Literature summary for 2.3.1.87 extracted from

Ferry, G.; Ubeaud, C.; Mozo, J.; Pean, C.; Hennig, P.; Rodriguez, M.; Scoul, C.; Bonnaud, A.; Nosjean, O.; Galizzi, J.P.; Delagrange, P.; Renard, P.; Volland, J.P.; Yous, S.; Lesieur, D.; Boutin, J.A.
New substrate analogues of human serotonin N-acetyltransferase produce in situ specific and potent inhibitors (2004), Eur. J. Biochem., 271, 418-428.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression in Escherichia coli	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
2-bromo-N-[2-(5-fluoro-1-benzothien-3-yl)ethyl]acetamide	IC50: 0.00039 mM	Homo sapiens
bromoacetyltryptamine	IC50: 0.0014 mM	Homo sapiens
methyl 3-[2-[(bromoacetyl)amino]ethyl]-1-benzothiophene-5-carboxylate	IC50: 0.00225 mM	Homo sapiens
N-[2-(2-benzyl-5-methoxy-benzofuran-3-yl)ethyl]iodoacetamide	IC50: 0.0087 mM	Homo sapiens
N-[2-(2-phenyl-benzo [b]thiophen-3-yl)ethyl]bromoacetamide	IC50: 0.001 mM	Homo sapiens
N-[2-(3-ethyl-7-methoxy-napht-1-yl)ethyl]iodoacetamide	IC50: 0.0006 mM	Homo sapiens
N-[2-(5-bromo-benzo[b]thiophen-3-yl)ethyl]bromoacetamide	IC50: 0.00378 mM	Homo sapiens
N-[2-(5-chloro-benzo[b]thiophen-3-yl)ethyl]bromoacetamide	IC50: 0.00018 mM	Homo sapiens
N-[2-(5-ethyl-1-benzothien-3-yl)ethyl]-2-iodoacetamide	IC50: 0.002 mM	Homo sapiens
N-[2-(5-ethyl-benzo[b]thiophen-3-yl)ethyl]bromoacetamide	IC50: 0.00071 mM	Homo sapiens
N-[2-(5-fluoro-1H-indol-3-yl)ethyl]bromoacetamide	IC50: 0.0056 mM	Homo sapiens
N-[2-(5-hydroxy-benzo[b]thiophen-3-yl)ethyl]bromoacetamide	IC50: 0.00018 mM	Homo sapiens
N-[2-(7-ethyl-1,2,3,4-tetrahydronapht-1-yl)ethyl]iodooacetamide	IC50: above 0.1 mM	Homo sapiens
N-[2-(7-ethyl-napht-1-yl)ethyl]-bromoacetamide	IC50: 0.00177 mM	Homo sapiens
N-[2-(7-hydroxy-naphth-1-yl)ethyl]bromoacetamide	IC50: 0.00072 mM	Homo sapiens
N-[2-(7-methoxy-3-(3-trifluoromethylphenyl)-napht-1-yl)ethyl]iodoacetamide	IC50: 0.045 mM	Homo sapiens
N-[2-(7-methoxy-8-propenyl-napht-1-yl)ethyl]-iodoacetamide	IC50: above 0.1 mM	Homo sapiens
N-[2-(7-methoxy-napht-1-yl)ethyl]bromoacetamide	IC50: 0.002 mM	Homo sapiens
N-[2-(7-propoxy-napht-1-yl)ethyl]iodoacetamide	IC50: 0.0042 mM	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	the enzyme catalyzes the rate-limiting step in melatonin synthesis	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
acetyl-CoA + phenylethylamine	-	Homo sapiens	CoA + N-acetyl-phenylethylamine	-	?
additional information	the enzyme catalyzes the rate-limiting step in melatonin synthesis	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
arylalkylamine N-acetyltransferase	-	Homo sapiens
serotonin N-acetyltransferase	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00018	-	IC50: 0.00018 mM	Homo sapiens	N-[2-(5-hydroxy-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
0.00018	-	IC50: 0.00018 mM	Homo sapiens	N-[2-(5-chloro-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
0.00039	-	IC50: 0.00039 mM	Homo sapiens	2-bromo-N-[2-(5-fluoro-1-benzothien-3-yl)ethyl]acetamide
0.0006	-	IC50: 0.0006 mM	Homo sapiens	N-[2-(3-ethyl-7-methoxy-napht-1-yl)ethyl]iodoacetamide
0.00071	-	IC50: 0.00071 mM	Homo sapiens	N-[2-(5-ethyl-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
0.00072	-	IC50: 0.00072 mM	Homo sapiens	N-[2-(7-hydroxy-naphth-1-yl)ethyl]bromoacetamide
0.001	-	IC50: 0.001 mM	Homo sapiens	N-[2-(2-phenyl-benzo [b]thiophen-3-yl)ethyl]bromoacetamide
0.0014	-	IC50: 0.0014 mM	Homo sapiens	bromoacetyltryptamine
0.00177	-	IC50: 0.00177 mM	Homo sapiens	N-[2-(7-ethyl-napht-1-yl)ethyl]-bromoacetamide
0.002	-	IC50: 0.002 mM	Homo sapiens	N-[2-(7-methoxy-napht-1-yl)ethyl]bromoacetamide
0.002	-	IC50: 0.002 mM	Homo sapiens	N-[2-(5-ethyl-1-benzothien-3-yl)ethyl]-2-iodoacetamide
0.00225	-	IC50: 0.00225 mM	Homo sapiens	methyl 3-[2-[(bromoacetyl)amino]ethyl]-1-benzothiophene-5-carboxylate
0.00378	-	IC50: 0.00378 mM	Homo sapiens	N-[2-(5-bromo-benzo[b]thiophen-3-yl)ethyl]bromoacetamide
0.0042	-	IC50: 0.0042 mM	Homo sapiens	N-[2-(7-propoxy-napht-1-yl)ethyl]iodoacetamide
0.0056	-	IC50: 0.0056 mM	Homo sapiens	N-[2-(5-fluoro-1H-indol-3-yl)ethyl]bromoacetamide
0.0087	-	IC50: 0.0087 mM	Homo sapiens	N-[2-(2-benzyl-5-methoxy-benzofuran-3-yl)ethyl]iodoacetamide
0.045	-	IC50: 0.045 mM	Homo sapiens	N-[2-(7-methoxy-3-(3-trifluoromethylphenyl)-napht-1-yl)ethyl]iodoacetamide
0.1	-	IC50: above 0.1 mM	Homo sapiens	N-[2-(7-ethyl-1,2,3,4-tetrahydronapht-1-yl)ethyl]iodooacetamide
0.1	-	IC50: above 0.1 mM	Homo sapiens	N-[2-(7-methoxy-8-propenyl-napht-1-yl)ethyl]-iodoacetamide

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Release 2023.1 (January 2023)