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1-benzofuran-DL-tryptophan + O2
?
-
1 mM, 22% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
1-benzothiophene-DL-tryptophan + O2
?
-
1 mM, 19% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
1-methyl-D-tryptophan + O2
N-methyl-N-formyl-D-kynurenine
-
-
-
?
1-methyl-DL-tryptophan + O2
?
-
1 mM, 7% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
1-methyl-L-tryptophan + O2
?
-
-
-
-
?
1-methyl-L-tryptophan + O2
N-methyl-N-formyl-L-kynurenine
1H-indole + H2O + O2
2,3-dihydro-1H-indole-2,3-diol
-
-
-
-
?
2-bromo-L-tryptophan + O2
?
-
1 mM, 21% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
2-chloro-L-tryptophan + O2
?
-
1 mM, 33% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
2-hydroxy-L-tryptophan + O2
?
-
1 mM, 4% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
3-indoleethanol + O2-
?
-
-
-
-
?
4-methyl-DL-tryptophan + O2
?
-
1 mM, 33% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-benzyloxy-DL-tryptophan + O2
?
-
1 mM, 1% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-bromo-DL-tryptophan + O2
?
-
1 mM, 36% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-fluoro-DL-tryptophan + O2
5-fluoro-N-formyl-DL-kynurenine
-
-
-
?
5-fluoro-DL-tryptophan + O2
?
5-fluoro-L-tryptophan + O2
5-fluoro-N-formyl-L-kynurenine
-
-
-
?
5-fluoro-tryptophan + O2
4-(2-amino-5-fluorophenyl)-2-(formylamino)-4-oxobutanoic acid
-
-
-
?
5-fluoro-tryptophan + O2
?
-
-
-
?
5-fluorotryptophan + O2
?
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
(2S)-4-(2-amino-5-hydroxyphenyl)-2-(formylamino)-4-oxobutanoic acid
5-hydroxy-L-tryptophan + O2
5-hydroxy-N-formyl-L-kynurenine
5-hydroxy-L-tryptophan + O2
?
5-hydroxy-L-tryptophan + O2
N-formyl-5-hydroxy-L-kynurenine
5-hydroxy-tryptophan + O2
4-(2-amino-5-hydroxyphenyl)-2-(formylamino)-4-oxobutanoic acid
-
-
-
?
5-hydroxytryptamine + O2
?
-
-
-
-
?
5-hydroxytryptophan + O2
?
-
-
-
-
?
5-hydroxytryptophan + O2-
N-formyl-5-hydroxykynurenine
-
-
-
-
?
5-methoxy-D,L-tryptophan + O2
?
-
1 mM, 70% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-methoxy-DL-tryptophan + O2
5-methoxy-N-formyl-DL-kynurenine
-
-
-
?
5-methoxy-L-tryptophan + O2
5-methoxy-N-formyl-L-kynurenine
-
-
-
?
5-methyl-D,L-tryptophan + O2
?
-
1 mM, 123% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-methyl-DL-tryptophan + O2
5-methyl-N-formyl-DL-kynurenine
5-methyl-DL-tryptophan + O2
?
-
-
-
?
5-methyl-tryptophan + O2
4-(2-amino-5-methylphenyl)-2-(formylamino)-4-oxobutanoic acid
-
-
-
?
5-methyltryptophan + O2
?
-
-
-
-
?
6-fluoro-DL-tryptophan + O2
?
6-fluorotryptophan + O2
?
-
-
-
-
?
6-methyl-DL-tryptophan + O2
6-methyl-N-formyl-DL-kynurenine
-
-
-
?
6-methyl-DL-tryptophan + O2
?
6-nitro-L-tryptophan + O2
?
-
1 mM, 2% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
7-methyl-DL-tryptophan + O2
?
-
1 mM, 18% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
alpha-methyl-DL-tryptophan + O2
?
-
1 mM, 35% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
alpha-methyl-DL-tryptophan + O2-
?
-
-
-
-
?
alpha-N-methyl-L-tryptophan + O2
?
-
1 mM, 21% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
beta-methyl-DL-tryptophan + O2
?
-
1 mM, 32% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
beta-[3-benzo(b)thienyl]-L-alanine + O2
?
-
-
-
?
D-5-hydroxytryptophan + O2
?
D-Trp + O2
D-formylkynurenine
D-Trp + O2
N-formyl-D-kynurenine
D-tryptophan + O2
?
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
DL-5-fluoro-methyltryptophan + O2
?
DL-5-methyltryptophan + O2
?
DL-6-fluorotryptophan + O2
?
DL-alpha-methyltryptophan + O2
alpha-methyl-N-formyl-DL-kynurenine
-
9.0% of the activity with L-Trp
-
-
?
indole-3-propionic acid + O2
?
altered kinetics for IPA (very long lag phase) as being consistent with a role for the ammonium group in stabilizing the ferric superoxide complex (via the radical pathway). The rate-limiting steps are different from the other substrates examined so that Compound II does not accumulate, but product formation is still possible, product formation ananlysis by LC-MS
-
-
?
L-5-hydroxytryptophan + O2
?
L-Trp + O2
L-formylkynurenine
L-Trp + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
L-tryptophan + O2
N-formylkynurenine
L-tryptophan + O2-
N-formyl-L-kynurenine
L-tryptophan ethyl ester + O2
?
-
1 mM, 14% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
L-tryptophan methyl ester + O2
?
-
1 mM, 15% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
N-acetyl-L-tryptophan + O2
?
-
1 mM, 3% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
serotonin + O2-
?
-
-
-
-
?
Trp + O2
formylkynurenine
-
-
-
-
?
tryptamine + O2-
?
-
-
-
-
?
tryptophan + O2
N-formylkynurenine
-
if the cellular environment protects indoleamine 2,3-dioxygenase from oxidation to the ferric form, no additional electron donor might by required for indolamine 2,3-dioxygenase activity in intact tissues
-
-
?
additional information
?
-
1-methyl-L-tryptophan + O2
N-methyl-N-formyl-L-kynurenine
-
-
-
?
1-methyl-L-tryptophan + O2
N-methyl-N-formyl-L-kynurenine
-
-
-
?
5-fluoro-DL-tryptophan + O2
?
-
1 mM, 46% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-fluoro-DL-tryptophan + O2
?
-
-
-
?
5-fluoro-DL-tryptophan + O2
?
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
(2S)-4-(2-amino-5-hydroxyphenyl)-2-(formylamino)-4-oxobutanoic acid
-
-
-
?
5-hydroxy-L-tryptophan + O2
(2S)-4-(2-amino-5-hydroxyphenyl)-2-(formylamino)-4-oxobutanoic acid
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
5-hydroxy-N-formyl-L-kynurenine
-
-
-
?
5-hydroxy-L-tryptophan + O2
5-hydroxy-N-formyl-L-kynurenine
-
-
-
?
5-hydroxy-L-tryptophan + O2
?
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
?
-
1 mM, 59% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
5-hydroxy-L-tryptophan + O2
N-formyl-5-hydroxy-L-kynurenine
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
N-formyl-5-hydroxy-L-kynurenine
-
-
-
-
?
5-hydroxy-L-tryptophan + O2
N-formyl-5-hydroxy-L-kynurenine
-
-
-
-
?
5-methyl-DL-tryptophan + O2
5-methyl-N-formyl-DL-kynurenine
-
-
-
?
5-methyl-DL-tryptophan + O2
5-methyl-N-formyl-DL-kynurenine
-
-
-
?
5-methyl-DL-tryptophan + O2
5-methyl-N-formyl-DL-kynurenine
high activity
-
-
?
6-fluoro-DL-tryptophan + O2
?
-
1 mM, 38% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
6-fluoro-DL-tryptophan + O2
?
-
-
-
?
6-fluoro-DL-tryptophan + O2
?
-
-
-
-
?
6-methyl-DL-tryptophan + O2
?
-
1 mM, 72% activity relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
-
-
?
6-methyl-DL-tryptophan + O2
?
-
-
-
?
D-5-hydroxytryptophan + O2
?
-
-
-
-
?
D-5-hydroxytryptophan + O2
?
-
enzyme from lung
-
-
?
D-Trp + O2
D-formylkynurenine
-
-
-
-
?
D-Trp + O2
D-formylkynurenine
-
-
-
?
D-Trp + O2
D-formylkynurenine
-
-
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
enzyme from brain
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-Trp + O2
N-formyl-D-kynurenine
-
0.7% of the activity with L-Trp
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
low activity
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
the initial deprotonation reaction of the indole NH group in hTDO is carried out by the evolutionarily conserved distal His. stereospecificity of hTDO is determined by the efficiency of the dioxygen chemistry
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
IDO displays a similar kcat for D- and L-tryptophan, but D-tryptophan has 173folds higher Km
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
L-Trp is a better substrate for IDO than D-Trp
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
IDO1
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
D-Trp is a substrate of hIDO1 but has very low affinity
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
ir
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
ir
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
IDO1
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
O2- binds first to the ferric enzyme and is followed by rapid binding of L-tryptophan
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
-
-
-
?
D-tryptophan + O2
N-formyl-D-kynurenine
while L and D-tryptophan have similar affinities (Km values), the kcat is 10times lower for D-tryptophan
-
-
?
DL-5-fluoro-methyltryptophan + O2
?
-
35% of the activity with L-Trp
-
-
?
DL-5-fluoro-methyltryptophan + O2
?
-
30.6% of the activity with L-Trp
-
-
?
DL-5-methyltryptophan + O2
?
-
90% of the activity with L-Trp
-
-
?
DL-5-methyltryptophan + O2
?
-
15.1% of the activity with L-Trp
-
-
?
DL-6-fluorotryptophan + O2
?
-
90% of the activity with L-Trp
-
-
?
DL-6-fluorotryptophan + O2
?
-
-
-
-
?
DL-6-fluorotryptophan + O2
?
-
-
-
-
?
DL-6-methyltryptophan
?
-
98% of the activity with L-Trp
-
-
?
DL-6-methyltryptophan
?
-
-
-
-
?
indole + O2
?
-
-
-
-
?
L-5-hydroxytryptophan + O2
?
-
-
-
-
?
L-5-hydroxytryptophan + O2
?
-
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
regulation of enzyme activity
-
-
?
L-Trp + O2
L-formylkynurenine
during larval life the enzyme controls the level of potentially harmful free Trp in the hemolymph by converting it to kynurenine, and during adult development the enzyme catalyzes the first step of brown eye pigment biosynthesis
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
Frog
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
lipopolysaccharide and muramyl tripeptide upregulate enzyme induction through a mechanism independent of interleukin 1alpha
-
-
?
L-Trp + O2
L-formylkynurenine
-
interleukin-4 inhibits expression of the enzyme in monocytes
-
-
?
L-Trp + O2
L-formylkynurenine
-
initial enzyme of tryptophan degradation pathway
-
-
?
L-Trp + O2
L-formylkynurenine
induction by interferongamma
-
-
?
L-Trp + O2
L-formylkynurenine
-
activity is increased in important biological processes, such as protection of the fetus from rejection during pregnancy and possibly T cell death in HIV-infected patients
-
-
?
L-Trp + O2
L-formylkynurenine
-
Trp degradation by the enzyme regulates lymphocyte proliferation
-
-
?
L-Trp + O2
L-formylkynurenine
rate-limiting enzyme in the catabolism of tryptophan
-
-
?
L-Trp + O2
L-formylkynurenine
-
IDO is the first enzyme in UV-filter pathway. UV-filter biosynthesis is active even in aged lenses
-
-
?
L-Trp + O2
L-formylkynurenine
-
the enzyme inhibits tumor cell proliferation by tryptophan depletion. IDO-induced suppression of antitumoral immune response in both adenocarcinoma and squamous cell carcinoma
-
-
?
L-Trp + O2
L-formylkynurenine
-
proposed reaction mechanism involves the proton abstraction by iron-bound dixoygen. The O-O bond is precisely controlled by the heme proximal and distal environment and is not cleaved before the incorporation of both oxygen atoms into the substrate
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
indoleamine 2,3-dioxygenase has almost no detectable activity at or below 0.1 mM oxygen and maximum activity at about 1.15 mM
-
?
L-Trp + O2
L-formylkynurenine
-
indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase catalyze the rate-limiting step in the kynurenine pathway from Trp to quinolinic acid
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
induction by interferongamma
-
-
?
L-Trp + O2
L-formylkynurenine
-
enzyme contributes to tumor cell evasion of T cell-mediated rejection
-
-
?
L-Trp + O2
L-formylkynurenine
-
expression of indoleamine 2,3-dioxygenase is an inducible feature of specific subsets of dendritic cells, and provides a potential mechanistic explanation for their T cell regulatory properties
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
enzyme from liver is specific for L-Trp, the enzyme from brain is active with L-Trp and D-Trp, the enzyme from lung is active with L-Trp and D-5-hydroxytryptophan
-
?
L-Trp + O2
L-formylkynurenine
-
superoxide anion is required for the initiation of the reaction and the maintenance of the catalytic cycle during the steady state
-
?
L-Trp + O2
L-formylkynurenine
-
tryptophan-derived catabolites are responsible for inhibition of T cell and natural killer cell proliferation induced by indoleamine 2,3-dioxygenase
-
-
?
L-Trp + O2
L-formylkynurenine
-
regulatory control
-
-
?
L-Trp + O2
L-formylkynurenine
-
a dramatic and specific induction of the pulmonary enzyme by virus and lipopolysaccharide is mediated by interferon. The enzyme may play an important role in the inflammatory processes, immune responses, and/or the mode of action of interferon
-
-
?
L-Trp + O2
L-formylkynurenine
-
influenza virus infection and tumor transplantation induce the enzyme
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
absolutely specific for L-Trp
-
?
L-Trp + O2
L-formylkynurenine
-
absolutely specific for L-Trp
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
regulatory control
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
enzyme from liver is specific for
-
?
L-Trp + O2
L-formylkynurenine
-
tryptophan 2,3-dioxygenase activity is appreciable even at 0.03 mM oxygen and rises steeply to a maximum at 0.04 mM
-
?
L-Trp + O2
L-formylkynurenine
-
regulation of enzyme activity
-
-
?
L-Trp + O2
L-formylkynurenine
-
indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase catalyze the rate-limiting step in the kynurenine pathway from Trp to quinolinic acid
-
-
?
L-Trp + O2
L-formylkynurenine
-
enzyme controls the physiological flux of Trp into both the serotonergic and kynureninic pathways
-
-
?
L-Trp + O2
L-formylkynurenine
-
key enzyme of tryptophan catabolism, importance as regulator of whole-body tryptophan catabolism and brain levels of tryptophan and serotonin
-
-
?
L-Trp + O2
L-formylkynurenine
-
the skin enzyme may play an important role in the initiation or suppression of rat hair growth
-
-
?
L-Trp + O2
L-formylkynurenine
-
regulatory control
-
-
?
L-Trp + O2
L-formylkynurenine
-
key regulatory enzyme, though irreversible degradation, controls the flux of tryptophan through physiologically relevant pathways
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-Trp + O2
L-formylkynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
tryptophan indirectly activates TDO through promoting the production of reactive oxygen species
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
tryptophan 2,3-dioxygenase is the only enzyme able to initiate L-tryptophan degradation through the kynurenine pathway
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
Glu132 in Blepharisma IDO-III is crucial for its high affinity for L-Trp. No activity with 5-hydroxy-L-tryptophan
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
no activity with 5-hydroxy-L-tryptophan
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
ir
L-tryptophan + O2
N-formyl-L-kynurenine
-
the enzyme is involved in tryptophan catabolism and in quinolinate biosynthesis
-
-
ir
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
enzyme shows induced-fit mechanism to bind L-Trp, two conserved but flexible loops undergo conformational changes, converting the active site from an open conformation to a closed conformation, key residues involved in recognition and binding of the heme and the substrate, Molecular modeling and dynamics simulation, overview
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
395463, 395469, 395472, 657496, 659233, 660498, 663910, 664443, 665164, 666239, 666378, 666763, 666895, 671990, 685239 -
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
687116, 687297, 687590, 696151, 700405, 711247, 711422, 711580, 711776, 711952, 712112, 712172, 712173, 712230, 712250, 712647, 712820, 712832, 712945, 712947, 713489, 724912 -
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
no activity with D-tryptophan
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
plays an important role in the immune response by catalyzing the oxidative degradation of L-tryptophan that contributes to immune suppression and tolerance
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
the initial deprotonation reaction of the indole NH group in hTDO is carried out by the evolutionarily conserved distal His. stereospecificity of hTDO is determined by the efficiency of the dioxygen chemistry
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
IDO displays a similar kcat for D- and L-tryptophan, but D-tryptophan has 173folds higher Km
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
L-Trp is a better substrate for IDO than D-Trp
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
human TDO displays a major specificity towards L-Trp, structural role of T342 in controlling the substrate stereoselectivity of the enzyme
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
IDO1 and IDO2
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
highly preferred substrate, T342 plays a pivotal role in controlling the substrate stereoselectivity of hTDO
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
the enzyme has broad substrate specificity for various indoleamines such as L-tryptophan and serotonin. It catalyzes the oxidation of the pyrrole ring of tryptophan to form N-formylkynurenine, which is later metabolized to formic acid and kynurenine
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
the reaction involves cleavage of the C2=C3 double bond in the Trp indole ring and insertion of two atomic oxygens from the iron-bound O2 into the indole 2 and 3 position
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
no activity with oxygen concentrations below 0.1 mM, maximum activity at 1.15 mM oxygen
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
ir
L-tryptophan + O2
N-formyl-L-kynurenine
-
first step during biosynthesis of 3-hydroxyquinaldic acid
-
-
ir
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
ir
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
663820, 663910, 665204, 665457, 666461, 666895, 684391, 686721, 687116, 710831, 711165, 712112, 712152, 712821, 713412, 713448, 713586 -
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
IDO represents an important immune regulatory enzyme under diverse physiological and pathological conditions in vivo and is of considerable medical importance
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
indoleamine 2,3-dioxygenase is a rate-limiting enzyme in the L-tryptophan-kynurenine pathway. IFN-gamma-induced expression of IDO expression is inhibited only by JAK inhibitor I. Lipopolysaccharide-induced expression of indoleamine 2,3-dioxygenase is inhibited by LY294002 and SP600125 but not by JAK inhibitor I, SB203580, or U0126. LPS can induce the expression of indoleamine 2,3-dioxygenase via an IFN-gamma-independent mechanism and PI3 kinase and JNK in the LPS-induced pathway leading to IDO expression
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
IDO1 and IDO2
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
the enzyme has broad substrate specificity for various indoleamines such as L-tryptophan and serotonin. It catalyzes the oxidation of the pyrrole ring of tryptophan to form N-formylkynurenine, which is later metabolized to formic acid and kynurenine
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
higher affinity at alkaline pH than at acidic pH
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
the enzyme is involved in the catabolic pathway of L-tryptophan degradation, overview
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
D-tryptophan is no substrate
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
no activity with oxygen concentrations below 0.1 mM, maximum activity at 1.15 mM oxygen
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
rate-limiting enzyme in L-tryptophan catabolism and thus a key serotonergic determinant
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
while L and D-tryptophan have similar affinities (Km values), the kcat is 10times lower for D-tryptophan
-
-
?
L-tryptophan + O2
N-formyl-L-kynurenine
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
?
L-tryptophan + O2
N-formylkynurenine
-
-
-
-
?
L-tryptophan + O2-
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2-
N-formyl-L-kynurenine
-
-
-
-
?
L-tryptophan + O2-
N-formyl-L-kynurenine
-
-
-
-
?
serotonin + O2
?
-
-
-
-
?
serotonin + O2
?
-
-
-
-
?
serotonin + O2
?
-
-
-
-
?
serotonin + O2
?
-
-
-
-
?
tryptamine + O2
?
-
-
-
-
?
tryptamine + O2
?
-
-
-
?
tryptamine + O2
?
-
-
-
-
?
additional information
?
-
-
first and rate-limiting enzyme in tryptophan metabolism
-
-
?
additional information
?
-
-
first enzyme of the kynurenine pathway of tryptophan metabolism
-
-
?
additional information
?
-
-
in the placenta, inhibition of the enzyme leads to spontaneous abortion. By catabolizing extracellular tryptophan the enzyme inhibits local T cell proliferation thereby preventing placental rejection. This mechanism can also be active in suppressing inflammatory responses in the central neurvous system, where inflammation must be tightly regulated to prevent the loss of irreplaceable neurons. Local expression of the enzyme during inflammation is a self-protection mechanism which limits antigen-specific immune responses in the central nervous system
-
-
?
additional information
?
-
-
Langerhans cells possess an immunoregulatory function in promoting T cell tolerance by production of IDO
-
-
?
additional information
?
-
the oxidative metabolism of melatonin is due, in presence of H2O2, to the activities of both myeloperoxidase, EC 1.11.1.7 and indolemanine 2,3-dioxygenase
-
-
?
additional information
?
-
-
the enzyme plays an important physiological role in the defense mechanism against a variety of infectious pathogens, in the regulation of T-cell function by macrophages and a subset of dendritic cells, and in the synthesis of UV filters in human lenses. Serious problems arise from the unregulated over-expression of the enzyme, which often results in a deleterious systemic Trp depletion and/or the accumulation of neurotoxin, quinolinic acidn the brain. Enzyme expression in malignant tumors helps them to avoid the immune surveillance through a local Trp depletion. The kynurenilation of the lens protein with UV filters thus appears to be the major cause of age-related cataract
-
-
?
additional information
?
-
-
the IDO enzyme is involved in the immune regulation of early atherosclerosis, particularly in young female adults
-
-
?
additional information
?
-
docking calculations and spatial coarse graining simulations are used to determine the molecular basis of substrate recognition, enhancer binding and conformational transitions of IDO in response to these events
-
-
?
additional information
?
-
-
no activity with tryptophanol, indole-3-propionic acid, tryptamine, N-methyl-Trp
-
-
?
additional information
?
-
no activity with tryptophanol, indole-3-propionic acid, tryptamine, N-methyl-Trp
-
-
?
additional information
?
-
-
the enzyme acts as a heme peroxidase that, in the absence of substrates, self-inactivates dioxygenase activity via compound I-initiated protein oxidation. L-Trp protects against dioxygenase inactivation by reacting with compound I and retarding compound II reduction to suppress peroxidase turnover. Catalytic cycle of hemeperoxidase enzymes, and enzyme peroxidase mechanism, overview
-
-
?
additional information
?
-
-
the enzyme catalyzes the oxidation of indole by H2O2, with generation of 2- and 3-oxoindole as the major products, in the absence of O2 and reducing agents and is not inhibited by superoxide dismutase or hydroxyl radical scavengers, although it is strongly inhibited by L-Trp. IDO inserts oxygen into indole in a reaction that is mechanistically analogous to the peroxide shunt pathway of cytochrome P450
-
-
?
additional information
?
-
formation of ferrous-oxy hIDO and comparison with the ternary complex, overview
-
-
?
additional information
?
-
substrate specificity, overview. Replacement of the 5-methoxy group by a methyl group has a negative influence in the binding of the molecule, decreasing its affinity threefold. 5-HO-L-Trp and melatonin are no substrates for IDO2
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additional information
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substrate specificity, overview. Replacement of the 5-methoxy group by a methyl group has a negative influence in the binding of the molecule, decreasing its affinity threefold. 5-HO-L-Trp and melatonin are no substrates for IDO2
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additional information
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substrate specificity, overview. Replacement of the 5-methoxy group by a methyl group has a negative influence in the binding of the molecule, decreasing its affinity threefold. 5-HO-L-Trp and melatonin are no substrates for IDO2
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additional information
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the heme enzyme catalyzes the oxidative cleavage of the Ltryptophan indole ring
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additional information
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the heme enzyme catalyzes the oxidative cleavage of the Ltryptophan indole ring
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additional information
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using a cytochrome b5-based activating system, the initial rates of O2 decay with a Clark-type oxygen electrode at physiologically-relevant levels of both substrates are measured. Kinetics are also studied in the presence of two inhibitory substrate analogues: 1-methyl L-tryptophan and norharmane. Quantitative analysis supports a steady-state rather than a rapid equilibrium kinetic mechanism, where the rates of individual pathways, leading to a ternary complex, are significantly different, and the overall rate of catalysis depends on contributions of both routes. One path, where O2 binds to ferrous hIDO1 first, is faster than the second route, which starts with the binding of L-Trp. L-Trp complexation with free ferrous hIDO1 is more rapid than that of O2. As the level of L-Trp increases, the slower route becomes a significant contributor to the overall rate, resulting in observed substrate inhibition. When 1-Me-L-Trp is the only indoleamine in the reaction mixture, it is a very slow substrate for hIDO1
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additional information
?
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using a cytochrome b5-based activating system, the initial rates of O2 decay with a Clark-type oxygen electrode at physiologically-relevant levels of both substrates are measured. Kinetics are also studied in the presence of two inhibitory substrate analogues: 1-methyl L-tryptophan and norharmane. Quantitative analysis supports a steady-state rather than a rapid equilibrium kinetic mechanism, where the rates of individual pathways, leading to a ternary complex, are significantly different, and the overall rate of catalysis depends on contributions of both routes. One path, where O2 binds to ferrous hIDO1 first, is faster than the second route, which starts with the binding of L-Trp. L-Trp complexation with free ferrous hIDO1 is more rapid than that of O2. As the level of L-Trp increases, the slower route becomes a significant contributor to the overall rate, resulting in observed substrate inhibition. When 1-Me-L-Trp is the only indoleamine in the reaction mixture, it is a very slow substrate for hIDO1
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additional information
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TioF is completely inactive towards tryptamine, 5-hydroxy-L-Trp, and indole propionic acid
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additional information
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TioF is completely inactive towards tryptamine, 5-hydroxy-L-Trp, and indole propionic acid
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additional information
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IDO2 enzyme may be involved in immune evasion by tumours
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additional information
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IDO2 enzyme may be involved in immune evasion by tumours
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additional information
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Trp suppresses 2,3-dioxygenase induction by IFN-gamma at the transcriptional level
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additional information
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Trp suppresses 2,3-dioxygenase induction by IFN-gamma at the transcriptional level
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additional information
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although the kcat of indoleamine-2,3-dioxygenase (IDO) is similar for D-Trp and L-Trp, the Km of IDO is approximately 170fold higher for L-Trp than that for D-Trp
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additional information
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although the kcat of indoleamine-2,3-dioxygenase (IDO) is similar for D-Trp and L-Trp, the Km of IDO is approximately 170fold higher for L-Trp than that for D-Trp
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additional information
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in the presence of guaiacol or potassium iodide the enzyme degrades H2O2
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additional information
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not active with indoleacetic acid and skatole
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additional information
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no activity with D-Trp and indolepropionic acid
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additional information
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no activity with D-Trp and indolepropionic acid
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additional information
additional information
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no activity with D-Trp
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additional information
additional information
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no activity with D-Trp
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(-)-kurarinone
non-competitive inhibitor
-
(10Z,13Z)-nonadecadienoic acid
-
32% inhibition at 0.02 mM
(11Z,14Z)-eicosadienoic acid
-
42% inhibition at 0.02 mM
(11Z,14Z,17Z)-eisosatrienoic acid
-
19% inhibition at 0.02 mM
(12Z,15Z)-heneicosadienoic acid
-
39% inhibition at 0.02 mM
(13Z,16Z)-docosadienoic acid
-
39% inhibition at 0.02 mM
(13Z,16Z,19Z)-docosatrienoic acid
-
52% inhibition at 0.02 mM
(1R,2S)-2-([[6-(trifluoromethyl)-1H-indazol-4-yl]amino]methyl)cyclohexan-1-ol
-
-
(1R,2S)-2-[[(5-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
(1R,2S)-2-[[(5-bromo-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol
-
-
(1R,2S)-2-[[(5-chloro-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol
-
-
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexyl acetate
-
-
(1R,2S)-2-[[(6-chloro-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
(1R,2S)-2-[[(6-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
(1S,2R)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
(2,4-dichlorophenyl)methanethiol
-
-
(2-chlorophenyl)methanethiol
-
-
(2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoic acid
-
-
(2S)-2'-methoxy kurarinone
non-competitive inhibitor
-
(3,4-dichlorophenyl)methanethiol
-
-
(3-hydroxyphenyl)(phenyl)methanone
-
(3R,4S and 3S,4R)-3-bromo-4-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-3-hydroxy-2,2-dimethyl-4-morpholino-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-3-hydroxy-4-methoxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-4-(allylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-4-(benzylthio)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3R,4S and 3S,4R)-4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-3,4-dihydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
alpha-lapachone
(3S,4S and 3R,4R)-3-hydroxy-2,2-dimethyl-4-morpholino-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-3-hydroxy-4-methoxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-4-(allylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-4-(benzyloxy)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S and 3R,4R)-4-(benzylthio)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S)-4-(benzylamino)-3,9-dihydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(3S,4S)-4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
(4-chlorophenyl)methanethiol
-
-
(4-chlorophenyl)methanol
-
-
(4-fluorophenyl)methanethiol
-
-
(4-methoxyphenyl)methanethiol
-
-
(4-methylphenyl)methanethiol
-
-
(4E,4'E)-4,4'-bis(isopropylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
-
(4E,4'E)-4,4'-bis(pentan-3-ylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
-
(4Z,7Z,10Z,13Z,16Z)-docosapentaenoic acid
-
48% inhibition at 0.02 mM
(4Z,7Z,10Z,13Z,16Z,19Z)-Docosahexaenoic acid
-
35% inhibition at 0.02 mM
(5Z,8Z)-7,7-dimethyl-5,8-eicosadienoic acid
-
29% inhibition at 0.02 mM
(5Z,8Z)-eicosadienoic acid
-
42% inhibition at 0.02 mM
(5Z,8Z,11Z)-eisosatrienoic acid
-
45% inhibition at 0.02 mM
(5Z,8Z,11Z,14Z)-eicosatetraenoic acid
-
55% inhibition at 0.02 mM; 80% inhibition at 0.02 mM
(5Z,8Z,11Z,14Z,17Z)-eicosapentaenoic acid
-
19% inhibition at 0.02 mM
(7Z,10Z,13Z,16Z)-docosatetraenoic acid
-
42% inhibition at 0.02 mM
(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)boronic acid
-
-
(8Z,11Z,14Z)-eisosatrienoic acid
-
68% inhibition at 0.02 mM
(9E,11Z)-octadecadienoic acid
-
26% inhibition at 0.02 mM
(9E,12E)-octadecadienoic acid
-
23% inhibition at 0.02 mM
(9Z,12Z)-octadecadienoic acid
-
16% inhibition at 0.02 mM
(9Z,12Z,15Z)-octadecatrienoic acid
-
23% inhibition at 0.02 mM
(E)-4-(isopropylimino)-2-methylnaphthalen-1(4H)-one
-
(E)-6-fluoro-3-[2-(3-pyridyl)vinyl]-1H-indole
-
-
(R)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
-
(S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(1,4-dihydroxy-3-methylnaphthalen-2-ylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid
-
(S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-ylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid
-
(S)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
-
1,6,6-trimethyl-10,11-dioxo-2-(thiophen-3-yl)-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
0.02 mM, 29.3% inhibition
-
1,6,6-trimethyl-10,11-dioxo-2-phenyl-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
0.02 mM, 21.5% inhibition
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl 1,3-thiazole-2-carboxylate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl acetate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl benzoate
0.02 mM, 54.5% inhibition
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl cyclohexanecarboxylate
0.02 mM, 48.0% inhibition
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl cyclopropanecarboxylate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl furan-3-carboxylate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl hydroxyacetate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
-
-
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl thiophene-2-carboxylate
0.02 mM, 60.4% inhibition
-
1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione
0.02 mM, 23.1% inhibition
1,6,6-trimethyl-6,7-dihydrophenanthro[1,2-b]furan-10,11-dione
0.02 mM, 61.2% inhibition
-
1,6,6-trimethylphenanthro[1,2-b]furan-7,10,11(6H)-trione
-
-
1,6,6-trimethylphenanthro[1,2-b]furan-9,10,11(6H)-trione
0.02 mM, 52.7% inhibition
-
1-(1,3-benzothiazol-2-ylsulfanyl)-N,N-dimethylmethanamine
-
1-(2-hydroxy-4-methylphenyl)-3-(2-methoxyphenyl)propane-1,3-dione
-
-
1-(2-hydroxy-4-methylphenyl)-3-{2-[(propan-2-yl)oxy]phenyl}propane-1,3-dione
-
-
1-(2-methylbenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(3-bromobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(3-bromothiophen-2-yl)-2-(3-methyl-1,4-dihydronaphthalen-2-yl)ethan-1-one
most potent inhibitor capable of blocking both indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) activity, with the IC50 value for BT-549 cells at 0.00342 mM
-
1-(3-chlorobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(3-[(4-acetyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
-
1-(3-[(4-methyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
-
1-(4-bromobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(4-bromophenyl)-2-[[5-(4-chlorophenyl)[1,3]thiazolo[2,3-c]-[1,2,4]triazol-3-yl]sulfanyl]ethanone
-
-
1-(4-chlorobenzyl)urea
-
-
1-(4-chlorophenyl)methanamine
-
-
1-(4-chlorophenyl)thiourea
-
-
1-(4-cyanophenyl)-3-(3-(cyclopropylethynyl)imidazo[2,1-b]thiazol-5-yl)thiourea
potent inhibitor. The basis for this high potency is a unique sulfur-aromatic interaction network formed by the thiourea moiety of the inhibitor with F163 and F226
-
1-(4-fluorobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(4-methylbenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(4-[(4-acetylpiperazin-1-yl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
-
1-(4-[(4-methoxypiperidin-1-yl)carbonyl]benzyl)-1Hnaphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-(hydroxymethyl)-6,6-dimethylphenanthro[1,2-b]furan-7,10,11(6H)-trione
-
-
1-(hydroxymethyl)-6,6-dimethylphenanthro[1,2-b]furan-9,10,11(6H)-trione
0.02 mM, 68% inhibition
-
1-benzofuran-DL-tryptophan
-
1 mM, 43% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
1-benzothiophene-DL-tryptophan
-
1 mM, 16% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
1-benzyl-5-phenyl-1H-imidazole
-
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol
1-hydroxy-5,6-dimethoxy-3-oxo-2-phenyl-3H-indol-1-ium
-
1-methyl tryptophan
a tryptophan analogue. Galanal does not decrease the IkappaB-alpha expression in LPS-stimulated THP-1 cells
1-oxo-2-phenyl-3H-1lambda5-indol-3-one
-
1-phenyl-2-(phenylsulfanyl)hydrazine
-
1-[(3-methylphenyl)methyl]-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-[(4-chlorophenyl)methyl]-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
-
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylic acid
-
-
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylic acid
-
-
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]proline
-
-
1-[2-(4-chlorophenyl)ethyl]thiourea
-
-
1-[3-(4-morpholinylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
-
1-[4-(morpholin-4-ylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
-
1-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
-
1-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-3-(4-methylphenyl)imidazolidin-2-one
-
-
15-deoxy-DELTA12,14-prostaglandin
-
-
1H-phenanthro[9,10-d]imidazole
-
2,2-dimethyl-1a,9b-dihydro-2H-benzo[g]oxireno[c]chromene-4,9-dione
-
2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
dehydro-alpha-lapachone
2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
2,2-dimethyl-3,4-epoxy-2H-naphtho[2,3-b]pyran-5,10-dione
-
2,3-dichloro-1,4-naphthoquinone
-
2,4-dichlorobenzyl carbamimidothioate hydrobromide
-
-
2-(1H-imidazol-4-yl)benzene-1,3-diol
-
2-(1H-imidazol-4-yl)benzenethiol
-
2-(1H-imidazol-4-yl)phenol
2-(1H-phenanthro[9,10-d]imidazol-2-yl)phenol
-
2-(1H-pyrazol-3-yl)phenol
-
2-(2-chlorophenyl)ethyl carbamimidothioate hydrobromide
-
-
2-(2-fluorophenyl)-1H-phenanthro[9,10-d]imidazole
-
2-(2-methylphenyl)-1-oxo-3H-1lambda5-indol-3-one
-
2-(2-methylphenyl)-1H-phenanthro[9,10-d]imidazole
-
2-(2-sulfanylidene-2,3-dihydro-1,3-thiazol-4-yl)benzoic acid
0.1 mM, 8% inhibition
-
2-(3-chlorophenyl)ethyl carbamimidothioate hydrobromide
-
-
2-(4-chlorophenyl)ethanamine
-
-
2-(4-chlorophenyl)ethyl carbamimidothioate hydrobromide
-
-
2-(4-methoxyphenyl)-1-oxo-3H-1lambda5-indol-3-one
-
2-(4-methoxyphenyl)-3H-indol-3-one
-
2-(4-methoxyphenyl)-3H-indole
-
2-(4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]-triazol-1-yl)methyl]phenyl)-N,N-diethylacetamide
-
2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide
poor inhibitor; poor inhibitor
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-chlorophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-hydroxyphenyl)acetate
0.001 mM, 73% inhibition
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-nitrophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3,4-dihydroxyphenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-chlorophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-cyanophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-hydroxyphenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (3-nitrophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-chlorophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-cyanophenyl)acetate
0.001 mM, 69% inhibition
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-hydroxyphenyl)acetate
0.001 mM, 89% inhibition
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-nitrophenyl)acetate
-
-
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl phenylacetate
0.001 mM, 72% inhibition
-
2-amino-3-hydroxy-N-(4-hydroxynaphthalen-1-yl)propanamide
-
2-amino-N-(4-hydroxynaphth-1-yl)acetamide
-
2-bromo-4-phenyl-1,3-thiazole
0.1 mM, 12% inhibition
-
2-bromo-L-tryptophan
-
1 mM, 11% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
2-chloro-4-phenyl-1,3-thiazole
0.1 mM, 0.5% inhibition
-
2-chloro-L-tryptophan
-
1 mM, 20% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
2-chloro-N-[[(4-chlorophenyl)sulfanyl]methyl]aniline
-
2-chlorobenzyl carbamimidothioate hydrochloride
-
-
2-Hydroxy-1,4-naphthoquinone
-
2-hydroxy-L-tryptophan
-
1 mM, 30% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
2-mercaptobenzothiazole
-
2-methoxy-1,4-naphthoquinone
-
2-methyl-1,4-naphthoquinone
-
2-methylnaphthalene-1,4-dione
-
2-phenyl-3H-indol-3-imine
-
2-phenyl-3H-indol-3-one
-
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(3-chlorophenyl)ethan-1-ol
-
-
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(4-hydroxyphenyl)ethan-1-one
-
-
2-[(6-bromo-1H-indazol-4-yl)amino]-2-(3-chlorophenyl)ethan-1-ol
-
-
2-[(6-bromo-1H-indazol-4-yl)amino]-2-phenylethan-1-ol
-
-
2-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
-
-
2-[[(2,4-dichlorophenyl)methyl]sulfanyl]-6-methylpyrimidin-4(5H)-one
-
2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
-
-
2-[[5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl]sulfanyl]-N-[5-(propan-2-yl)thiophen-2-yl]butanamide
0.01 mM, 24.4% inhibition
-
3'-[[(2-chlorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
3'-[[(2-fluorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(2-methylpropyl)(propan-2-yl)amino][1,1'-biphenyl]-2-carboxylic acid
-
-
3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(4aS,8aS)-octahydroquinolin-1(2H)-yl][1,1'-biphenyl]-2-carboxylic acid
-
-
3,4-dichlorobenzyl carbamimidothioate hydrochloride
-
-
3-(1H-1,2,3-triazol-5-yl)pyridine
3-(1H-imidazol-4-yl)benzaldehyde
-
3-(1H-imidazol-4-yl)benzenethiol
-
3-(1H-imidazol-4-yl)benzonitrile
-
3-(1H-imidazol-4-yl)phenol
-
3-(1H-phenanthro[9,10-d]imidazol-2-yl)phenol
-
3-(2-aminoethyl)-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 74.88% inhibition
-
3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazole
-
-
3-(4H-imidazol-4-yl)benzenethiol
-
3-chlorobenzyl carbamimidothioate hydrochloride
-
-
3-hydroxy-2,2-dimethyl-4-(morpholin-4-yl)-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
3-hydroxy-4-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
3-hydroxyanthranilic acid
-
-
3-indoleethanol
-
lowers Km value for D-tryptophan by 25% at pH 7, enhances Vmax by 40-60%
3-methyl-8-(4,4,4-trifluorobutoxy)-5H-indeno[1,2-c]pyridazin-5-one
-
31% inhibition at 0.025 mM
3-methyl-8-[(3-methylbenzyl)oxy]-5H-indeno[1,2-c]pyridazin-5-one
-
66% inhibition at 0.025 mM
3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
-
3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
-
3-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
-
-
3-[2-(cyclohexylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 64.95% inhibition
-
3-[2-(diethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 64.21% inhibition
-
3-[2-(dimethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 71.26% inhibition
-
3-[2-(ethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 81.67% inhibition
-
3-[2-(propylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 79.17% inhibition
-
3-[2-(tert-butylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 79.45% inhibition
-
3-[2-[(2-phenylethyl)amino]ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 68.26% inhibition
-
3-[2-[(propan-2-yl)amino]ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
0.01 mM, 63.75% inhibition
-
3-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]propanoic acid
EC50 is 183 nm
4'-(2,3-dimethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-chlorophenoxy)-3'-([[4-(2-hydroxypropan-2-yl)phenyl]carbamoyl]amino)-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-chlorophenoxy)-3'-[[(4-chlorophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-chlorophenoxy)-3'-[[(4-cyanophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methoxyphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-ethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-tert-butylanilino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-2-fluoro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-4-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-4-ethoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(2-tert-butylphenoxy)-5-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(3-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-(cyclohexylamino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-(dibutylamino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-[(2,3-dihydro-1H-inden-4-yl)oxy]-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
-
-
4'-[bis(2-methylpropyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-[bis(2-methylpropyl)amino]-N-(methanesulfonyl)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxamide
-
-
4'-[bis(cyclopropylmethyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-[cyclohexyl(methyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4'-[cyclopentyl(ethyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
-
-
4-(1H-1,2,3-triazol-5-yl)pyridine
-
4-(1H-imidazol-4-yl)phenol
-
4-(1H-phenanthro[9,10-d]imidazol-2-yl)phenol
-
4-(2,6-dimethoxyphenyl)-1H-imidazole
-
4-(2-(diethylamino)ethylamino)-1-naphthol
-
4-(2-(methylthio)phenyl)-1H-imidazole
-
4-(2-fluorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 77% inhibition
-
4-(2-fluorophenyl)-1H-imidazole
-
4-(2-hydroxyethoxy)-1-naphthol
-
4-(2-methoxyphenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 53% inhibition
-
4-(2-sulfanylidene-2,3-dihydro-1,3-thiazol-4-yl)benzonitrile
0.1 mM, 8% inhibition
-
4-(3-(methylthio)phenyl)-1H-imidazole
-
4-(3-bromophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 81% inhibition
-
4-(3-chlorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 40% inhibition
-
4-(3-chlorophenyl)-imidazole
-
-
4-(3-fluorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 28% inhibition
-
4-(3-fluorophenyl)-1H-imidazole
-
4-(4-(methylthio)phenyl)-1H-imidazole
-
4-(4-bromophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 100% inhibition
-
4-(4-chlorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 95% inhibition
-
4-(4-fluorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 72% inhibition
-
4-(4-fluorophenyl)-1H-imidazole
-
4-(4-methoxyphenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 68% inhibition
-
4-(4-methylbenzene-1-sulfinyl)-7-nitro-2,1,3-benzoxadiazole
-
4-(4-methylphenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 90% inhibition
-
4-(benzylamino)-1-naphthol
-
4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
4-(cyclohexylamino)-1-naphthol
-
4-(dimethylamino)naphthalen-1-ol
-
4-(ethylamino)-1-naphthol
-
4-(isobutylamino)-1-naphthol
-
4-(isopropylamino)-1-naphthol
-
4-(methanesulfonyl)-N'-(3-methylphenyl)benzene-1-sulfonohydrazide
EC5 is 7846 nm
4-(methylamino)naphthalen-1-ol
-
4-(pent-3-ylamino)-1-naphthol
-
4-(phenylcarbonyl)benzyl carbamimidothioate hydrobromide
-
-
4-(propan-2-yl)benzyl carbamimidothioate hydrobromide
-
-
4-(propylamino)-1-naphthol
-
4-(pyridin-3-yl)-1,3-thiazole-2(3H)-thione
0.1 mM, 48% inhibition
-
4-(pyridin-4-yl)-1,3-thiazole-2(3H)-thione
0.1 mM, 21% inhibition
-
4-(tert-butylamino)naphthalen-1-ol
-
4-(thiophen-2-yl)-1H-imidazole
-
4-(trifluoromethyl)benzyl carbamimidothioate hydrochloride
-
-
4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylic acid
-
-
4-amino-1,2,3-oxadiazole-3-carboximidamide
-
-
4-amino-1,2,5-oxadiazole-3-carboximidamide
-
competitive
4-amino-N'-hydroxy-N-(3-isopropylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N'-hydroxy-N-(3-methoxyphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N'-hydroxy-N-(3-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N'-hydroxy-N-phenyl-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(2-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-bromophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
4-amino-N-(3-chlorophenyl)-1,2,5-oxadiazole-3-carbohydrazonamide
-
-
4-amino-N-(3-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-ethylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-tert-butylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(4-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-benzyl-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-bromo-5-(4-methylphenyl)-1H-1,2,3-triazole
-
-
4-bromo-N'-(4-bromophenyl)benzene-1-sulfonohydrazide
EC50 is 374 nm
4-bromobenzyl carbamimidothioate hydrobromide
-
-
4-chloro-2-(1H-1,2,3-triazol-4-yl)phenol
i.e. MMG-0358
-
4-chlorobenzenesulfonic acid
-
-
4-chlorobenzyl carbamimidothioate hydrochloride
-
-
4-chlorobenzyl N,N'-dimethylcarbamimidothioate - 1-chlorotetraoxidane (1:1)
-
-
4-chlorophenyl-1,2,3-triazol-4-amine
-
-
4-cyano-N'-(3-methylphenyl)benzene-1-sulfonohydrazide
EC50 is 3404 nm
4-cyanobenzyl carbamimidothioate hydrobromide
-
-
4-ethylbenzyl carbamimidothioate hydrochloride
-
-
4-fluoro-2-(1H-pyrazol-3-yl)phenol
-
4-fluorobenzyl carbamimidothioate hydrochloride
-
-
4-iodo-5-phenyl-1H-1,2,3-triazole
-
-
4-methoxy-1-naphthylamine
-
4-methoxy-3'-[(phenylcarbamoyl)amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(2-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(3-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-(2-propylphenoxy)[1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-(propan-2-yl)phenoxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-methyl-3-[(prop-2-yn-1-yl)oxy]phenoxy][1,1'-biphenyl]-3-carboxylic acid
-
-
4-methoxybenzyl carbamimidothioate hydrochloride
-
-
4-methyl-DL-tryptophan
-
1 mM, 26% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
4-methylbenzyl carbamimidothioate hydrochloride
-
-
4-nitro-2,1,3-benzothiadiazole
-
4-nitro-5-(4-nitrophenyl)-1H-1,2,3-triazole
-
-
4-nitro-7-[(1-oxo-1lambda5--pyridin-2-yl)sulfanyl]-2,1,3-benzoxadiazole
-
4-nitrobenzyl carbamimidothioate hydrochloride
-
-
4-phenyl-1,3-thiazol-2(3H)-one
0.1 mM, 15% inhibition
-
4-phenyl-1,3-thiazol-2-amine
4-phenyl-1,3-thiazole-2(3H)-thione
0.1 mM, 76% inhibition
-
4-phenyl-1,3-thiazole-2-thiol
-
4-phenyl-imidazole
4-phenyl-imidazole coordinates transiently to the heme iron
4-tert-butylbenzyl carbamimidothioate hydrobromide
-
-
4-[(1Z)-2-[(6-bromo-1H-indazol-4-yl)amino]-N-hydroxyethanimidoyl]phenol
-
-
4-[(2,4-dichlorophenyl)sulfanyl]-7-nitro-2,1,3-benzoxadiazole
-
4-[(3-chlorophenyl)sulfanyl]-7-nitro-2,1,3-benzoxadiazole
-
4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
-
4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
-
4-[(4-fluorophenyl)sulfanyl]-7-nitro-2,1,3-benzoxadiazole
-
4-[(4-methylphenyl)sulfanyl]-7-nitro-2,1,3-benzoxadiazole
-
4-[(carbamimidoylsulfanyl)methyl]benzoic acid hydrochloride
-
-
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzamide
-
-
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzene-1-sulfonamide
potent inhibitor with a moderate pharmacokinetic profile. 25% tumor growth inhibition and 30% reduction in tumor weight in a murine CT26 syngeneic model on day 18, with 100 mg/kg oral administration twice daily
-
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
-
-
4-[2-(4-bromophenyl)hydrazinesulfonyl]benzoic acid
EC50 is 172 nm
4-[2-(methylsulfanyl)phenyl]-1H-imidazole
-
4-[3-(hydroxymethyl)phenyl]-1,3-thiazole-2(3H)-thione
0.1 mM, 16% inhibition
-
4-[3-(methylsulfanyl)phenyl]-1H-imidazole
-
4-[4-(trifluoromethyl)phenyl]-1,3-thiazole-2(3H)-thione
0.1 mM, 37% inhibition
-
4-[[(2,4-dichlorophenyl)methyl]sulfanyl]-6-methylpyrimidin-2(1H)-one
-
4-[[(2,4-dichlorophenyl)methyl]sulfanyl]pyrimidin-2(1H)-one
-
4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]phenol
-
-
5-(2-bromophenyl)-1H-1,2,3-triazole
-
-
5-(2-chlorophenyl)-1H-1,2,3-triazole
-
-
5-(2-fluorophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 29% inhibition
-
5-(2-methoxyphenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 12% inhibition
-
5-(2-methoxyphenyl)-1H-1,2,3-triazole
-
-
5-(3-bromophenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 48% inhibition
-
5-(4-bromophenyl)-1H-1,2,3-triazole
-
-
5-(4-chlorophenyl)-1H-1,2,3-triazole
-
-
5-(4-chlorophenyl)-3-[(2-methylpropyl)sulfanyl][1,3]thiazolo-[2,3-c][1,2,4]triazole
-
-
5-(4-fluorophenyl)-1H-1,2,3-triazole
-
-
5-(4-methoxyphenyl)-1H-1,2,3-triazole
-
-
5-(4-methylphenyl)-1,3-thiazole-2(3H)-thione
0.1 mM, 15% inhibition
-
5-(ethylamino)quinolin-8-ol
-
5-(isopropylamino)quinolin-8-ol
-
5-amino-8-hydroxyquinoline
-
5-benzyloxy-DL-tryptophan
-
1 mM, 2% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-bromo-DL-tryptophan
-
1 mM, 56% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-chloro-1,3-benzothiazole-2(3H)-thione
-
5-fluoro-DL-tryptophan
-
1 mM, 32% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-hydroxy-1,4-naphthoquinone
-
5-hydroxy-D-tryptophan
-
0.1 mM, 26% inhibition of cleavage of D-tryptophan, 29% inhibition of cleavage of L-tryptophan
5-hydroxyindole acetic acid
-
1 mM, 61.5% inhibition
5-hydroxytryptamine
-
1 mM, 82.3% inhibition
5-hydroxytryptophan
-
1 mM, 78.6% inhibition
5-methoxy-DL-tryptophan
-
1 mM, 35% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-methyl-DL-tryptophan
-
1 mM, 6% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-phenyl-1,3-thiazole-2(3H)-thione
0.1 mM, 16% inhibition
-
5-phenyl-1H-1,2,3-triazole
5-[(2E)-2-[(4-bromophenyl)methylidene]hydrazinyl]-1-(naphthalen-1-yl)tetrazolidine
0.01 mM, 54.3% inhibition
-
5-[[(2,4-dichlorophenyl)methyl]sulfanyl]-1H-1,2,4-triazole
-
6-(4-iodo-2-methylanilino)-2,1,3-benzoxadiazole-5-carboxylic acid
-
6-(4-iodo-2-methylanilino)-3-oxo-2,1,3lambda~5~-benzoxadiazole-5-carboxylic acid
-
6-bromo-1H-indazol-4-amine
-
-
6-bromo-N-(cyclohexylmethyl)-1H-indazol-4-amine
-
-
6-bromo-N-[(1,4-dioxaspiro[4.5]decan-6-yl)methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[(1R,2R)-2-hydroxycyclohexyl]-1H-indazole-4-carboxamide
-
-
6-bromo-N-[(pyridin-2-yl)methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[(pyrrolidin-3-yl)methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(1S,2R)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(1S,2S)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(2R)-piperidin-2-yl]methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(2R)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(2S)-piperidin-2-yl]methyl]-1H-indazol-4-amine
-
-
6-bromo-N-[[(2S)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine
-
-
6-fluoro-DL-tryptophan
-
1 mM, 54% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
6-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
6-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
-
6-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
6-methyl-DL-tryptophan
-
1 mM, 20% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
6-nitro-D-tryptophan
-
1 mM, 7% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
6-nitro-L-tryptophan
-
1 mM, competitive inhibition, 52% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
7-amino-2-[(2E)-3-(2H-1,3-benzodioxol-5-yl)prop-2-enoyl]-4-bromocyclohepta-2,4,6-trien-1-one
0.01 mM, 21.4% inhibition
-
7-fluoro-4-(2-fluoro-4-iodoanilino)-2,1,3-benzoxadiazole-5-carboxylic acid
-
7-hydroxy-1,6,6-trimethyl-6,7-dihydrophenanthro[1,2-b]furan-10,11-dione
-
-
7-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
7-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
7-methyl-DL-tryptophan
-
1 mM, 36% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
7-nitro-N-phenyl-2,1,3-benzoxadiazol-4-amine
-
8-(4,4,4-trifluorobutoxy)-3-[3-(trifluoromethyl)phenyl]-5H-indeno[1,2-c]pyridazin-5-one
-
20% inhibition at 0.025 mM
8-(benzyloxy)-3-[3-(trifluoromethyl)phenyl]-5H-indeno[1,2-c]pyridazin-5-one
-
-
8-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolo[2,1-b]quinazoline-6,12-dione
-
-
8-fluoro-2-[(1H-1,2,3-triazol-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
-
-
8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbaldehyde
-
-
8-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
8-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
8-methoxy-3-[3-(trifluoromethyl)phenyl]-5H-indeno[1,2-c]pyridazin-5-one
-
18% inhibition at 0.025 mM
8-[(3-chlorobenzyl)oxy]-3-methyl-5H-indeno[1,2-c]pyridazin-5-one
-
19% inhibition at 0.025 mM
9-hydroxy-1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione
-
-
9-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
alpha-caryopterone
9-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
-
acetaminophen
-
no affect on holoenzyme, significant inhibition of apoenzyme, changes in brain serotonin levels due to inhibition of hepatic tryptophan 2,3-dioxygenase
alpha-methyl-DL-tryptophan
-
1 mM, 1% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
alpha-N-methyl-L-tryptophan
-
1 mM, 33% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
antisense oligonucleotide A06007H
+G*+A*+T*T*G*T*C*C*A*G*G*A*+G*+T*+T, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A06008H
+C*+T*+C*A*A*C*T*C*T*T*T*C*+T*+C*+G, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A06030H
+A*+G*+G*C*G*C*T*G*T*G*A*C*T*+T*+G*+T, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A06043H
+C*+C*+A*G*A*C*T*C*T*A*T*G*A*G*+A*+T*+C, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A06044H
+G*+A*+G*A*T*G*A*T*C*A*A*T*G*C*+T*+G*+A, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A06045H
+A*+G*+G*C*G*C*T*G*T*G*A*C*T*T*+G*+T*+G, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A07006H
+T*+G*+T*A*T*G*A*C*A*G*C*+C*+G*+T, (+) LNA-modified nucleotide, (*) PTO linkage
-
antisense oligonucleotide A07058H
+A*+T*+C*G*T*G*G*T*G*C*T*G*A*A*+C*+A*+A, (+) LNA-modified nucleotide, (*) PTO linkage
-
baicalein
-
uncompetitive reversible potent IDO-1 inhibitor
Bathocuproinesulfonate
-
competitive with respect to L-Trp and noncompetitive with respect to O2
benzyl carbamimidothioate hydrochloride
-
-
Berberine
-
uncompetitive reversible potent IDO-1 inhibitor
beta-Methyl-DL-tryptophan
-
1 mM, 7% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
Cd2+
-
0.5-1.0 mM, non-competitive
Cu2+
-
0.005 mM, 50% inhibition
DL-5-hydroxytryptophan
-
1 mM, 55% inhibition
DL-alpha-methyltryptophan
-
-
epigallocatechin gallate
-
-
ethyl (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoate
-
-
ethyl 1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl (2E)-but-2-enedioate
-
-
ethyl 1-(4-chlorophenyl)-1H-1,2,3-triazole-4-carboxylate
-
-
galanal
competitive inhibitor, IC50 value of 45 nM in the cell-based assay. galanal interfered with the transcriptional function of the nuclear factor-kappaB and the interferon-gamma signaling pathway. These effects of galanal are important for immune response. The inhibitory effect of galanal on IDO1 activity is stronger than that of 1-methyl tryptophan, a tryptophan analogue
gamma-glutamyl-S-(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl)cysteinylglycine
-
hydroxylamine sulfate
-
0.1 mM causes 79% inhibition, 1 mM causes 94% inhibition
imidazole
-
negatively cooperative or competitive
imidodicarbonimidic diamide, N-methyl-N''-9-phenanthrenyl-, monohydrochloride
-
-
INCB024360
0.01 mM, 97.59% inhibition
-
indole-3-acetic acid
-
1 mM, 19% inhibition of cleavage of D-tryptophan, 27% inhibition of cleavage of L-tryptophan
indole-3-acrylic acid
-
competitive inhibitor
Indole-3-propionic acid
-
-
iodoacetic acid
-
1 mM, 12% inhibition of cleavage of D-tryptophan, 7% inhibition of cleavage of L-tryptophan
Jatrorrhizine
-
irreversible potent IDO-1 inhibitor
K3Fe(CN)6
-
1 mM, complete inhibition
kushenol E
non-competitive inhibitor, the inhibitor might be useful in the development of immunotherapeutic agents against cancers
kushenol F
non-competitive inhibitor
-
Kynurenic acid
-
0.1 mM, 57.2% inhibition. 1 mM, 99.4% inhibition
L-kynurenine
-
0.1 mM, 17.7% inhibition. 1 mM, 93.6% inhibition
L-tryptophan ethyl ester
-
1 mM, 7% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
L-tryptophan methyl ester
-
1 mM, 30% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
levo-1-methyl tryptophan
-
-
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylate
-
-
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylate
-
-
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]prolinate
-
-
methyl 2-methyl-5,10-dioxo-5,10-dihydro-2H-benzo[g]chromene-2-carboxylate
-
methyl 3-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]propanoate
EC50 is 465 nm
methyl 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylate
-
-
methyl 4-[(carbamimidoylsulfanyl)methyl]benzenesulfinate hydrobromide
-
-
methyl 7-fluoro-4-(2-fluoro-4-iodoanilino)-2,1,3-benzoxadiazole-5-carboxylate
-
methyl N-(4-chlorophenyl)carbamimidothioate hydroiodide
-
-
methyl N-[2-(4-chlorophenyl)ethyl]carbamimidothioate hydroiodide
-
-
methyl thiohydantoin-Trp
-
methyl-thiohydantoin tryptophan
-
-
methyl-thiohydantoin-L-tryptophan
-
competitive inhibitor
methyl-thiohydantoin-tryptophan
-
limited selectivity towards indoleamine 2,3-dioxygenase
methylene blue
addition of methylene blue (0-0.1 mM) to NADPH-cytochrome P450 reductase-supported D-Trp incubations (with or without cytochrome b5) leads to concentration-dependent inhibition of IDO activity, addition of methylene blue (0-0.03 mM) to NADPH-cytochrome P450 reductase-supported L-Trp oxidation reactions results in a switch from substrate inhibition kinetics to Michaelis-Menten with increasing methylene blue concentration decreasing the affinity of IDO for L-Trp
methylthiohydantoin-DL-tryptophan
-
N'-(3-methylphenyl)-4-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzene-1-sulfonohydrazide
EC50 is 296 nm
N'-(4-bromophenyl)-4-cyanobenzene-1-sulfonohydrazide
EC50 is 134 nm
N'-(4-bromophenyl)-4-methoxybenzene-1-sulfonohydrazide
EC50 is 640 nm
N'-(4-bromophenyl)benzenesulfonohydrazide
EC50 is 128 nm
N'-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N-methyl-N-(4-methylphenyl)urea
-
-
N,N-dimethyl-1-[(4-phenyl-1,3-thiazol-2-yl)sulfanyl]methanamine
-
N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
a reversible inhibitor of IDO1. highly specific for IDO1 compared to IDO2, docking analysis with IDO1 and IDO2; a reversible inhibitor of IDO1. highly specific for IDO1 compared to IDO2, docking analysis with IDO1 and IDO2
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
-
-
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
selective inhibitor of IDO1 against L-Trp dioxygenase (TDO) at 0.001 mM, yet when the concentration is increased up to 0.010 mM, an inhibition of TDO is observed to some extent
-
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
-
-
N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[[2-(sulfamoylamino)ethyl]amino]-1,2,5-oxadiazole-3-carboximidamide
-
-
N-(4'-[bis(2-methylpropyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-yl)-1,1,1-trifluoromethanesulfonamide
-
-
N-(4-bromophenyl)-7-nitro-2,1,3-benzoxadiazol-4-amine
-
N-(4-bromophenyl)-N'-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]urea
-
-
N-(4-chlorophenyl)-2H-1,2,3-triazol-4-amine
i.e. Vertex-AT
-
N-(4-hydroxy-1-naphthyl)ethane-1,2-diaminium chloride
-
N-(4-hydroxy-1-naphthyl)propane-1,3-diaminium chloride
-
N-(4-hydroxynaphthalen-1-yl)pyrrolidine-2-carboxamide
-
N-(4-methoxyphenyl)-7-nitro-2,1,3-benzoxadiazol-4-amine
-
N-(4-methylphenyl)-2,1,3-benzoxadiazol-4-amine
-
N-(4-methylphenyl)-7-nitro-2,1,3-benzoxadiazol-4-amine
-
N-(4-[2-[4-(trifluoromethyl)phenyl]hydrazinesulfonyl]phenyl)acetamide
EC50 is 181 nm
N-(4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexylidene)hydroxylamine
-
-
N-(phenyldisulfanyl)aniline
-
N-acetyl-L-tryptophan
-
1 mM, 7% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
n-butyl isocyanide
-
heme ligand which binds tightly to the ferrous enzyme
N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
poor inhibitor; poor inhibitor
N-ethylmaleimide
-
1 mM, 58% inhibition of cleavage of D-tryptophan, 45% inhibition of cleavage of L-tryptophan
N-phenyl-p-phenylenediamine
-
N-[(1,3-benzothiazol-2-yl)sulfanyl]-2-nitrobenzene-1-sulfonamide
0.01 mM, 35.9% inhibition
-
N-[(azetidin-3-yl)methyl]-6-bromo-1H-indazol-4-amine
-
-
N-[(E)-(2-phenyl-3H-indol-3-yl)methylidene]hydroxylamine
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-3-methoxy-N-methylbenzamide
-
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-4-methoxy-N-methylbenzamide
-
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-(4-cyanophenyl)acetamide
-
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-methyl-4-nitrobenzamide
-
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-methylacetamide
-
-
N-[2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl]-N-phenylacetamide
-
-
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]-2,2-dimethylpropanamide
0.01 mM, 72.35% inhibition
-
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]acetamide
0.01 mM, 57.47% inhibition
-
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]benzamide
0.01 mM, 65.72% inhibition
-
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]benzenesulfonamide
0.01 mM, 59.71% inhibition
-
N-[4-(2-phenylhydrazinesulfonyl)phenyl]acetamide
EC50 is over 0.010 mM
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(2-methylphenyl)urea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(3-methylphenyl)urea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methoxyphenyl)urea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-phenylurea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(difluoromethoxy)phenyl]urea
-
-
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(trifluoromethoxy)phenyl]urea
-
-
N-[4-[2-(2,4-difluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is over 0.010 mM
N-[4-[2-(3,4-dichlorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 350 nm
N-[4-[2-(3,5-dichlorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 508 nm
N-[4-[2-(3,5-difluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 2229 nm
N-[4-[2-(3-bromo-4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 2494 nm
N-[4-[2-(3-bromophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 7563 nm
N-[4-[2-(3-chloro-4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 2588 nm
N-[4-[2-(3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is over 0.010 mM
N-[4-[2-(3-methylphenyl)hydrazinesulfonyl]benzoyl]glycine
EC50 is 571 nm
N-[4-[2-(3-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 241 nm
N-[4-[2-(4-bromo-3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 187 nm
N-[4-[2-(4-bromo-3-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 130 nm
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-chlorophenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-cyanophenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-fluorophenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-methoxyphenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-methylphenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-chlorophenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-methoxyphenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-methylphenyl)urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-butylurea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-cyclohexylurea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-[3-(1H-tetrazol-5-yl)phenyl]urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-[4-(1H-tetrazol-5-yl)phenyl]urea
-
-
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 85 nm
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]butanamide
EC50 is 187 nm
N-[4-[2-(4-chloro-3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 84 nm
N-[4-[2-(4-chlorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 142 nm
N-[4-[2-(4-cyanophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 1393 nm
N-[4-[2-(4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 609 nm
N-[4-[2-(4-methoxyphenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is over 0.010 mM
N-[4-[2-(4-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 1171 nm
N-[4-[2-(4-sulfamoylphenyl)hydrazinesulfonyl]phenyl]acetamide
EC50 is 3118 nm
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-2-(4-methylphenyl)acetamide
-
-
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
-
-
N-[[(1S,2R)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine
-
-
N-[[(1S,2S)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine
-
-
N-[[(4-chlorophenyl)sulfanyl]methyl]-2-nitroaniline
-
N-[[(4-chlorophenyl)sulfanyl]methyl]-4-methylaniline
-
N-[[(4-chlorophenyl)sulfanyl]methyl]-4-nitroaniline
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-2-hydroxyacetamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-4-oxobutanamide
0.001 mM, 97% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-(phenylacetyl)glycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-(phenylacetyl)glycinamide
0.001 mM, 62% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(2-nitrophenyl)acetyl]glycinamide
0.001 mM, 67% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(3-nitrophenyl)acetyl]glycinamide
0.001 mM, 65% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(4-nitrophenyl)acetyl]glycinamide
0.001 mM, 66% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(2-chlorophenyl)acetyl]-N2-methylglycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3,4-dihydroxyphenyl)acetyl]-N2-methylglycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-chlorophenyl)acetyl]-N2-methylglycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-hydroxyphenyl)acetyl]-N2-methylglycinamide
0.001 mM, 63% inhibition
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-chlorophenyl)acetyl]-N2-methylglycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-cyanophenyl)acetyl]-N2-methylglycinamide
-
-
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(4-hydroxyphenyl)acetyl]-N2-methylglycinamide
-
-
N1-acetyl-N2-formyl-5-methoxykynurenine
-
N2-[(2S)-2-amino-2-phenylacetyl]-N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]glycinamide
-
-
NADH
-
0.1 mM, 51.3% inhibition
NaN3
-
10 mM, 33% inhibition of cleavage of D-tryptophan, 32% inhibition of cleavage of L-tryptophan
nitric oxide
-
nitric oxide can potentially inhibit isozyme IDO2 activity
noranhydroicaritin
non-competitive inhibitor
norharmane
NHM, noncompetitive versus L-Trp and competitive versus O2
NSC 401366
-
competitive with respect to tryptophan
palmatine
-
irreversible potent IDO-1 inhibitor
propan-2-yl 4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoate
-
-
prostaglandin (19R)-hydroxy-PGE2
-
-
prostaglandin 13,14-dihydro-15-oxo-PGE2
-
-
prostaglandin 15-oxo-PGE2
-
-
prostaglandin 15-oxo-PGF2alpha
-
-
prostaglandin 20-hydroxy PGE2
-
-
prostaglandin DELTA12-PGJ2
-
-
prostaglandin PGD2 ethanolamide
-
-
prostaglandin PGE2 ethanolamide
-
-
prostaglandin PGF2beta
-
-
S-(2-chlorophenyl) (4-chlorophenyl)carbamothioate
-
serotonin
-
1 mM, 36% inhibition of cleavage of D-tryptophan, 37% inhibition of cleavage of L-tryptophan
sodium 4-chlorobenzenesulfinate
-
-
sophoraflavanone B
non-competitive inhibitor
streptovaricin C
NSC19990
tenatoprazole
-
highly selective for IDO2 inhibition, no inhibition of IDO1 or tryptophan dioxygenase
tert-butyl 3-[[(6-bromo-1H-indazol-4-yl)amino]methyl]pyrrolidine-1-carboxylate
-
-
tert-butyl [2-(4,7-dioxo-5-phenyl-4,7-dihydro-1H-indol-3-yl)ethyl]carbamate
0.01 mM, 56.38% inhibition
-
tert-butyl [2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 66.51% inhibition
-
tert-butyl [2-[4,7-dioxo-5-(pyridin-4-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 12.42% inhibition
-
tert-butyl [2-[5-(2-fluorophenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 67.30% inhibition
-
tert-butyl [2-[5-(2-methoxyphenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 63.23% inhibition
-
tert-butyl [2-[5-(4-fluorophenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 43.34% inhibition
-
tert-butyl [2-[5-(4-methoxyphenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 34.45% inhibition
-
tert-butyl [2-[5-(4-methylphenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
0.01 mM, 25.52% inhibition
-
transforming growth factor-beta
-
inhibits expression in skin and synovial fibroblasts
-
xanthurenic acid
-
0.1 mM, 50.6% inhibition. 1 mM, 96.2% inhibition
[3-(4-bromobenzoyl)-1,2-oxazol-4-yl](naphthalen-2-yl)methanone
0.01 mM, 28.4% inhibition
-
[4-(1,4-dioxido-1,2,4-benzotriazin-3-yl)aminobutyl]-(2S)-N-tert-butoxycarbonyl-2-amino-(1-methyl-indole-3-yl)propanamide
-
-
[4-(1-oxido-1,2,4-benzotriazin-3-yl)aminobutyl]-(2S)-N-tert-butoxycarbonyl-2-amino-(1-methyl-indole-3-yl)propanamide
-
-
[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenoxy]acetic acid
EC50 is 152 nm
[5-(1,4-dioxido-1,2,4-benzotriazin-3-yl)aminopentyl]-(2S)-N-tert-butoxycarbonyl-2-amino-(1-methyl-indole-3-yl)propanamide
-
-
[5-(1-oxido-1,2,4-benzotriazin-3-yl)aminopentyl]-(2S)-N-tert-butoxycarbonyl-2-amino-(1-methyl-indole-3-yl)propanamide
-
-
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol
-
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol
-
-
1-L-methyltryptophan
-
-
1-methyl-D-tryptophan
-
IDO2 is the preferred biochemical target of the antitumor indoleamine 2,3-dioxygenase inhibitory compound D-1-methyl-tryptophan
1-methyl-D-tryptophan
-
-
1-methyl-D-tryptophan
-
competitive inhibitor
1-methyl-D-tryptophan
-
the isomer is more effective in inhibiting IDO than 1-methyl-L-tryptophan
1-methyl-D-tryptophan
-
selective inhibition of IDO2, 1DMT is not efficacious in a tumor model on an IDO1-/- background
1-methyl-D-tryptophan
competitive inhibition of IDO2, antitumour activity, selectivity of 1-methyltryptophan inhibition of IDO1 and IDO2
1-methyl-D-tryptophan
IDO inhibitor with selectivity for IDO2
1-methyl-D-tryptophan
-
-
1-methyl-D-tryptophan
-
poor non-competitive inhibitor of both IDO1 and IDO2 activity
1-methyl-D-tryptophan
-
-
1-methyl-D-tryptophan
-
the isomer is more effective in inhibiting IDO than 1-methyl-L-tryptophan
1-methyl-D-tryptophan
-
-
1-methyl-DL-Trp
-
-
1-methyl-DL-tryptophan
-
competitive inhibition with L-tryptophan, 2 mM, 70% inhibition
1-methyl-DL-tryptophan
-
-
1-methyl-DL-tryptophan
-
1 mM, 26% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
1-methyl-DL-tryptophan
-
-
1-methyl-DL-tryptophan
-
competitive inhibitor
1-methyl-DL-tryptophan
-
pharmacologic inhibition of indoleamine 2,3-dioxygenase skews cytokine responses of invariant natural killer T cells towards a Th1 profile
1-methyl-DL-tryptophan
-
-
1-methyl-L-tryptophan
-
1-methyl-L-tryptophan
-
-
1-methyl-L-tryptophan
-
substrate inhibition, 1-methyl-D-tryptophan exhibits no inhibitory effect
1-methyl-L-tryptophan
-
competitive inhibitor
1-methyl-L-tryptophan
-
the isomer is less effective in inhibiting IDO than 1-methyl-D-tryptophan
1-methyl-L-tryptophan
-
-
1-methyl-L-tryptophan
-
better inhibitor of IDO2 enzymatic activity than 1DMT in both cell-free and cellular assays
1-methyl-L-tryptophan
competitive inhibition of IDO1, antitumour activity, selectivity of 1-methyl L-tryptophan inhibition of IDO1 and IDO2; competitive inhibition of IDO2, antitumour activity, selectivity of 1-methyltryptophan inhibition of IDO1 and IDO2
1-methyl-L-tryptophan
competitive versus L-Trp and noncompetitive versus O2. When 1-Me-L-Trp is the only indoleamine in the reaction mixture, it is a very slow substrate for hIDO1
1-methyl-L-tryptophan
-
-
1-methyl-L-tryptophan
-
-
1-methyl-L-tryptophan
-
poor competitive inhibitor of isozyme IDO1
1-methyl-L-tryptophan
-
the isomer is less effective in inhibiting IDO than 1-methyl-D-tryptophan
1-methyl-L-tryptophan
-
better inhibitor of IDO2 enzymatic activity than 1DMT in both cell-free and cellular assays
1-methyl-tryptophan
-
-
1-methyl-tryptophan
-
competitive
1-methyl-tryptophan
non-competitive inhibitor
1-Methyltryptophan
-
2 mM, 70% inhibition; competitive
1-Methyltryptophan
-
competitive
1-Methyltryptophan
-
treatment of pregnant mice result in rapid T-cell-induces rejection of allogeneic concepti
2-(1H-imidazol-4-yl)phenol
-
2-(1H-imidazol-4-yl)phenol
-
-
2-(1H-imidazol-4-yl)phenol
-
3-(1H-1,2,3-triazol-5-yl)pyridine
-
3-(1H-1,2,3-triazol-5-yl)pyridine
-
-
3-hydroxykynurenine
-
0.1 mM, 89.8% inhibition
3-hydroxykynurenine
-
0.1 mM, weak inhibition amounting to about 30%
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
-
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
-
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
i.e. Incyte-5l
4-phenyl-1,3-thiazol-2-amine
-
4-phenyl-1,3-thiazol-2-amine
0.1 mM, 13% inhibition
4-phenylimidazole
-
-
4-phenylimidazole
weak noncompetitive inhibitor of IDO
4-phenylimidazole
-
an IDO1 inhibitor
4-phenylimidazole
-
heme ligand, non competitive, 0.1 M potassium phosphate buffer (pH 5.5-8), 0.1 M Tris-HCl buffer (pH 7.5-8), 25°C
5-hydroxy-L-tryptophan
-
1 mM, 12% inhibition relative to L-tryptophan, 50 mM potassium phosphate, pH 6.5, 10 mM ascorbic acid, 0.01 mM methylene blue, 0.1 mg catalase, 37°C, 10 min
5-hydroxy-L-tryptophan
-
0.1 mM, 40% inhibition of cleavage of D-tryptophan, 53% inhibition of cleavage of L-tryptophan
5-phenyl-1H-1,2,3-triazole
-
5-phenyl-1H-1,2,3-triazole
-
-
annulin B
-
-
brassinin
-
-
CN-
-
0.4 mM, 86% inhibition
CN-
-
9.6 mM, 50% inhibition
CN-
-
5 mM, 98% inhibition
CO
-
20% with 80% air, 78% inhibition
CO
-
negatively cooperative
CO
-
reversed by illumination
cyanide
-
prebinding of cyanide to the enzyme facilitates L-Trp binding by 22fold but retards its dissociation by 2fold, indicating that cyanide binding to the heme iron introduces structural changes to the protein matrix allowing faster access of the substrate to the active site and slower dissociation from it. Prebinding of L-Trp to the enzyme retards cyanide binding by about 13fold
cyanide
-
inhibits the dioxygenase activity
cyanide
-
heme ligand, competitive for the ferric enzyme
D-Trp
-
no inhibition
D-tryptophan
low inhibition
dexamethasone
-
inhibits IDO activity in brain and lung after systemic pokeweed mitogen administration and brains of mice suffering from malaria
diethyldithiocarbamate
-
-
diethyldithiocarbamate
-
5 mM, markedly enhances activity
diethyldithiocarbamate
-
-
DL-4-fluorotryptophan
-
-
DL-4-fluorotryptophan
-
-
DL-4-methyltryptophan
-
-
DL-4-methyltryptophan
-
-
DL-5-fluorotryptophan
-
-
DL-5-fluorotryptophan
-
-
DL-5-fluorotryptophan
-
-
DL-5-Methyltryptophan
-
-
DL-5-Methyltryptophan
-
-
DL-5-Methyltryptophan
-
-
epacadostat
pH and temperature not specified in the publication
-
exiguamine A
-
inihibor isolated from the marine sponge Neopetrosia exigua
H2O2
at high concentrations
H2O2
-
inhibits the dioxygenase activity in a manner abrogated by L-Trp. Physiological peroxidase substrates, ascorbate or tyrosine, enhanced rIDO-mediated H2O2 consumption and attenuated H2O2-induced protein oxidation and dioxygenase inhibition. H2O2 alters the heme active site of recombinant IDO
H2O2
-
inactivated by H2O formed by ascorbic acid in presence of methylen blue
hydroxylamine
-
-
indole
-
1 mM, 44% inhibition
indole
-
lowers Km value for D-tryptophan by 60% at pH 7, lowers Vmax by 12-24%, at 1 mM lowers activity by 13%
Indolepropionic acid
-
1 mM, 31% inhibition
KCN
-
0.01 mM, 39% inhibition of cleavage of D-tryptophan, 48% inhibition of cleavage of L-tryptophan
L-5-hydroxytryptophan
-
-
L-5-hydroxytryptophan
-
-
L-tryptophan
-
substrate inhibition at 0.14 mM and greater
L-tryptophan
-
substrate inhibition
L-tryptophan
-
substrate inhibition (above 0.05 mM)
L-tryptophan
-
substrate inhibition at concentrations above 0.04 mM
L-tryptophan
-
substrate inhibition of IDO1, not of IDO2
L-tryptophan
-
substrate inhibition
menadione
menadione effectively inhibits L-Trp oxidation from reactions supported with ascorbaic acid/methylene blue
N3-
-
2 mM, 22% inhibition
N3-
-
5 mM, 5% inhibition
NH2OH
-
2 mM, 54% inhibition
NO
-
-
NO
can inhibit hIDO by directly binding to the heme iron
NO
-
inhibits activity reversibly by binding to the active site heme to trap the enzyme as an inactive nitrosyl-FeII enzyme adduct with Trp bound and O2 displaced. Reversible inhibition by NO may represent an important mechanism in controlling the immune regulatory actions of IDO
NO
-
inhibits the transcription of IDO in murine macrophages
norharman
-
2 mM, 98% inhibition, uncompetitive; uncompetitive inhibition, 2 mM, 98% inhibition
norharman
-
non competitive, competitive for the ferric enzyme, 0.1 M potassium phosphate buffer (pH 5.5-8), 0.1 M Tris-HCl buffer (pH 7.5-8), 25°C
norharman
-
can bind to the ferric and ferrous enzyme to from a quarternary complex
O2
-
-
O2
inhibition of mutant forms H55A and H55S at high concentrations
Sodium azide
-
1 mM causes 20% inhibition
Superoxide dismutase
-
80-98% inhibition
-
Superoxide dismutase
-
-
-
Superoxide dismutase
-
can be inhibited by diethyldithiocarbamate
-
Tiron
-
10 mM, 2% inhibition of cleavage of D-tryptophan, 6% inhibition of cleavage of L-tryptophan
Tiron
-
1 mM causes 40% inhibition
tryptamine
-
1 mM, 23% inhibition
tryptamine
-
0.1 mM, 16% inhibition of cleavage of D-tryptophan, 11% inhibition of cleavage of L-tryptophan
additional information
-
synthesis and inhibition study of tryptophan 2,3-dioxygenase with 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives, overview. No inhibition by 7b
-
additional information
-
no inhibition by D-5-hydroxytryptophan
-
additional information
-
not inhibited by indo-3-acetamide, beta-indoylacetonitrile snd 3-beta-indoleacrylic acid
-
additional information
-
not inhibited by 6-nitro-D-tryptophan and indole-nitrogen substituted analogues of trytophan
-
additional information
review article sumarizing data of many inhibitors of indoleamine 2,3-dioxygenase
-
additional information
-
sodium butyrate does not inhibit the activity of IDO
-
additional information
-
the traditional Chinese medicinal prescription Oren-gedoku-to significantly inhibits recombinant human IDO-1 activity in vitro
-
additional information
not inhibited by 1-methyl-D-tryptophan
-
additional information
F5H5G0
no inhibition by phenylthiohydantoin-Trp; no inhibition by phenylthiohydantoin-Trp
-
additional information
no inhibition by phenylthiohydantoin-Trp; no inhibition by phenylthiohydantoin-Trp
-
additional information
-
no inhibition by phenylthiohydantoin-Trp; no inhibition by phenylthiohydantoin-Trp
-
additional information
-
structure-activity relationship and enzyme kinetics of 4-aryl-1H-1,2,3-triazoles as indoleamine 2,3-dioxygenase inhibitors, molecular docking studies, overview. An electron-withdrawing group with low steric hindrance near the NH group of triazoles is necessary for the IDO inhibition. No inhibition by 5-(4-methylphenyl)-1H-1,2,3-triazole, methyl 4-(1H-1,2,3-triazol-5-yl)benzoate, 4-bromo-5-phenyl-1H-1,2,3-triazole, 4-chloro-5-phenyl-1H-1,2,3-triazole, 1H-benzotriazol-1-ol, and 5-(4-bromophenyl)-1H-tetrazole
-
additional information
-
the dioxygenase enzyme activity is inhibited by free radical scavengers. Protection of the dioxygenase enzyme function by L-Trp coincides with its oxidation into oxindolylalanine and kynurenine and the formation of a compound II-type ferryl-oxo heme
-
additional information
no inhibition of IDO1 by 1-methy-D-tryptophan; no inhibition of IDO1 by L-tryptophan
-
additional information
no inhibition of IDO1 by 1-methy-D-tryptophan; no inhibition of IDO1 by L-tryptophan
-
additional information
-
no inhibition of IDO1 by 1-methy-D-tryptophan; no inhibition of IDO1 by L-tryptophan
-
additional information
structure-activity relationships of phenyl benzenesulfonylhydrazides as indoleamine 2,3-dioxygenase inhibitors, overview. Coupling reactions between various benzenesulfonyl chlorides and phenylhydrazides are utilized to synthesize the sulfonylhydrazides bearing various substituents. EC50 values, overview
-
additional information
NCI library inhibitor screening, and analysis of active site-inhibitor interactions, overview. Importance of Ser167 and Cys129 residues in the IDO1 active site for inhibitor binding. Structure-activity relationship studies propose substituents interacting with Ser167 on four investigated IDO1 inhibitors. Three of these four Ser167 interactions associate with an increased IDO1 inhibition and are correctly predicted by molecular docking supporting Ser167 as an important mediator of potency for IDO1 inhibitors. IC50 values in presence or absence of Tween 20 and reduced glutathione
-
additional information
identification of substituted naphthotriazolediones as tryptophan 2,3-dioxygenase (TDO) inhibitors through structure-based virtual screening, homology modeling and virtual screening, ligand docking analysis, overview
-
additional information
suppressive effect of plant extracts or phytochemicals on IDO1 induction and activity. The methanol extracts of Myoga flower buds, which are traditional Japanese foods, and labdane-type diterpene galanal derived from Myoga flowers significantly suppress IDO1 activity
-
additional information
-
suppressive effect of plant extracts or phytochemicals on IDO1 induction and activity. The methanol extracts of Myoga flower buds, which are traditional Japanese foods, and labdane-type diterpene galanal derived from Myoga flowers significantly suppress IDO1 activity
-
additional information
-
inhibition of indoleamine 2,3-dioxygenase activity by fatty acids, eicosanoids and prostaglandins, structure-function-analysis, overview. No inhibition by (6Z,9Z,12Z)-octadecatrienoic and (6Z,9Z,12Z,15Z)-octadecatetraenoic
-
additional information
a high throughput virtual screening cascade protocol is validated and can be employed in discovery of IDO1 inhibitors
-
additional information
1H-indazole-4-amines inhibit both human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) by a mechanism involving direct coordination with the heme ferrous and ferric states
-
additional information
-
1H-indazole-4-amines inhibit both human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) by a mechanism involving direct coordination with the heme ferrous and ferric states
-
additional information
-
inhibition of indoleamine 2,3-dioxygenase may be developed as an anticancer immunotherapeutic strategy
-
additional information
-
not inhibited by superoxide dismutase
-
additional information
-
review article sumarizing data of many inhibitors of indoleamine 2,3-dioxygenase
-
additional information
-
3-indoleethanol and indole affect the L-tryptophan affinity of the ferrous enzyme, indole enhances affinity of enzyme for cyanide and azide and norharman, L-tryptophan lowers norharman affinity for the ferrous dioxygenase
-
additional information
-
not inhibited by catalase and D-tryptophan
-
additional information
-
catabolite repression of the pathway by glucose and glutamate, arginine does not cause repression, no inhibition by D-tryptophan
-
additional information
-
no inhibition by D-5-hydroxytryptophan
-
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0.0234
(-)-kurarinone
Homo sapiens
pH 6.5, 37°C
-
0.00317
(1R,2S)-2-([[6-(trifluoromethyl)-1H-indazol-4-yl]amino]methyl)cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.00123
(1R,2S)-2-[[(5-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.03801
(1R,2S)-2-[[(5-bromo-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.06604
(1R,2S)-2-[[(5-chloro-1H-indazol-7-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.00064
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.00578
(1R,2S)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexyl acetate
Homo sapiens
22°C, pH 6.5
-
0.1783
(1R,2S)-2-[[(6-chloro-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.00187
(1R,2S)-2-[[(6-methyl-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.00285
(1S,2R)-2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.0035
(2,4-dichlorophenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0012
(2-chlorophenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.00012
(2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.0314
(2S)-2'-methoxy kurarinone
Homo sapiens
pH 6.5, 37°C
-
0.0001
(3,4-dichlorophenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.5
(3-hydroxyphenyl)(phenyl)methanone
Homo sapiens
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
0.000512
(3R,4S and 3S,4R)-3-bromo-4-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000361
(3R,4S and 3S,4R)-3-hydroxy-2,2-dimethyl-4-morpholino-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00396
(3R,4S and 3S,4R)-3-hydroxy-4-methoxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000183
(3R,4S and 3S,4R)-4-(allylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000252
(3R,4S and 3S,4R)-4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00345
(3R,4S and 3S,4R)-4-(benzylthio)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000082
(3R,4S and 3S,4R)-4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.0015
(3S,4S and 3R,4R)-3,4-dihydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
alpha-lapachone
0.0011
(3S,4S and 3R,4R)-3-hydroxy-2,2-dimethyl-4-morpholino-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000976
(3S,4S and 3R,4R)-3-hydroxy-4-methoxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000186
(3S,4S and 3R,4R)-4-(allylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.000055
(3S,4S and 3R,4R)-4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00109
(3S,4S and 3R,4R)-4-(benzyloxy)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00212
(3S,4S and 3R,4R)-4-(benzylthio)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00013
(3S,4S)-4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.0032
(4-chlorophenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
(4-chlorophenyl)methanol
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0018
(4-fluorophenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0014
(4-methoxyphenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0013
(4-methylphenyl)methanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.00045
(4E,4'E)-4,4'-bis(isopropylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
Homo sapiens
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
0.00052
(4E,4'E)-4,4'-bis(pentan-3-ylimino)-2,2'-binaphthyl-1,1'-(4H,4'H)-dione
Homo sapiens
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
0.00179
(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)boronic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.0002
(E)-4-(isopropylimino)-2-methylnaphthalen-1(4H)-one
Homo sapiens
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
0.09
(R)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
Homo sapiens
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
0.00034
(S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(1,4-dihydroxy-3-methylnaphthalen-2-ylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid
Homo sapiens
-
0.00088
(S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-ylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid
Homo sapiens
-
0.06
(S)-2-amino-N-(4-hydroxynaphth-1-yl)propanamide
Homo sapiens
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
0.0071
1,2-naphthoquinone
Homo sapiens
-
0.00099
1,4-naphtho-quinone
Homo sapiens
-
0.0293
1,6,6-trimethyl-10,11-dioxo-2-(thiophen-3-yl)-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
Homo sapiens
37°C, pH 6.5
-
0.0215
1,6,6-trimethyl-10,11-dioxo-2-phenyl-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
Homo sapiens
37°C, pH 6.5
-
0.00571
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl 1,3-thiazole-2-carboxylate
Homo sapiens
37°C, pH 6.5
-
0.00372
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl acetate
Homo sapiens
37°C, pH 6.5
-
0.00705
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl cyclopropanecarboxylate
Homo sapiens
37°C, pH 6.5
-
0.0046
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl furan-3-carboxylate
Homo sapiens
37°C, pH 6.5
-
0.00274
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl hydroxyacetate
Homo sapiens
37°C, pH 6.5
-
0.00472
1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl propanoate
Homo sapiens
37°C, pH 6.5
-
0.00084
1,6,6-trimethylphenanthro[1,2-b]furan-7,10,11(6H)-trione
Homo sapiens
37°C, pH 6.5
-
0.05
1-(1,3-benzothiazol-2-ylsulfanyl)-N,N-dimethylmethanamine
Homo sapiens
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
0.000809
1-(2-methylbenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.003163
1-(3-bromobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.000767
1-(3-chlorobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.000602
1-(3-[(4-acetyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.00064
1-(3-[(4-methyl-1-piperazinyl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.01
1-(4-bromobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
above, pH 8.0, 37°C
0.000339
1-(4-bromophenyl)-2-[[5-(4-chlorophenyl)[1,3]thiazolo[2,3-c]-[1,2,4]triazol-3-yl]sulfanyl]ethanone
Homo sapiens
pH and temperature not specified in the publication
-
0.1
1-(4-chlorobenzyl)urea
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
1-(4-chlorophenyl)methanamine
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
1-(4-chlorophenyl)thiourea
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0000164
1-(4-cyanophenyl)-3-(3-(cyclopropylethynyl)imidazo[2,1-b]thiazol-5-yl)thiourea
Homo sapiens
pH and temperature not specified in the publication
-
0.002587
1-(4-fluorobenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.00177
1-(4-methylbenzyl)-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.001097
1-(4-[(4-acetylpiperazin-1-yl)carbonyl]benzyl)-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.001593
1-(4-[(4-methoxypiperidin-1-yl)carbonyl]benzyl)-1Hnaphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.00037
1-(hydroxymethyl)-6,6-dimethylphenanthro[1,2-b]furan-7,10,11(6H)-trione
Homo sapiens
37°C, pH 6.5
-
0.032
1-benzyl-5-phenyl-1H-imidazole
Homo sapiens
-
0.000081
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol
Homo sapiens
22°C, pH 6.5
0.4233
1-methyl-tryptophan
Homo sapiens
pH 6.5, 37°C
0.004612
1-[(3-methylphenyl)methyl]-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.01
1-[(4-chlorophenyl)methyl]-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
above, pH 8.0, 37°C
0.00057
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.00048
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.00055
1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]proline
Homo sapiens
pH and temperature not specified in the publication
-
0.1
1-[2-(4-chlorophenyl)ethyl]thiourea
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.000936
1-[3-(4-morpholinylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.000982
1-[4-(morpholin-4-ylcarbonyl)benzyl]-1H-naphtho[2,3-d]-[1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.002069
1-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]-1H-naphtho-[2,3-d][1,2,3]triazole-4,9-dione
Homo sapiens
pH 8.0, 37°C
0.000028
1-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-3-(4-methylphenyl)imidazolidin-2-one
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0044 - 0.013
15-deoxy-DELTA12,14-prostaglandin
2.57
1H-benzotriazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.00495
2,2-dimethyl-1a,9b-dihydro-2H-benzo[g]oxireno[c]chromene-4,9-dione
Homo sapiens
pH and temperature not specified in the publication
0.000214
2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
dehydro-alpha-lapachone
0.00434
2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00495
2,2-dimethyl-3,4-epoxy-2H-naphtho[2,3-b]pyran-5,10-dione
Homo sapiens
-
0.00028
2,3-dichloro-1,4-naphthoquinone
Homo sapiens
-
0.0004
2,4-dichlorobenzyl carbamimidothioate hydrobromide
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0053
2-(1H-imidazol-4-yl)benzene-1,3-diol
Homo sapiens
-
0.025
2-(1H-imidazol-4-yl)benzenethiol
Homo sapiens
-
0.0048
2-(1H-imidazol-4-yl)phenol
Homo sapiens
-
0.035
2-(1H-pyrazol-3-yl)phenol
Homo sapiens
-
0.1
2-(2-chlorophenyl)ethyl carbamimidothioate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
2-(3-chlorophenyl)ethyl carbamimidothioate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
2-(4-chlorophenyl)ethanamine
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.057
2-(4-chlorophenyl)ethyl carbamimidothioate hydrobromide
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.000922
2-(4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]-triazol-1-yl)methyl]phenyl)-N,N-diethylacetamide
Homo sapiens
pH 8.0, 37°C
0.25
2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide
0.00087
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (2-hydroxyphenyl)acetate
Homo sapiens
pH and temperature not specified in the publication
-
0.00034
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-cyanophenyl)acetate
Homo sapiens
pH and temperature not specified in the publication
-
0.0002
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl (4-hydroxyphenyl)acetate
Homo sapiens
pH and temperature not specified in the publication
-
0.00058
2-([[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]amino)-2-oxoethyl phenylacetate
Homo sapiens
pH and temperature not specified in the publication
-
0.4
2-amino-3-hydroxy-N-(4-hydroxynaphthalen-1-yl)propanamide
Homo sapiens
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
0.105
2-amino-N-(4-hydroxynaphth-1-yl)acetamide
Homo sapiens
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
0.01
2-chlorobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.675
2-Hydroxy-1,4-naphthoquinone
Homo sapiens
-
0.05
2-mercaptobenzothiazole
Homo sapiens
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
0.00072
2-methoxy-1,4-naphthoquinone
Homo sapiens
-
0.0011
2-methyl-1,4-naphthoquinone
Homo sapiens
-
0.0011
2-methylnaphthalene-1,4-dione
Homo sapiens
pH and temperature not specified in the publication
1
2-phenoxyaniline
Homo sapiens
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
0.01309
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(3-chlorophenyl)ethan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.1371
2-[(6-bromo-1H-indazol-4-yl)amino]-1-(4-hydroxyphenyl)ethan-1-one
Homo sapiens
22°C, pH 6.5
-
0.01833
2-[(6-bromo-1H-indazol-4-yl)amino]-2-(3-chlorophenyl)ethan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.04287
2-[(6-bromo-1H-indazol-4-yl)amino]-2-phenylethan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.0000787
2-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.00412
2-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexan-1-ol
Homo sapiens
22°C, pH 6.5
-
0.000022
3'-[[(2-chlorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00005
3'-[[(2-fluorophenyl)carbamoyl]amino]-4-methoxy-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000042
3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(2-methylpropyl)(propan-2-yl)amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000159
3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(4aS,8aS)-octahydroquinolin-1(2H)-yl][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.017
3,4-dichlorobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.68 - 0.708
3-(1H-1,2,3-triazol-5-yl)pyridine
0.825
3-(1H-imidazol-4-yl)benzaldehyde
0.0076
3-(1H-imidazol-4-yl)benzenethiol
Homo sapiens
-
0.041
3-(1H-imidazol-4-yl)benzonitrile
Homo sapiens
-
0.365
3-(1H-imidazol-4-yl)phenol
Homo sapiens
-
0.00051
3-(2-aminoethyl)-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.000379
3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazole
Homo sapiens
pH and temperature not specified in the publication
-
0.0077
3-(4H-imidazol-4-yl)benzenethiol
Homo sapiens
-
0.0046
3-chlorobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.00036
3-hydroxy-2,2-dimethyl-4-(morpholin-4-yl)-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.00396
3-hydroxy-4-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.161
3-phenylpyridine
Homo sapiens
-
0.000977
3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
Homo sapiens
pH 8.0, 37°C
0.001242
3-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
Homo sapiens
pH 8.0, 37°C
0.000065
3-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.0015
3-[2-(cyclohexylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00226
3-[2-(diethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.0005
3-[2-(dimethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00016
3-[2-(ethylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00088
3-[2-(propylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00056
3-[2-(tert-butylamino)ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.004
3-[2-[(2-phenylethyl)amino]ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00051
3-[2-[(propan-2-yl)amino]ethyl]-5-(pyridin-3-yl)-1H-indole-4,7-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.000141
3-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]propanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.00016
4'-(2,3-dimethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0024
4'-(2-chlorophenoxy)-3'-([[4-(2-hydroxypropan-2-yl)phenyl]carbamoyl]amino)-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00083
4'-(2-chlorophenoxy)-3'-[[(4-chlorophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.006
4'-(2-chlorophenoxy)-3'-[[(4-cyanophenyl)carbamoyl]amino]-4-methoxy[1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0021
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methoxyphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00084
4'-(2-chlorophenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00054
4'-(2-ethylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0006
4'-(2-tert-butylanilino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0045
4'-(2-tert-butylphenoxy)-2-fluoro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00007
4'-(2-tert-butylphenoxy)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0024
4'-(2-tert-butylphenoxy)-4-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00012
4'-(2-tert-butylphenoxy)-4-ethoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00035
4'-(2-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00025
4'-(2-tert-butylphenoxy)-5-chloro-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00069
4'-(3-tert-butylphenoxy)-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000504
4'-(cyclohexylamino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000045
4'-(dibutylamino)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00028
4'-[(2,3-dihydro-1H-inden-4-yl)oxy]-4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000013
4'-[bis(2-methylpropyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000661
4'-[bis(2-methylpropyl)amino]-N-(methanesulfonyl)-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000348
4'-[bis(cyclopropylmethyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000014
4'-[cyclohexyl(methyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000023
4'-[cyclopentyl(ethyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.005
4-(1H-1,2,3-triazol-5-yl)pyridine
Homo sapiens
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
1.2
4-(1H-imidazol-4-yl)phenol
Homo sapiens
-
0.734
4-(2,6-dimethoxyphenyl)-1H-imidazole
Homo sapiens
-
0.003
4-(2-(diethylamino)ethylamino)-1-naphthol
Homo sapiens
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
0.038
4-(2-(methylthio)phenyl)-1H-imidazole
Homo sapiens
-
0.179
4-(2-fluorophenyl)-1H-imidazole
0.0125
4-(2-hydroxyethoxy)-1-naphthol
Homo sapiens
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
0.073
4-(3-(methylthio)phenyl)-1H-imidazole
Homo sapiens
-
0.00033
4-(3-chlorophenyl)-imidazole
Homo sapiens
pH and temperature not specified in the publication
-
0.06
4-(3-fluorophenyl)-1H-imidazole
Homo sapiens
-
0.209
4-(4-(methylthio)phenyl)-1H-imidazole
Homo sapiens
-
0.0034
4-(4-bromophenyl)-1,3-thiazole-2(3H)-thione
Homo sapiens
pH 6.5, 22°C
-
0.0026
4-(4-chlorophenyl)-1,3-thiazole-2(3H)-thione
Homo sapiens
pH 6.5, 22°C
-
0.123
4-(4-fluorophenyl)-1H-imidazole
Homo sapiens
-
0.0059
4-(4-methylphenyl)-1,3-thiazole-2(3H)-thione
Homo sapiens
pH 6.5, 22°C
-
0.0025
4-(benzylamino)-1-naphthol
Homo sapiens
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
0.000055 - 0.00025
4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
0.00013
4-(butylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.015
4-(cyclohexylamino)-1-naphthol
Homo sapiens
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
1
4-(dimethylamino)naphthalen-1-ol
Homo sapiens
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
0.016
4-(ethylamino)-1-naphthol
Homo sapiens
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
0.025
4-(isobutylamino)-1-naphthol
Homo sapiens
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
0.0025
4-(isopropylamino)-1-naphthol
Homo sapiens
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
0.000043
4-(methanesulfonyl)-N'-(3-methylphenyl)benzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0125
4-(methylamino)naphthalen-1-ol
Homo sapiens
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
0.0035
4-(pent-3-ylamino)-1-naphthol
Homo sapiens
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
0.1
4-(phenylcarbonyl)benzyl carbamimidothioate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
4-(propan-2-yl)benzyl carbamimidothioate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0045
4-(propylamino)-1-naphthol
Homo sapiens
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
0.004
4-(tert-butylamino)naphthalen-1-ol
Homo sapiens
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
0.422
4-(thiophen-2-yl)-1H-imidazole
0.0026
4-(trifluoromethyl)benzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.03022
4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylic acid
Homo sapiens
22°C, pH 6.5
-
0.003
4-amino-1-naphthol
Homo sapiens
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
0.0021
4-amino-N'-hydroxy-N-(3-isopropylphenyl)-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.0044
4-amino-N'-hydroxy-N-(3-methoxyphenyl)-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.00055
4-amino-N'-hydroxy-N-(3-methylphenyl)-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.0032
4-amino-N'-hydroxy-N-phenyl-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.0065
4-amino-N-(2-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.000059
4-amino-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.000073
4-amino-N-(3-bromophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.000067
4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.0014
4-amino-N-(3-chlorophenyl)-1,2,5-oxadiazole-3-carbohydrazonamide
Homo sapiens
-
-
0.000086
4-amino-N-(3-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.00043
4-amino-N-(3-ethylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.0005
4-amino-N-(3-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.025
4-amino-N-(3-tert-butylphenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
0.006
4-amino-N-(4-chlorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
-
-
1.028
4-bromo-5-(4-methylphenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.000085
4-bromo-N'-(4-bromophenyl)benzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0013
4-bromobenzyl carbamimidothioate hydrobromide
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
4-chlorobenzenesulfonic acid
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0019
4-chlorobenzenethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0022
4-chlorobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.021
4-chlorobenzyl N,N'-dimethylcarbamimidothioate - 1-chlorotetraoxidane (1:1)
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.00011
4-chlorophenyl-1,2,3-triazol-4-amine
Homo sapiens
pH and temperature not specified in the publication
-
0.000059
4-cyano-N'-(3-methylphenyl)benzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.019
4-cyanobenzyl carbamimidothioate hydrobromide
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.016
4-ethylbenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.026
4-fluoro-2-(1H-pyrazol-3-yl)phenol
0.013
4-fluorobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.4
4-hydroxycarbazole
Homo sapiens
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
1.371
4-iodo-5-phenyl-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.0055
4-methoxy-1-naphthylamine
Homo sapiens
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
0.000062
4-methoxy-3'-[(phenylcarbamoyl)amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000049
4-methoxy-3'-[[(2-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0001
4-methoxy-3'-[[(3-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00033
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-(2-propylphenoxy)[1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0001
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[(5,6,7,8-tetrahydronaphthalen-1-yl)oxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00034
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-(propan-2-yl)phenoxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00005
4-methoxy-3'-[[(4-methylphenyl)carbamoyl]amino]-4'-[2-methyl-3-[(prop-2-yn-1-yl)oxy]phenoxy][1,1'-biphenyl]-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.052
4-methoxybenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.03
4-methylbenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.533
4-nitro-5-(4-nitrophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.011
4-nitrobenzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
1
4-phenyl-1,3-thiazol-2-amine
Homo sapiens
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
0.024
4-phenyl-1,3-thiazole-2(3H)-thione
Homo sapiens
pH 6.5, 22°C
-
0.05
4-phenyl-1,3-thiazole-2-thiol
Homo sapiens
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
0.00048 - 0.048
4-phenylimidazole
0.1
4-tert-butylbenzyl carbamimidothioate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.05718
4-[(1Z)-2-[(6-bromo-1H-indazol-4-yl)amino]-N-hydroxyethanimidoyl]phenol
Homo sapiens
22°C, pH 6.5
-
0.001928
4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]-N,N-diethylbenzamide
Homo sapiens
pH 8.0, 37°C
0.002323
4-[(4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-1-yl)methyl]benzoic acid
Homo sapiens
pH 8.0, 37°C
0.1
4-[(carbamimidoylsulfanyl)methyl]benzoic acid hydrochloride
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0002
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzamide
Homo sapiens
pH and temperature not specified in the publication
-
0.000199 - 0.000203
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzene-1-sulfonamide
-
0.0000836
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
-
0.000061
4-[2-(4-bromophenyl)hydrazinesulfonyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.038
4-[2-(methylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
pH and temperature not specified in the publication
0.073
4-[3-(methylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
pH and temperature not specified in the publication
0.00564
4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]phenol
Homo sapiens
22°C, pH 6.5
-
0.148
5-(2-bromophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.086
5-(2-chlorophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
1.028
5-(2-methoxyphenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
1.256
5-(4-bromophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.817
5-(4-chlorophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.000256
5-(4-chlorophenyl)-3-[(2-methylpropyl)sulfanyl][1,3]thiazolo-[2,3-c][1,2,4]triazole
Homo sapiens
pH and temperature not specified in the publication
-
0.58
5-(4-fluorophenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
6
5-(4-methoxyphenyl)-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.04
5-(ethylamino)quinolin-8-ol
Homo sapiens
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
0.015
5-(isopropylamino)quinolin-8-ol
Homo sapiens
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
0.003
5-amino-8-hydroxyquinoline
Homo sapiens
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
0.05
5-chloro-1,3-benzothiazole-2(3H)-thione
Homo sapiens
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
0.001
5-hydroxy-1,4-naphthoquinone
Homo sapiens
-
0.06 - 0.143
5-phenyl-1H-1,2,3-triazole
0.0088
5-[(2E)-2-[(4-bromophenyl)methylidene]hydrazinyl]-1-(naphthalen-1-yl)tetrazolidine
Homo sapiens
pH 6.5, 37°C
-
0.00945
6-bromo-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00109
6-bromo-N-(cyclohexylmethyl)-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.03207
6-bromo-N-[(1,4-dioxaspiro[4.5]decan-6-yl)methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.203
6-bromo-N-[(1R,2R)-2-hydroxycyclohexyl]-1H-indazole-4-carboxamide
Homo sapiens
22°C, pH 6.5
-
0.05155
6-bromo-N-[(pyridin-2-yl)methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.1049
6-bromo-N-[(pyrrolidin-3-yl)methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.0555
6-bromo-N-[[(1S,2R)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00029
6-bromo-N-[[(1S,2S)-2-chlorocyclohexyl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.01736
6-bromo-N-[[(2R)-piperidin-2-yl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.05645
6-bromo-N-[[(2R)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.01375
6-bromo-N-[[(2S)-piperidin-2-yl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00474
6-bromo-N-[[(2S)-pyrrolidin-2-yl]methyl]-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00019
6-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00019
6-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.00213
6-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.0031
7-hydroxy-1,6,6-trimethyl-6,7-dihydrophenanthro[1,2-b]furan-10,11-dione
Homo sapiens
37°C, pH 6.5
-
0.00552
7-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00302
7-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.01309
8-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indolo[2,1-b]quinazoline-6,12-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00078
8-fluoro-2-[(1H-1,2,3-triazol-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione
Homo sapiens
pH and temperature not specified in the publication
-
0.00046
8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbaldehyde
Homo sapiens
pH and temperature not specified in the publication
-
0.000534
8-fluorotryptanthrin
Homo sapiens
pH and temperature not specified in the publication
-
0.002 - 0.00205
8-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
0.000933
8-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.2
9-fluorenone
Homo sapiens
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
0.00283
9-hydroxy-1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione
Homo sapiens
37°C, pH 6.5
-
0.000121
9-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
alpha-caryopterone
1
9-hydroxyfluorene
Homo sapiens
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
0.00292
9-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
0.000017
antisense oligonucleotide A06007H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000036
antisense oligonucleotide A06008H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000011
antisense oligonucleotide A06030H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000049
antisense oligonucleotide A06043H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000205
antisense oligonucleotide A06044H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000078
antisense oligonucleotide A06045H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000368
antisense oligonucleotide A07006H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000842
antisense oligonucleotide A07058H
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
1
benzophenone
Homo sapiens
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
0.061
benzyl carbamimidothioate hydrochloride
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0093
Berberine
Homo sapiens
-
pH and temperature not specified in the publication
0.07
Dichlorophene
Homo sapiens
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
0.00001 - 0.00009
epacadostat
-
0.00019
ethyl (2E)-3-(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)prop-2-enoate
Homo sapiens
pH and temperature not specified in the publication
-
0.00747
ethyl 1,6,6-trimethyl-10,11-dioxo-6,7,8,9,10,11-hexahydrophenanthro[1,2-b]furan-9-yl (2E)-but-2-enedioate
Homo sapiens
37°C, pH 6.5
-
2
ethyl 1-(4-chlorophenyl)-1H-1,2,3-triazole-4-carboxylate
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.0077
galanal
Homo sapiens
pH 6.5, 37°C, recombinant His-tagged enzyme
0.00088
gamma-glutamyl-S-(3-methyl-1,4-dioxo-1,4-dihydronaphthalen-2-yl)cysteinylglycine
Homo sapiens
pH and temperature not specified in the publication
0.000097
INCB024360
Homo sapiens
pH and temperature not specified in the publication
-
0.0077
kushenol E
Homo sapiens
pH 6.5, 37°C
0.0254
kushenol F
Homo sapiens
pH 6.5, 37°C
-
0.00064
menadione
Homo sapiens
in PBS buffer (pH 7.4), at 37°C
0.00143
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-3-carboxylate
Homo sapiens
pH and temperature not specified in the publication
-
0.0012
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]piperidine-4-carboxylate
Homo sapiens
pH and temperature not specified in the publication
-
0.00046
methyl 1-[(8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl]prolinate
Homo sapiens
pH and temperature not specified in the publication
-
0.000247
methyl 2-methyl-5,10-dioxo-5,10-dihydro-2H-benzo[g]chromene-2-carboxylate
Homo sapiens
-
0.000121
methyl 3-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]propanoate
Homo sapiens
pH and temperature not specified in the publication
0.00366
methyl 4-([[(1S,2R)-2-hydroxycyclohexyl]methyl]amino)-1H-indazole-6-carboxylate
Homo sapiens
22°C, pH 6.5
-
0.1
methyl 4-[(carbamimidoylsulfanyl)methyl]benzenesulfinate hydrobromide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
methyl N-(4-chlorophenyl)carbamimidothioate hydroiodide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.1
methyl N-[2-(4-chlorophenyl)ethyl]carbamimidothioate hydroiodide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0216 - 0.0826
methyl thiohydantoin-Trp
0.000059
N'-(3-methylphenyl)-4-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000176
N'-(4-bromophenyl)-4-cyanobenzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.001431
N'-(4-bromophenyl)-4-methoxybenzene-1-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000172
N'-(4-bromophenyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000405
N'-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N-methyl-N-(4-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
1
N,N-dimethyl-1-[(4-phenyl-1,3-thiazol-2-yl)sulfanyl]methanamine
Homo sapiens
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
0.003 - 0.25
N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
0.0000093 - 0.0000132
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
-
0.00000546 - 0.0000127
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
-
0.0000323 - 0.000112
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
-
0.000056
N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[[2-(sulfamoylamino)ethyl]amino]-1,2,5-oxadiazole-3-carboximidamide
Homo sapiens
22°C, pH 6.5
-
0.000076
N-(4'-[bis(2-methylpropyl)amino]-3'-[[(4-methylphenyl)carbamoyl]amino][1,1'-biphenyl]-2-yl)-1,1,1-trifluoromethanesulfonamide
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0029
N-(4-bromophenyl)-N'-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.044
N-(4-hydroxy-1-naphthyl)ethane-1,2-diaminium chloride
Homo sapiens
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
0.005
N-(4-hydroxy-1-naphthyl)propane-1,3-diaminium chloride
Homo sapiens
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
0.2
N-(4-hydroxynaphthalen-1-yl)pyrrolidine-2-carboxamide
Homo sapiens
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
0.001605
N-(4-[2-[4-(trifluoromethyl)phenyl]hydrazinesulfonyl]phenyl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00161
N-(4-[[(6-bromo-1H-indazol-4-yl)amino]methyl]cyclohexylidene)hydroxylamine
Homo sapiens
22°C, pH 6.5
-
0.25
N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
0.4
N-phenyl-p-phenylenediamine
Homo sapiens
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
0.0238
N-[(1,3-benzothiazol-2-yl)sulfanyl]-2-nitrobenzene-1-sulfonamide
Homo sapiens
pH 6.5, 37°C
-
0.1127
N-[(azetidin-3-yl)methyl]-6-bromo-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00077
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]-2,2-dimethylpropanamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00136
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00208
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00351
N-[2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]benzenesulfonamide
Homo sapiens
pH and temperature not specified in the publication
-
0.000071
N-[4-(2-phenylhydrazinesulfonyl)phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.001
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(2-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00057
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(3-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0018
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methoxyphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.00079
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0015
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-phenylurea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0026
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(difluoromethoxy)phenyl]urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.004
N-[4-(2-tert-butylphenoxy)[1,1'-biphenyl]-3-yl]-N'-[4-(trifluoromethoxy)phenyl]urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000608
N-[4-[2-(2,4-difluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000247
N-[4-[2-(3,4-dichlorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000352
N-[4-[2-(3,5-dichlorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.001746
N-[4-[2-(3,5-difluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000128
N-[4-[2-(3-bromo-4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000255
N-[4-[2-(3-bromophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N-[4-[2-(3-chloro-4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000122
N-[4-[2-(3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00008
N-[4-[2-(3-methylphenyl)hydrazinesulfonyl]benzoyl]glycine
Homo sapiens
pH and temperature not specified in the publication
0.000049
N-[4-[2-(3-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000205
N-[4-[2-(4-bromo-3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
N-[4-[2-(4-bromo-3-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00023
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-chlorophenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.000146
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-cyanophenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.00048
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-fluorophenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.0000461
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-methoxyphenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.0000536
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(3-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.000184
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-chlorophenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.0000607
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-methoxyphenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.0000703
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-(4-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication
-
0.000157
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-butylurea
Homo sapiens
pH and temperature not specified in the publication
-
0.000161
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-cyclohexylurea
Homo sapiens
pH and temperature not specified in the publication
-
0.0000726
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-[3-(1H-tetrazol-5-yl)phenyl]urea
Homo sapiens
pH and temperature not specified in the publication
-
0.000207
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]-N'-[4-(1H-tetrazol-5-yl)phenyl]urea
Homo sapiens
pH and temperature not specified in the publication
-
0.00013
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000132
N-[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000194
N-[4-[2-(4-chloro-3-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000155
N-[4-[2-(4-chlorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.005667
N-[4-[2-(4-cyanophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000079
N-[4-[2-(4-fluorophenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000254
N-[4-[2-(4-methoxyphenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000051
N-[4-[2-(4-methylphenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.002475
N-[4-[2-(4-sulfamoylphenyl)hydrazinesulfonyl]phenyl]acetamide
Homo sapiens
pH and temperature not specified in the publication
0.000005 - 0.000097
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-2-(4-methylphenyl)acetamide
-
0.000004
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-N'-(4-methylphenyl)urea
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.0007
N-[[(1S,2R)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00142
N-[[(1S,2S)-2-aminocyclohexyl]methyl]-6-bromo-1H-indazol-4-amine
Homo sapiens
22°C, pH 6.5
-
0.00008
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-4-oxobutanamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00069
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-(phenylacetyl)glycinamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00073
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(2-nitrophenyl)acetyl]glycinamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00063
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(3-nitrophenyl)acetyl]glycinamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00081
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-methyl-N2-[(4-nitrophenyl)acetyl]glycinamide
Homo sapiens
pH and temperature not specified in the publication
-
0.00045
N-[[3-(4-bromophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]methyl]-N2-[(3-hydroxyphenyl)acetyl]-N2-methylglycinamide
Homo sapiens
pH and temperature not specified in the publication
-
0.0015
naphthalene-1,4-diol
Homo sapiens
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
0.00099
naphthalene-1,4-dione
Homo sapiens
pH and temperature not specified in the publication
0.0235
noranhydroicaritin
Homo sapiens
pH 6.5, 37°C
0.0017
phenylmethanethiol
Homo sapiens
-
in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.05
primaquine
Homo sapiens
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
0.001202
propan-2-yl 4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzoate
Homo sapiens
pH and temperature not specified in the publication
-
0.006 - 0.0095
prostaglandin (19R)-hydroxy-PGE2
0.0067 - 0.03
prostaglandin 13,14-dihydro-15-oxo-PGE2
0.0068 - 0.009
prostaglandin 15-oxo-PGE2
0.0076 - 0.0231
prostaglandin 15-oxo-PGF2alpha
0.0074 - 0.0112
prostaglandin 20-hydroxy PGE2
0.0046 - 0.0071
prostaglandin DELTA12-PGJ2
0.0049 - 0.0078
prostaglandin PGA2
0.0041 - 0.0074
prostaglandin PGD2
0.0047 - 0.0057
prostaglandin PGD2 ethanolamide
0.01 - 0.0221
prostaglandin PGE2
0.0046 - 0.0063
prostaglandin PGE2 ethanolamide
0.0071 - 0.0074
prostaglandin PGF2beta
0.0092 - 0.0112
prostaglandin PGG2
0.0072 - 0.0096
prostaglandin PGH2
0.0042 - 0.0067
prostaglandin PGJ2
0.75
quinolin-8-ol
Homo sapiens
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
0.1
sodium 4-chlorobenzenesulfinate
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM potassium phosphate buffer (pH 6.5), 20 mM ascorbic acid (neutralized with NaOH and HCl), 0.01 mM methylene blue, at 37°C
0.0193
sophoraflavanone B
Homo sapiens
pH 6.5, 37°C
0.00902
tert-butyl 3-[[(6-bromo-1H-indazol-4-yl)amino]methyl]pyrrolidine-1-carboxylate
Homo sapiens
22°C, pH 6.5
-
0.00294
tert-butyl [2-(4,7-dioxo-5-phenyl-4,7-dihydro-1H-indol-3-yl)ethyl]carbamate
Homo sapiens
pH and temperature not specified in the publication
-
0.0019
tert-butyl [2-[4,7-dioxo-5-(pyridin-3-yl)-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
Homo sapiens
pH and temperature not specified in the publication
-
0.00209
tert-butyl [2-[5-(2-fluorophenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
Homo sapiens
pH and temperature not specified in the publication
-
0.00238
tert-butyl [2-[5-(2-methoxyphenyl)-4,7-dioxo-4,7-dihydro-1H-indol-3-yl]ethyl]carbamate
Homo sapiens
pH and temperature not specified in the publication
-
0.001
vitamin K3
Homo sapiens
-
0.000125
[4-[2-(4-bromophenyl)hydrazinesulfonyl]phenoxy]acetic acid
Homo sapiens
pH and temperature not specified in the publication
additional information
additional information
-
0.0044
15-deoxy-DELTA12,14-prostaglandin
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.013
15-deoxy-DELTA12,14-prostaglandin
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.25
2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide
Homo sapiens
above, pH 7.0, 22°C, IDO1
0.25
2-([5-(3-methoxyphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)-N-(5-methyl-1,3-thiazol-2-yl)acetamide
Homo sapiens
above, pH 7.0, 22°C, IDO2
0.68
3-(1H-1,2,3-triazol-5-yl)pyridine
Homo sapiens
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
0.708
3-(1H-1,2,3-triazol-5-yl)pyridine
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.825
3-(1H-imidazol-4-yl)benzaldehyde
Homo sapiens
-
0.825
3-(1H-imidazol-4-yl)benzaldehyde
Homo sapiens
pH and temperature not specified in the publication
0.179
4-(2-fluorophenyl)-1H-imidazole
Homo sapiens
-
0.179
4-(2-fluorophenyl)-1H-imidazole
Homo sapiens
pH and temperature not specified in the publication
0.000055
4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.00025
4-(benzylamino)-3-hydroxy-2,2-dimethyl-3,4-dihydro-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.422
4-(thiophen-2-yl)-1H-imidazole
Homo sapiens
-
0.422
4-(thiophen-2-yl)-1H-imidazole
Homo sapiens
pH and temperature not specified in the publication
0.026
4-fluoro-2-(1H-pyrazol-3-yl)phenol
Homo sapiens
-
0.026
4-fluoro-2-(1H-pyrazol-3-yl)phenol
Homo sapiens
pH and temperature not specified in the publication
0.00048
4-phenylimidazole
Homo sapiens
pH and temperature not specified in the publication
0.048
4-phenylimidazole
Homo sapiens
-
0.000199
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
-
0.000203
4-[([4-[2-(4-bromophenyl)hydrazinesulfonyl]phenyl]carbamoyl)amino]benzene-1-sulfonamide
Homo sapiens
pH and temperature not specified in the publication
-
0.06
5-phenyl-1H-1,2,3-triazole
Homo sapiens
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
0.143
5-phenyl-1H-1,2,3-triazole
Homo sapiens
-
pH 6.5, 37°C, recombinant enzyme
0.002
8-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.00205
8-hydroxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00292
9-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
-
0.00292
9-methoxy-2,2-dimethyl-2H-benzo[g]chromene-5,10-dione
Homo sapiens
pH and temperature not specified in the publication
0.00001
epacadostat
Homo sapiens
pH and temperature not specified in the publication
-
0.000086
epacadostat
Homo sapiens
pH 6.5, 37°C
-
0.00009
epacadostat
Homo sapiens
pH and temperature not specified in the publication
-
0.0216
methyl thiohydantoin-Trp
Homo sapiens
pH 7.0, 22°C, IDO1
0.0826
methyl thiohydantoin-Trp
Homo sapiens
pH 7.0, 22°C, IDO2
0.003
N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
Homo sapiens
pH 7.0, 22°C, IDO1
0.25
N-(1,3-benzodioxol-5-yl)-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
Homo sapiens
above, pH 7.0, 22°C, IDO2
0.0000093
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.IDO1
-
0.0000132
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.TDO
-
0.00000546
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.TDO
-
0.0000127
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.IDO1
-
0.0000323
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.TDO
-
0.000112
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
Mus musculus
pH and temperature not specified in the publication, in cell line P1.IDO1
-
0.25
N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
Homo sapiens
above, pH 7.0, 22°C, IDO1
0.25
N-carbamoyl-2-([5-(4-methylphenyl)[1,3]thiazolo[2,3-c][1,2,4]triazol-3-yl]sulfanyl)acetamide
Homo sapiens
above, pH 7.0, 22°C, IDO2
0.000005
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-2-(4-methylphenyl)acetamide
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.000097
N-[4-[bis(2-methylpropyl)amino]-2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]-2-(4-methylphenyl)acetamide
Homo sapiens
pH and temperature not specified in the publication, cellular assay of kynurenine production
-
0.006
prostaglandin (19R)-hydroxy-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0095
prostaglandin (19R)-hydroxy-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0067
prostaglandin 13,14-dihydro-15-oxo-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.03
prostaglandin 13,14-dihydro-15-oxo-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0068
prostaglandin 15-oxo-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.009
prostaglandin 15-oxo-PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0076
prostaglandin 15-oxo-PGF2alpha
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0231
prostaglandin 15-oxo-PGF2alpha
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0074
prostaglandin 20-hydroxy PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0112
prostaglandin 20-hydroxy PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0046
prostaglandin DELTA12-PGJ2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0071
prostaglandin DELTA12-PGJ2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0049
prostaglandin PGA2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0078
prostaglandin PGA2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0041
prostaglandin PGD2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0074
prostaglandin PGD2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0047
prostaglandin PGD2 ethanolamide
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0057
prostaglandin PGD2 ethanolamide
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.01
prostaglandin PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0221
prostaglandin PGE2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0046
prostaglandin PGE2 ethanolamide
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0063
prostaglandin PGE2 ethanolamide
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0071
prostaglandin PGF2beta
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0074
prostaglandin PGF2beta
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0092
prostaglandin PGG2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0112
prostaglandin PGG2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0072
prostaglandin PGH2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
0.0096
prostaglandin PGH2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0042
prostaglandin PGJ2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human monocytes
0.0067
prostaglandin PGJ2
Homo sapiens
-
pH not specified in the publication, 37°C, inhibition of human THP-1 cells
additional information
additional information
Mus musculus
-
review article sumarizing data of many inhibitors of indoleamine 2,3-dioxygenase
-
additional information
additional information
Homo sapiens
review article sumarizing data of many inhibitors of indoleamine 2,3-dioxygenase
-
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drug target
as an immunosuppressive enzyme, indoleamine 2,3-dioxygenase 1 is considered a promising target for oncology immunotherapy
drug target
combined treatment of cancer cells in vitro with indoleamine 2,3-dioxygenase 1-specific antisense oligonucleotides and small molecule inhibitors can reduce the production of kynurenine by cancer cells in a synergistic manner
drug target
conversion of tryptophan to N-formylkynurenine is the first and rate-limiting step of the tryptophan metabolic pathway (i.e., the kynurenine pathway). This conversion is catalyzed by three enzyme isoforms: indoleamine 2,3-dioxygenase 1 (IDO1), indoleamine 2,3-dioxygenase 2 (IDO2), and tryptophan-2,3-dioxygenase (TDO). As this pathway generates numerous metabolites that are involved in various pathological conditions, IDOs and TDO represent important targets for therapeutic intervention. Despite their poor sequence similarities, their active sites are highly conserved, and therefore allow the design of inhibitors with multiple activities that can target at least two isoforms
drug target
human indoleamine 2,3-dioxygenase 1 (hIDO1) and tryptophan 2,3-dioxygenase (hTDO) are closely linked to the pathogenesis of Parkinson's disease
drug target
Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are promising drug development targets due to their implications in pathologies such as cancer and neurodegenerative diseases. IDO1/TDO dual inhibitors and provides chemical molecules for potential development into drugs
drug target
the enzyme is a promising target for cancer immunotherapy
drug target
the enzyme is a tumour cell survival factor that causes immune escape in several types of cancer
drug target
the enzyme is an anti-cancer drug target
drug target
the enzyme is an attractive target for cancer immunotherapy
evolution
-
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
evolution
indoleamine 2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) enzymes have independently evolved to catalyze the first step in the catabolism of tryptophan (L-Trp) through the kynurenine pathway. Enzyme TDO is found in almost all metazoan and many bacterial species, but not in fungi, distribution of IDO/TDO genes among invertebrates, overview. Some lineages have independently generated multiple IDO paralogues through gene duplications. Only mammalian IDO1s and fungal typical IDOs have high affinity and catalytic efficiency for L-Trp catabolism, comparable to TDOs. Invertebrate IDO enzymes have low affinity and catalytic efficiency for L-Trp catabolism. Phylogenetic analysis. the phylogenetic distribution of low catalytic-efficiency IDOs indicates the ancestral IDO also had low affinity and catalytic efficiency for L-Trp catabolism. IDOs with high catalytic-efficiency for L-Trp catabolism may have evolved in certain lineages to fulfill particular biological roles. The low catalytic efficiency IDOs have been well conserved in a number of lineages throughout their evolution, although it is not clear that the enzymes contribute significantly to L-Trp catabolism in these species
malfunction
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IDO deficiency leads to diminished phenotypic and functional maturation of dendritic cells in vitro and in vivo
malfunction
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IDO inhibition significantly affects the ability of CD103+ dendritic cells to promote conversion of naive T cells into Foxp3+Tregs while the ability of CD103- cells is unaffected. IDO inhibition impinges on the development of oral tolerance
malfunction
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IDO inhibition significantly affects the ability of CD103+ denxritic cells to promote conversion of naive T cells into Foxp3+Tregs while the ability of CD103- cells is unaffected. IDO inhibition impinges on the development of oral tolerance
malfunction
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the attenuation of Francisella novicida tryptophan mutant bacteria is rescued in the lungs of IDO1-deficient mice
malfunction
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hemodialysis patients characterized by impaired adaptive immunity, exhibit increased IDO expression, further enhanced in the non-responders to hepatitis B virus vaccination
malfunction
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IDO1 pharmacological inhibition causes the rejection of mouse allogeneic concepti, mediated by T cells, and its expression in tumors is associated with their immune evasion. Deletion of IDO1 genomic sequences has the potential to also impact on IDO2 expression due to the chromosomal proximity of the genes, transcription of the IDO2 gene is reduced in the liver of IDO1-/- mice, although protein levels appear to be maintained
malfunction
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the kynurenine pathway is over-activated in Alzheimer's disease mice
metabolism
IDO catalyzes the initial and rate-limiting step in the catabolism of tryptophan along the kynurenine pathway
metabolism
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IDO is a key enzyme that catalyzes the initial, rate-limiting step in tryptophan degradation
metabolism
-
IDO is the first and rate-limiting enzyme in the kynurenine pathway
metabolism
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tryptophan 2,3-dioxygenase is an essential enzyme in the pathway of NAD biosynthesis
metabolism
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indoleamine 2,3-dioxygenase catalyses the initial rate-limiting step of tryptophan degradation along the kynurenine pathway
metabolism
indoleamine 2,3-dioxygenase catalyzes the first step in tryptophan breakdown along the kynurenine pathway
metabolism
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three enzymes are now known to catalyze the first and rate-limiting step in the catabolism of tryptophan along the kynurenine pathway: tryptophan 2,3-dioxygenase, indoleamine 2,3-dioxygenase subsequently and a third enzyme, indoleamine 2,3-dioxygenase 2. The kynurenine pathway is a major route for NAD+ synthesis. The pathway is implicated in many disorders and/or their complications, including cerebral malaria, neurological and neurodegenerative diseases
metabolism
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three enzymes are now known to catalyze the first and rate-limiting step in the catabolism of tryptophan along the kynurenine pathway: tryptophan 2,3-dioxygenase, indoleamine 2,3-dioxygenase subsequently and a third enzyme, indoleamine 2,3-dioxygenase 2. The kynurenine pathway is a major route for NAD+ synthesis. The pathway is implicated in many disorders and/or their complications, including cerebral malaria, neurological and neurodegenerative diseases
metabolism
-
tryptophan 2,3 dioxygenase is the key regulatory enzyme of the kynurenine pathway
metabolism
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tryptophan 2,3 dioxygenase is the key regulatory enzyme of the kynurenine pathway
metabolism
tryptophan 2,3-dioxygenase catalyzes the oxidative cleavage of the indole ring of L-tryptophan to N-formylkynurenine in the kynurenine pathway
metabolism
comparison of contribution percentage of tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO) to the conversion of L-tryptophan, the calculated percentage conversions indicats that TDO and IDO oxidize 70% and 30%, respectively, of the dietary L-tryptophan. The amount of D-Trp converted to nicotinamide via indole-3-pyruvic acid (IPA) is very low, this amount of D-Trp is converted to L-Trp, which is primarily used for protein synthesis rather than catabolism via the Kyn biosynthesis pathway in mice
metabolism
indoleamine 2,3-dioxygenase-2 (IDO2) is one of three enzymes, alongside tryptophan 2,3-dioxygenase (EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO1), that catalyse dioxygenation of L-tryptophan as the first step in the kynurenine pathway
metabolism
the first and rate limiting step of the kynurenine pathway is carried out by two heme-containing enzymes, tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO), which differ in their tissue distribution and regulation
metabolism
the initial and rate-limiting step of the kynurenine pathway involves oxidation of L-Trp toN-formylkynurenine. This is an O2-dependent process and catalyzed by indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase, EC 1.13.11.11
metabolism
infection of THP-1 cells with GRA15-intact Toxoplasma gondii produces IL-1beta in a manner dependent on NLRP3 and caspase-1. This leads to an indirect reduction in IDO1 proteins, thereby supporting parasite growth in human cells
metabolism
overexpression of indoleamine 2,3-dioxygenase in tumor microenvironment results in tumor immune escape
metabolism
the enzyme catalyzes the rate limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging
metabolism
the enzyme is a tumour cell survival factor that causes immune escape in several types of cancer
metabolism
-
comparison of contribution percentage of tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO) to the conversion of L-tryptophan, the calculated percentage conversions indicats that TDO and IDO oxidize 70% and 30%, respectively, of the dietary L-tryptophan. The amount of D-Trp converted to nicotinamide via indole-3-pyruvic acid (IPA) is very low, this amount of D-Trp is converted to L-Trp, which is primarily used for protein synthesis rather than catabolism via the Kyn biosynthesis pathway in mice
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physiological function
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activation of IDO is a key event in the switch from sickness to depression, activation of the innate immune system in the brain is sufficient to activate IDO and to induce depressive-like behavior in the absence of detectable interferon-gamma
physiological function
-
IDO inhibits lymphocyte proliferation induced by lectins
physiological function
-
IDO is a mechanism for Kupffer cells to induce immune tolerance
physiological function
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IDO is an immunoregulatory enzyme that is implicated in suppressing T-cell immunity in normal and pathological settings. IDO5-specific T cells are specifically able to kill IDO-expressing cells. IDO-specific T cells boost viral immunity
physiological function
-
IDO is central in the regulation of immune responses
physiological function
-
IDO is involved in the maintenance of immune tolerance at the maternal-fetal interface
physiological function
-
IDO-1 is one of the key players involved in the pathogenesis of Alzheimer's disease
physiological function
-
IDO-expressing skin substitutes significantly suppress T cell infiltration and improve neovascularization by 4fold
physiological function
-
indoleamine 2,3-dioxygenase 1 is a lung-specific innate immune defense mechanism that inhibits growth of Francisella tularensis tryptophan auxotrophs
physiological function
-
indoleamine 2,3-dioxygenase activity is implicated in the promotion of tolerance to tumors and in autoimmune and inflammatory conditions, itplays a role in arthritis, ischemia-reperfusion injury, haemostatic system, sepsis, atherosclerosis, diabetes, and gut, allergy, and airway inflammation
physiological function
-
indoleamine 2,3-dioxygenase is an enzyme involved in tryptophan catabolism with immunosuppressive effects influencing T regulatory/T effector cell balance and oral tolerance induction
physiological function
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indoleamine 2,3-dioxygenase is an enzyme involved in tryptophan catabolism with immunosuppressive effects influencing T regulatory/T effector cell balance and oral tolerance induction
physiological function
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indoleamine 2,3-dioxygenase is critical for regulating immune responses and suppression of inflammation. In human chronic granulomatous disease, IDO metabolic activity is intact
physiological function
indoleamine 2,3-dioxygenase mediates the antiviral effect of interferon-gamma against hepatitis B virus in human hepatocyte-derived cells, indoleamine 2,3-dioxygenase efficiently reduces the level of intracellular hepatitis B virus DNA without altering the steady-state level of viral RNA
physiological function
-
TDO expression distinguishes stem cells from more differentiated cells among the granule cells of the adult mouse dentate gyrus. TDO is required at a late-stage of granule cell development, such as during axonal and dendritic growth, synaptogenesis and its maturation
physiological function
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the induction of IDO by interferon-gamma in HLE-B3 cells causes increases in intracellular reactive oxygen species, cytosolic cytochrome c and caspase-3 activity, along with a decrease in protein-free thiol content, are accompanied by apoptosis. IDO-mediated kynurenine formation plays a role in cataract formation related to chronic inflammation
physiological function
-
heme enzyme indoleamine 2,3-dioxygenase is a key regulator of immune responses through catalyzing L-tryptophan oxidation. Peroxidase-mediated dioxygenase inactivation, NO consumption, or protein nitration may modulate the biological actions of IDO expressed in inflammatory tissues where the levels of H2O2 and NO are elevated and L-Trp is low
physiological function
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immune regulatory effects of Ido1 and ability of nitric oxide to regulate Ido1 activity, Ido1-mediated metabolism of tryptophan to kynurenine can modulate vascular tone After transient cerebral ischaemia induction in wild-type and Ido1 gene-deficient (Ido1-/-) mice, cerebral ischaemia-reperfusion in wild-type mice increases Ido activity and its expression in cerebral arterioles, while Ido1-/- and 1-methyl-D-tryptophan-treated wild-type mice have lower Ido activity but similar post-stroke neurological function and similar total brain infarct volume and swelling, relative to control mice. Ido1 expression does not appear to affect overall outcome following acute ischaemic stroke
physiological function
-
in mammals, IDO1 acts as a defence molecule in combating bacterial and viral infections, as its expression is up-regulated by cytokines such as IFN-gamma, leading to local depletion of L-Trp and causing inhibition of pathogen growth
physiological function
-
in mammals, IDO1 acts as a defence molecule in combating bacterial and viral infections, as its expression is up-regulated by cytokines such as IFN-gamma, leading to local depletion of L-Trp and causing inhibition of pathogen growth. IDO2 mRNA is also upregulated in the brain of mice infected with Toxoplasma gondii, an infection in which IFN-gamma driven responses play an important role in controlling parasite growth
physiological function
-
indoleamine 2,3-dioxygenase suppresses adaptive immunity. It induces T-cell differentiation to regulatory T-cells through tryptophan depletion and/or kynurenine pathway products. The enzyme decreases glucose uptake by stimulated lymphocytes, increases mitochondrial function in stimulated lymphocytes, decreases aerobic glycolysis in stimulated lymphocytes, and induces the production of the immunosuppressive cytokine IL-10 by stimulated lymphocytes. Effect of IDO on glucose metabolism of lymphocytes, overview
physiological function
-
the enzyme is responsible for L-Trp processing that ultimately leads to the biosynthesis of NAD+ and NADP+
physiological function
indoleamine 2,3-dioxygenase depletes tryptophan, activates general control non-derepressible 2 kinase and down-regulates key enzymes involved in fatty acid synthesis in primary human CD4+ T cells. Indoleamine 2,3-dioxygenase is expressed in antigen-presenting cells and exerts immunosuppressive effects on CD4+ T cells through the inhibition of aerobic glycolysis or through downregulation of key enzymes that directly or indirectly promote fatty acid synthesis, a prerequisite for CD4+ T-cell proliferation and differentiation into effector cell lineages. IDO activates GCN2 kinase which inhibits CD4+ T-cell proliferation
physiological function
indoleamine 2,3-dioxygenase, by degrading L-tryptophan, enhances carnitine palmitoyltransferase I activity and fatty acid oxidation, and exerts fatty acid-dependent effects in human alloreactive CD4+ T-cells. The enzyme has an immunoregulatory role in various models of autoimmunity and allotransplantation. IDO increases fatty acid oxidation in mixed lymphocyte reactions and CPT1 enzymatic activity in mixed lymphocyte reaction-derived CD4+ T-cells. IDO decreases ACC2 expression, whereas it increases the level of phosphorylated ACC2 in mixed lymphocyte reaction-derived CD4+ T-cells. IDO increases L-tryptophan degradation in mixed lymphocyte reactions enhances eIF2alpha phosphorylation and CYP1A1 expression in mixed lymphocyte reaction-derived CD4+ T-cells, but does not affect p70S6K phosphorylation in mixed lymphocyte reaction-derived CD4+ T-cells
physiological function
the cytokine-inducible extrahepatic human indoleamine 2,3-dioxygenase (hIDO1) catalyzes the first step of the kynurenine pathway. Immunosuppressive activity of hIDO1 in tumor cells weakens host T-cell immunity, contributing to the progression of cancer
physiological function
-
the enzyme catalyses the first and rate-limiting step in the metabolism of L-tryptophan. Degradation of L-Trp leads to the production of several immunosuppressive metabolites, including N-formyl kynurenine and kynurenine. Enzyme IDO-1 also plays a crucial role in immune suppression and tumour induced tolerance. IDO-1 acts as an inducible negative regulator of T cell viability, proliferation and activation
physiological function
the enzyme catalyzes the first and rate-limiting step in the degradation of L-tryptophan, has an important immunomodulatory function. The activity of IDO1 increases in various inflammatory diseases, including tumors, autoimmune diseases, and different kinds of inflammation
physiological function
the enzyme IDO2 might have an immunomodulatory role unrelated to that of IDO1
physiological function
the enzyme is involved in L-tryptophan catabolism to produce bioactive metabolites including kynurenine, kynurenic acid, quinolinic acid, and the coenzyme NAD+ via the kynurenine pathway
physiological function
the enzyme is involved in nicotinamide biosynthesis. Comparison of contribution percentage of tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO) to the conversion of L-tryptophan, the calculated percentage conversions indicats that TDO and IDO oxidize 70% and 30%, respectively, of the dietary L-tryptophan. The amount of D-Trp converted to nicotinamide via indole-3-pyruvic acid (IPA) is very low, this amount of D-Trp is converted to L-Trp, which is primarily used for protein synthesis rather than catabolism via the Kyn biosynthesis pathway in mice
physiological function
the immunoregulatory enzyme indoleamine 2,3-dioxygenase (IDO) suppresses T-cell responses and promotes immune tolerance in tumor resistance, indoleamine 2,3-dioxygenase regulates T cell activity through Vav1/Rac pathway, the inhibitory effects of IDO on T cell immune responses may occur through the downregulation of Vav1 protein expression and the suppression of Vav1/Rac cascade . Enzyme IDO cannot downregulate the expression of the two early signal transductions, namely, ZAP-70 and CD3lambda
physiological function
conversion of tryptophan to N-formylkynurenine is the first and rate-limiting step of the tryptophan metabolic pathway (i.e., the kynurenine pathway). This conversion is catalyzed by three enzyme isoforms: indoleamine 2,3-dioxygenase 1 (IDO1), indoleamine 2,3-dioxygenase 2 (IDO2), and tryptophan-2,3-dioxygenase (TDO)
physiological function
IFN-gamma stimulates the expression of indoleamine 2,3-dioxygenase to degrade tryptophan, an essential nutritional amino acid for the intracellular growth of Toxoplasma gondii in human cells
physiological function
in the tryptophan-nicotinamide pathway, indoleamine 2,3-dioxygenase 1 (IDO1) participates in the first step and catalyzes the formation of N-formylkynurnine by promoting the oxidative cleavage of indole 2,3-double bonds
physiological function
key enzyme in degradation of tryptophan into immunosuppressive kynurenine
physiological function
the enzyme catalyses the rate-limiting step in the kynurenine pathway, an important biochemical mechanism for immunological responsecancers express tryptophan catabolising enzymes indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO2) to produce immunosuppressive tryptophan metabolites that undermine thr immune systems of patients, leading to poor disease outcomes
physiological function
the enzyme catalyzes the rate limiting step in the kynurenine pathway of tryptophan metabolism, which is involved in immunity, neuronal function, and aging
physiological function
the enzyme is overactivated or overexpressed in many human cancers, which is associated with poor patient outcomes
physiological function
the enzyme plays a crucial role in immune tolerance
physiological function
the enzyme plays an important role in the immune escape of tumors
physiological function
the enzyme plays multiple roles in the immunity of fish
physiological function
-
the enzyme is involved in nicotinamide biosynthesis. Comparison of contribution percentage of tryptophan 2,3-dioxygenase (TDO, EC 1.13.11.11) and indoleamine 2,3-dioxygenase (IDO) to the conversion of L-tryptophan, the calculated percentage conversions indicats that TDO and IDO oxidize 70% and 30%, respectively, of the dietary L-tryptophan. The amount of D-Trp converted to nicotinamide via indole-3-pyruvic acid (IPA) is very low, this amount of D-Trp is converted to L-Trp, which is primarily used for protein synthesis rather than catabolism via the Kyn biosynthesis pathway in mice
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additional information
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H2O2 activates the peroxidase function to induce protein oxidation and inhibit dioxygenase activity, overview. Dioxygenase inhibition correlated with IDO-catalyzed H2O2 consumption, compound I-mediated formation of protein-centered radicals, altered protein secondary structure, and opening of the distal heme pocket to promote nonproductive substrate binding, inhibited by L-Trp, the heme ligand cyanide, or free radical scavengers
additional information
F5H5G0
IDO1 and IDO2 have different kinetic parameters and different inhibition profiles
additional information
IDO1 and IDO2 have different kinetic parameters and different inhibition profiles
additional information
-
IDO1 and IDO2 have different kinetic parameters and different inhibition profiles
additional information
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molecular dynamics simulation studies, overview. Structural role of T342 in controlling the substrate stereoselectivity of the enzyme
additional information
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transcription of the IDO2 gene is complex. IDO1 expression is found in most tissues and is regulated by immunological signals, including interferon-gamma, lipopolysaccharide and tumor necrosis factor
additional information
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transcription of the IDO2 gene is complex. IDO1 expression is found in most tissues and is regulated by immunological signals, including interferon-gamma, lipopolysaccharide and tumor necrosis factor
additional information
-
Xanthomonas campestris TDO shows an H-bond between T254 and the ammonium group of the substrate is present in the L-Trp-bound enzyme, but not in the D-Trp bound enzyme, molecular dynamics simulation studies. T254 controls the substrate stereoselectivity of the enzyme by modulating the H-bonding interaction between the NH3-group and epoxide oxygen of the ferryl/indole 2,3-epoxide intermediate of the enzyme, and regulating the dynamics of two active site loops, loop250-260 and loop117-130, critical for substrate-binding, O2 and L-trp both are bound in the active site
additional information
active site-inhibitor interactions, overview. Importance of the Ser167 and the Cys129 residues in the IDO1 active site
additional information
conformational dynamics in three-dimensional structure of hIDO, and structure-function analysis, modeling using structures PDB IDs 2D0T, 2NW8, and 2X67, overview. Flexible active site loop in human indoleamine 2,3-dioxygenase
additional information
-
conformational dynamics in three-dimensional structure of hIDO, and structure-function analysis, modeling using structures PDB IDs 2D0T, 2NW8, and 2X67, overview. Flexible active site loop in human indoleamine 2,3-dioxygenase
additional information
human indoleamine 2,3-dioxygenase-2 substrate specificity and inhibition characteristics are distinct from those of indoleamine 2,3-dioxygenase-1
additional information
human indoleamine 2,3-dioxygenase-2 substrate specificity and inhibition characteristics are distinct from those of indoleamine 2,3-dioxygenase-1
additional information
-
human indoleamine 2,3-dioxygenase-2 substrate specificity and inhibition characteristics are distinct from those of indoleamine 2,3-dioxygenase-1
additional information
IDO homology modeling, overview
additional information
important amino acid residues that stabilize the substrate in the active site: a cluster of small side chain residues at positions 260-265 ensures structural flexibility of the binding site. Thr379 and Arg231 are key residues acting in concert to bind the substrate. Thr379 is the final residue of a disordered loop, the neighboring Gly380 is 20 A away from the heme iron. Residues Ser167, Phe226, Phe227, and Arg231 may play critical roles. Stucture-function analysis by spectrocopic methods, overview. The hIDO1 distal heme pocket is in part lined by a sequence of residues with small side chains (residues 260-265: AGGSAG) rendering structural flexibility to the active site, which may be required to accommodate the substrate
additional information
-
important amino acid residues that stabilize the substrate in the active site: a cluster of small side chain residues at positions 260-265 ensures structural flexibility of the binding site. Thr379 and Arg231 are key residues acting in concert to bind the substrate. Thr379 is the final residue of a disordered loop, the neighboring Gly380 is 20 A away from the heme iron. Residues Ser167, Phe226, Phe227, and Arg231 may play critical roles. Stucture-function analysis by spectrocopic methods, overview. The hIDO1 distal heme pocket is in part lined by a sequence of residues with small side chains (residues 260-265: AGGSAG) rendering structural flexibility to the active site, which may be required to accommodate the substrate
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