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Literature summary for 1.13.11.52 extracted from

  • Roehrig, U.F.; Awad, L.; Grosdidier, A.; Larrieu, P.; Stroobant, V.; Colau, D.; Cerundolo, V.; Simpson, A.J.; Vogel, P.; Van den Eynde, B.J.; Zoete, V.; Michielin, O.
    Rational design of indoleamine 2,3-dioxygenase inhibitors (2010), J. Med. Chem., 53, 1172-1189.
    View publication on PubMed
Search for more literature for 1.13.11.52

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 AI cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3-hydroxyphenyl)(phenyl)methanone
-
 Homo sapiens
(4E,4'E)-4,4'-bis(isopropylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
-
 Homo sapiens
(4E,4'E)-4,4'-bis(pentan-3-ylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
-
 Homo sapiens
(E)-4-(isopropylimino)-2-methylnaphthalen-1(4H)-one
-
 Homo sapiens
(R)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
-
 Homo sapiens
(S)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
-
 Homo sapiens
1-(1,3-benzothiazol-2-ylsulfanyl)-N,N-dimethylmethanamine
-
 Homo sapiens
1-methyl-L-tryptophan
-
 Homo sapiens
2-amino-3-hydroxy-N-(4-hydroxynaphthalen-1-yl)propanamide
-
 Homo sapiens
2-amino-N-(4-hydroxynaphth-1-yl)acetamide
-
 Homo sapiens
2-mercaptobenzothiazole
-
 Homo sapiens
2-phenoxyaniline
-
 Homo sapiens
3-(1H-1,2,3-triazol-5-yl)pyridine
-
 Homo sapiens
4-(1H-1,2,3-triazol-5-yl)pyridine
-
 Homo sapiens
4-(2-(diethylamino)ethylamino)-1-naphthol
-
 Homo sapiens
4-(2-hydroxyethoxy)-1-naphthol
-
 Homo sapiens
4-(benzylamino)-1-naphthol
-
 Homo sapiens
4-(cyclohexylamino)-1-naphthol
-
 Homo sapiens
4-(dimethylamino)naphthalen-1-ol
-
 Homo sapiens
4-(ethylamino)-1-naphthol
-
 Homo sapiens
4-(isobutylamino)-1-naphthol
-
 Homo sapiens
4-(isopropylamino)-1-naphthol
-
 Homo sapiens
4-(methylamino)naphthalen-1-ol
-
 Homo sapiens
4-(pent-3-ylamino)-1-naphthol
-
 Homo sapiens
4-(propylamino)-1-naphthol
-
 Homo sapiens
4-(tert-butylamino)naphthalen-1-ol
-
 Homo sapiens
4-amino-1-naphthol
-
 Homo sapiens
4-hydroxycarbazole
-
 Homo sapiens
4-methoxy-1-naphthylamine
-
 Homo sapiens
4-phenyl-1,3-thiazol-2-amine
-
 Homo sapiens
4-phenyl-1,3-thiazole-2-thiol
-
 Homo sapiens
5-(ethylamino)quinolin-8-ol
-
 Homo sapiens
5-(isopropylamino)quinolin-8-ol
-
 Homo sapiens
5-amino-8-hydroxyquinoline
-
 Homo sapiens
5-chloro-1,3-benzothiazole-2(3H)-thione
-
 Homo sapiens
5-phenyl-1H-1,2,3-triazole
-
 Homo sapiens
9-fluorenone
-
 Homo sapiens
9-hydroxyfluorene
-
 Homo sapiens
annulin B
-
 Homo sapiens
benzophenone
-
 Homo sapiens
brassinin
-
 Homo sapiens
Dichlorophene
-
 Homo sapiens
exiguamine A
-
 Homo sapiens
additional information not inhibited by 1-methyl-D-tryptophan Homo sapiens
N,N-dimethyl-1-[(4-phenyl-1,3-thiazol-2-yl)sulfanyl]methanamine
-
 Homo sapiens
N-(4-hydroxy-1-naphthyl)ethane-1,2-diaminium chloride
-
 Homo sapiens
N-(4-hydroxy-1-naphthyl)propane-1,3-diaminium chloride
-
 Homo sapiens
N-(4-hydroxynaphthalen-1-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
N-phenyl-p-phenylenediamine
-
 Homo sapiens
naphthalene-1,4-diol
-
 Homo sapiens
primaquine
-
 Homo sapiens
quinolin-8-ol
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
D-tryptophan + O2 Homo sapiens
-
 N-formyl-D-kynurenine
-
 ?
L-tryptophan + O2 Homo sapiens
-
 N-formyl-L-kynurenine
-
 ?
serotonin + O2 Homo sapiens
-
 ?
-
 ?
tryptamine + O2 Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P14902
-
-

Purification (Commentary)

Purification (Comment) Organism
IMAC nickel affinity column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-tryptophan + O2
-
 Homo sapiens N-formyl-D-kynurenine
-
 ?
L-tryptophan + O2
-
 Homo sapiens N-formyl-L-kynurenine
-
 ?
serotonin + O2
-
 Homo sapiens ?
-
 ?
tryptamine + O2
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
IDO
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
heme
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0002
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (E)-4-(isopropylimino)-2-methylnaphthalen-1(4H)-one
0.00045
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (4E,4'E)-4,4'-bis(isopropylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
0.00052
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (4E,4'E)-4,4'-bis(pentan-3-ylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
0.0015
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens naphthalene-1,4-diol
0.0025
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(isopropylamino)-1-naphthol
0.0025
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(benzylamino)-1-naphthol
0.003
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-amino-1-naphthol
0.003
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 5-amino-8-hydroxyquinoline
0.003
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(2-(diethylamino)ethylamino)-1-naphthol
0.0035
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(pent-3-ylamino)-1-naphthol
0.004
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(tert-butylamino)naphthalen-1-ol
0.0045
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(propylamino)-1-naphthol
0.005
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(1H-1,2,3-triazol-5-yl)pyridine
0.005
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens N-(4-hydroxy-1-naphthyl)propane-1,3-diaminium chloride
0.0055
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-methoxy-1-naphthylamine
0.0125
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(methylamino)naphthalen-1-ol
0.0125
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(2-hydroxyethoxy)-1-naphthol
0.015
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 5-(isopropylamino)quinolin-8-ol
0.015
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(cyclohexylamino)-1-naphthol
0.016
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(ethylamino)-1-naphthol
0.025
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(isobutylamino)-1-naphthol
0.04
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 5-(ethylamino)quinolin-8-ol
0.044
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens N-(4-hydroxy-1-naphthyl)ethane-1,2-diaminium chloride
0.05
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens primaquine
0.05
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 2-mercaptobenzothiazole
0.05
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 5-chloro-1,3-benzothiazole-2(3H)-thione
0.05
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 1-(1,3-benzothiazol-2-ylsulfanyl)-N,N-dimethylmethanamine
0.05
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-phenyl-1,3-thiazole-2-thiol
0.06
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 5-phenyl-1H-1,2,3-triazole
0.06
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (S)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
0.07
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens Dichlorophene
0.09
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (R)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
0.105
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 2-amino-N-(4-hydroxynaphth-1-yl)acetamide
0.2
-
 IC50 above 0.2 mM, in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 9-fluorenone
0.2
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens N-(4-hydroxynaphthalen-1-yl)pyrrolidine-2-carboxamide
0.4
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens N-phenyl-p-phenylenediamine
0.4
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 2-amino-3-hydroxy-N-(4-hydroxynaphthalen-1-yl)propanamide
0.4
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-hydroxycarbazole
0.5
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens (3-hydroxyphenyl)(phenyl)methanone
0.68
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 3-(1H-1,2,3-triazol-5-yl)pyridine
0.75
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens quinolin-8-ol
1
-
 IC50 above 1.0 mM, in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 9-hydroxyfluorene
1
-
 IC50 above 1.0 mM, in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens N,N-dimethyl-1-[(4-phenyl-1,3-thiazol-2-yl)sulfanyl]methanamine
1
-
 IC50 above 1.0 mM, in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 2-phenoxyaniline
1
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens benzophenone
1
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-phenyl-1,3-thiazol-2-amine
1
-
 in potassium phosphate buffer (100 mM, pH 6.5) ascorbic acid (20 mM), catalase (200 units/ml), methylene blue (0.01 mM), at 37°C Homo sapiens 4-(dimethylamino)naphthalen-1-ol

General Information

General Information Comment Organism
metabolism IDO catalyzes the initial and rate-limiting step in the catabolism of tryptophan along the kynurenine pathway Homo sapiens