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Literature summary for 1.13.11.52 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
Search for more literature for 1.13.11.52

Cloned(Commentary)

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
indoleamine 2,3-dioxygenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme
-
 Homo sapiens

Ki Value [mM]

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

IC50 Value

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