyl-L-ornithine
0.079
-
-
 Homo sapiens N5-[(3E)-pent-3-enimidoyl]-L-ornithine
0.189
-
-
 Homo sapiens N5-(but-3-en-1-ylcarbamimidoyl)-L-ornithine
0.207
-
-
 Homo sapiens N5-(prop-2-en-1-ylcarbamimidoyl)-L-ornithine
0.283
-
-
 Homo sapiens N5-(propylcarbamimidoyl)-L-ornithine
0.3
-
-
 Homo sapiens N5-propanimidoyl-L-ornithine