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2-bromo-N-[2-(5-fluoro-1-benzothien-3-yl)ethyl]acetamide
-
IC50: 0.00039 mM
9-carboxy-11-nor-delta-9-tetrahydrocannabinol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
alpha-trifluoromethyltryptamine
-
modest, competitive
cannabidiol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
cannabinoid
cannabinoids inhibit AANAT activity and attenuate melatonin biosynthesis through intracellular actions without involvement of classical cannabinoid receptor-dependent signaling cascades
cannabinol
significantly reduces norepinephrine-induced arylalkylamine N-acetyltransferase activity
catechin
-
poorest inhibitor tested, 0.1 mM, 1.6fold inhibition of isoform SNAT1 at 0.1 mM
CoA-S-N-acetyl-7-hydroxynaphthylethylamine
fluorescent variant of CoA-T, a bisubstrate inhibitor, synthesis and enzyme binding structure, molecular modelling, overview
CoA-S-N-acetyltryptamine
total inhibition of N-acetyldopamine synthesis in presence of acetyl coenzyme-A and dopamine occurs in the presence of CoA-S-N-acetyltryptamine in liver
desulfo-CoA
-
dead end inhibitor analog, competitive versus CoA
glutathione
reversible, acetyl-CoA protects
methyl 3-[2-[(bromoacetyl)amino]ethyl]-1-benzothiophene-5-carboxylate
-
IC50: 0.00225 mM
N-acetylserotonin
IC50: 0.68 mM; very slightly
N-ethylmaleimide
irreversible, acetyl-CoA protects
N-[2-(2-benzyl-5-methoxy-benzofuran-3-yl)ethyl]iodoacetamide
-
IC50: 0.0087 mM
N-[2-(2-phenyl-benzo [b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.001 mM
N-[2-(3-ethyl-7-methoxy-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.0006 mM
N-[2-(5-bromo-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00378 mM
N-[2-(5-chloro-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00018 mM
N-[2-(5-ethyl-1-benzothien-3-yl)ethyl]-2-iodoacetamide
-
IC50: 0.002 mM
N-[2-(5-ethyl-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00071 mM
N-[2-(5-fluoro-1H-indol-3-yl)ethyl]bromoacetamide
-
IC50: 0.0056 mM
N-[2-(5-hydroxy-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
-
IC50: 0.00018 mM
N-[2-(7-ethyl-1,2,3,4-tetrahydronapht-1-yl)ethyl]iodooacetamide
-
IC50: above 0.1 mM
N-[2-(7-ethyl-napht-1-yl)ethyl]-bromoacetamide
-
IC50: 0.00177 mM
N-[2-(7-hydroxy-naphth-1-yl)ethyl]bromoacetamide
-
IC50: 0.00072 mM
N-[2-(7-methoxy-3-(3-trifluoromethylphenyl)-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.045 mM
N-[2-(7-methoxy-8-propenyl-napht-1-yl)ethyl]-iodoacetamide
-
IC50: above 0.1 mM
N-[2-(7-methoxy-napht-1-yl)ethyl]bromoacetamide
-
IC50: 0.002 mM
N-[2-(7-propoxy-napht-1-yl)ethyl]iodoacetamide
-
IC50: 0.0042 mM
oxygen
reversible, acetyl-CoA protects
p-chloro-mercuribenzoate
-
-
Peptides containing a disulfide bond
-
tryptamine-coenzyme A
a bisubstrate inhibitor, enzyme binding structure, molecular modelling, overview
tryptophol
-
dead end inhibitor analog, competitive versus tryptamine
UV light
-
NAT activity and melatonin content are suppressed by blue light of 450 nm wavelength, no effects of red light at 650 nm.UV radiation has intensity-dependent dual effects on the NAT activity and melatonin content: it is supressing at low intensity and activating at high intensity irradiation, overview
-
acetyl-CoA-tryptamine
IC50: 0.00041 mM, GST-AANAT fusion protein
acetyl-CoA-tryptamine
-
IC50: 0.00062 mM, GST-AANAT fusion protein
acetyl-CoA-tryptamine
IC50: 0.0008 mM, GST-AANAT fusion protein
bromoacetyltryptamine
-
IC50: 0.0014 mM
bromoacetyltryptamine
IC50: 0.00143 mM, GST-AANAT fusion protein
bromoacetyltryptamine
-
IC50: 0.00128 mM, GST-AANAT fusion protein
bromoacetyltryptamine
IC50: 0.0051 mM, GST-AANAT fusion protein
Disulfides
-
in vivo and in vitro, reversible by dithiothreitol
Disulfides
-
in vivo and in vitro, reversible by dithiothreitol
Melatonin
-
-
morin
-
0.1 mM, 2fold inhibition
morin
0.1 mM, 2fold inhibition
myricetin
-
best inhibitor tested, 8fold inhibition of isoform SNAT1 at 0.1 mM
myricetin
0.1 mM, 1.6fold inhibition
Peptides containing a disulfide bond
-
-
-
Peptides containing a disulfide bond
-
-
-
quercetin
-
-
quercetin
0.1 mM, 1.2fold inhibition
S 20251
IC50: 0.002 mM, GST-AANAT fusion protein
S 20251
-
IC50: 0.0013 mM, GST-AANAT fusion protein
S 20251
IC50: 0.0024 mM, GST-AANAT fusion protein
S 23823
IC50: 0.005 mM, GST-AANAT fusion protein
-
S 23823
IC50: 0.031 mM, GST-AANAT fusion protein
-
S 27244
IC50: 0.00072 mM, GST-AANAT fusion protein
S 27244
-
IC50: 0.00026 mM, GST-AANAT fusion protein
S 27244
IC50: 0.00036 mM, GST-AANAT fusion protein
S 27481
IC50: 0.00018 mM, GST-AANAT fusion protein
S 27481
-
IC50: 0.0004 mM, GST-AANAT fusion protein
S 27481
IC50: 0.0004 mM, GST-AANAT fusion protein
S 28036
IC50: 0.0056 mM,GST-AANAT fusion protein
S 28036
-
IC50: 0.00073 mM, GST-AANAT fusion protein
S 28036
IC50: 0.0017 mM, GST-AANAT fusion protein
serotonin
-
strong, mixed kinetics
tryptamine
inhibitory above 0.03 mM
Zn2+
-
at low concentration
Zn2+
-
at low concentration
additional information
both white and blue light pulses significantly inhibit AA-NAT activity at zeitgeber time ZT18, detailed overview
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additional information
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both white and blue light pulses significantly inhibit AA-NAT activity at zeitgeber time ZT18, detailed overview
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additional information
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strong substrate inhibition at 45°C
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additional information
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strong substrate inhibition at 45°C
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additional information
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inhibition values of peptide inhibitors
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additional information
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strong substrate inhibition at 45°C
-
additional information
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strong substrate inhibition at 45°C
-
additional information
no inhibition by serotonin or tryptamin above 1 mM. No inhibition by melatonin
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additional information
no inhibition by serotonin or tryptamin above 1 mM. No inhibition by melatonin
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additional information
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no inhibition by serotonin or tryptamin above 1 mM. No inhibition by melatonin
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