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Literature summary extracted from

  • Yue, E.W.; Douty, B.; Wayland, B.; Bower, M.; Liu, X.; Leffet, L.; Wang, Q.; Bowman, K.J.; Hansbury, M.J.; Liu, C.; Wei, M.; Li, Y.; Wynn, R.; Burn, T.C.; Koblish, H.K.; Fridman, J.S.; Metcalf, B.; Scherle, P.A.; Combs, A.P.
    Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model (2009), J. Med. Chem., 52, 7364-7367.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.13.11.52 N-terminal His tag, expressed in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.11.52 1-Methyltryptophan
-
 Homo sapiens
1.13.11.52 4-amino-1,2,5-oxadiazole-3-carboximidamide competitive Homo sapiens
1.13.11.52 4-amino-N'-hydroxy-N-(3-isopropylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N'-hydroxy-N-(3-methoxyphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N'-hydroxy-N-(3-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N'-hydroxy-N-phenyl-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(2-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-bromophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-chlorophenyl)-1,2,5-oxadiazole-3-carbohydrazonamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-ethylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(3-tert-butylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 4-amino-N-(4-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.13.11.52 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.13.11.52
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.11.52 L-tryptophan + O2
-
 Homo sapiens N-formylkynurenine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.13.11.52 indoleamine 2,3-dioxygenase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.13.11.52 heme
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.13.11.52 0.0015
-
 4-amino-1,2,5-oxadiazole-3-carboximidamide
-
 Homo sapiens
1.13.11.52 0.034
-
 1-Methyltryptophan
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.11.52 0.000059
-
-
 Homo sapiens 4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.000067
-
-
 Homo sapiens 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.000073
-
-
 Homo sapiens 4-amino-N-(3-bromophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.000086
-
-
 Homo sapiens 4-amino-N-(3-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.00043
-
-
 Homo sapiens 4-amino-N-(3-ethylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.0005
-
-
 Homo sapiens 4-amino-N-(3-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.00055
-
-
 Homo sapiens 4-amino-N'-hydroxy-N-(3-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.0014
-
-
 Homo sapiens 4-amino-N-(3-chlorophenyl)-1,2,5-oxadiazole-3-carbohydrazonamide
1.13.11.52 0.0021
-
-
 Homo sapiens 4-amino-N'-hydroxy-N-(3-isopropylphenyl)-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.0032
-
-
 Homo sapiens 4-amino-N'-hydroxy-N-phenyl-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.0044
-
-
 Homo sapiens 4-amino-N'-hydroxy-N-(3-methoxyphenyl)-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.006
-
-
 Homo sapiens 4-amino-N-(4-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.0065
-
-
 Homo sapiens 4-amino-N-(2-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1.13.11.52 0.025
-
-
 Homo sapiens 4-amino-N-(3-tert-butylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide