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Literature summary for 3.4.19.12 extracted from

  • Hirayama, K.; Aoki, S.; Nishikawa, K.; Matsumoto, T.; Wada, K.
    Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening (2007), Bioorg. Med. Chem., 15, 6810-6818.
    View publication on PubMed
Search for more literature for 3.4.19.12

Application

Application Comment Organism
drug development three-step docking (DOCK, rough GOLD, and fine GOLD) and in vitro enzyme assay methods to identify UCH-L3 inhibitors. UCH-L3 inhibitors may be useful for future apoptosis-inducing anti-cancer drug development Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-benzyl-3-hydroxy-4-(5-methyl-2-furoyl)-5-(3-pyridinyl)-1,5-dihydro-2H-pyrrol-2-one is a competitive inhibitor of UCH-L3, significantly inhibits hydrolysis activity of UCH-L3 by 83.2% Homo sapiens
3-hydroxy-5-(4-methoxyphenyl)-1-(1,3,4-thiadiazol-2-yl)-4-(2-thienylcarbonyl)-1,5-dihydro-2H-pyrrol-2-one significantly inhibits hydrolysis activity of UCH-L3 by 76.5% Homo sapiens
3-[4-methyl-5-(([3-(2-thienyl)-1,2,4-oxadiazol-5-yl]methyl)thio)-4H-1,2,4-triazol-3-yl]-1H-indole inhibits hydrolysis activity by 16.2% Homo sapiens
5-(4-fluorophenyl)-3-hydroxy-4-(5-methyl-2-furoyl)-1-(3-pyridinylmethyl)-1,5-dihydro-2H-pyrrol-2-one significantly inhibits hydrolysis activity of UCH-L3 by 76.8% Homo sapiens
iodoacetamide is a non-competitive inhibitor of UCH-L3 Homo sapiens
additional information not inhibited by N1-cyclopropyl-N2-(4-methoxyphenyl)-N2-[(4-methylphenyl)sulfonyl]glycinamide, N-(3-[1-acetyl-5-(2-thienyl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl)ethanesulfonamide, N1-cyclopropyl-N2-[(4-methoxyphenyl)sulfonyl]-N2-(4-methylphenyl)glycinamide, N1-cyclopentyl-N2-(3-methoxyphenyl)-N2-(phenylsulfonyl)glycinamide and 4-(([5-(2-furyl)-4-phenyl-4H-1,2,4-triazol-3-yl]thio)methyl)-1,3-thiazol-2-amine Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0000833
-
 ubiquitin-7-amido-4-methylcoumarin
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ubiquitin-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ubiquitin + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
ubiquitin C-terminal hydrolase-L3
-
 Homo sapiens
UCH-L3
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.103
-
-
 Homo sapiens 1-benzyl-3-hydroxy-4-(5-methyl-2-furoyl)-5-(3-pyridinyl)-1,5-dihydro-2H-pyrrol-2-one
0.123
-
-
 Homo sapiens 5-(4-fluorophenyl)-3-hydroxy-4-(5-methyl-2-furoyl)-1-(3-pyridinylmethyl)-1,5-dihydro-2H-pyrrol-2-one
0.154
-
-
 Homo sapiens 3-hydroxy-5-(4-methoxyphenyl)-1-(1,3,4-thiadiazol-2-yl)-4-(2-thienylcarbonyl)-1,5-dihydro-2H-pyrrol-2-one