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Literature summary extracted from

  • Egleton, J.E.; Thinnes, C.C.; Seden, P.T.; Laurieri, N.; Lee, S.P.; Hadavizadeh, K.S.; Measures, A.R.; Jones, A.M.; Thompson, S.; Varney, A.; Wynne, G.M.; Ryan, A.; Sim, E.; Russell, A.J.
    Structure-activity relationships and colorimetric properties of specific probes for the putative cancer biomarker human arylamine N-acetyltransferase 1 (2014), Bioorg. Med. Chem., 22, 3030-3054.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.5 expressed in Escherichia coli Rosetta(DE3)pLysS cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.5 N-(3-((2''-methoxyethyl)amino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(2''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenoxy)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenylamino)-5-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenylamino)-6-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenylamino)-7-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3'',5''-dimethylphenylamino)-8-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzamide
-
Homo sapiens
2.3.1.5 N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)phenylacetamide
-
Homo sapiens
2.3.1.5 N-(3-(4''-bromophenoxy)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(4''-bromophenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(4''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(4''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(benzylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(cyclopentylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(furan-2''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(furan-3''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-(furan-3''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)phenylacetamide
-
Homo sapiens
2.3.1.5 N-(3-phenoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(3-phenylamino-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(5-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(6-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(7-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(8-amino-1,4-dioxo-3-(phenylamino)-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(8-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-(8-nitro-1,4-dioxo-3-(phenylamino)-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
-
Homo sapiens
2.3.1.5 N-[3-(3,5-dimethylanilino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]-N-methylbenzenesulfonamide
-
Homo sapiens
2.3.1.5 rhodanine
-
Homo sapiens
2.3.1.5 tamoxifen
-
Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.3.1.5 34000
-
x * 34000, SDS-PAGE Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.5 acetyl-CoA + an arylamine Homo sapiens
-
CoA + an N-acetylarylamine
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.5 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.5 Ni-NTA affinity column chromatography, and gel filtration Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.5 breast cancer cell
-
Homo sapiens
-
2.3.1.5 ZR-75-1 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.5 acetyl-CoA + an arylamine
-
Homo sapiens CoA + an N-acetylarylamine
-
?

Subunits

EC Number Subunits Comment Organism
2.3.1.5 ? x * 34000, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
2.3.1.5 arylamine N-acetyltransferase 1
-
Homo sapiens
2.3.1.5 NAT1
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.5 0.00012
-
pH and temperature not specified in the publication Homo sapiens N-(8-amino-1,4-dioxo-3-(phenylamino)-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.00054
-
pH and temperature not specified in the publication Homo sapiens N-(8-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0009
-
pH and temperature not specified in the publication Homo sapiens N-(3-(4''-bromophenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0017
-
pH and temperature not specified in the publication Homo sapiens N-(3-phenylamino-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
2.3.1.5 0.0019
-
pH and temperature not specified in the publication Homo sapiens N-(3-(4''-bromophenoxy)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0026
-
pH and temperature not specified in the publication Homo sapiens N-(7-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0028
-
pH and temperature not specified in the publication Homo sapiens N-(3-phenoxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
2.3.1.5 0.0041
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0042
-
pH and temperature not specified in the publication Homo sapiens N-(5-amino-3-(3'',5''-dimethylphenylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0058
-
pH and temperature not specified in the publication Homo sapiens N-[3-(3,5-dimethylanilino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl]-N-methylbenzenesulfonamide
2.3.1.5 0.0066
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3'',5''-dimethylphenylamino)-5-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.008
-
pH and temperature not specified in the publication Homo sapiens N-(3-(2''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0084
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0096
-
pH and temperature not specified in the publication Homo sapiens N-(3-(furan-2''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
2.3.1.5 0.01
-
pH and temperature not specified in the publication Homo sapiens N-(3-(furan-3''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-benzenesulfonamide
2.3.1.5 0.01
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzamide
2.3.1.5 0.0103
-
pH and temperature not specified in the publication Homo sapiens N-(3-(4''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0121
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3'',5''-dimethylphenoxy)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0121
-
pH and temperature not specified in the publication Homo sapiens N-(3-(4''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.0145
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3''-chlorophenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.019
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzamide
2.3.1.5 0.0193
-
pH and temperature not specified in the publication Homo sapiens N-(3-(furan-3''-yl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)phenylacetamide
2.3.1.5 0.0221
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3''-formylphenyl)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)phenylacetamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(3-((2''-methoxyethyl)amino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(3-(cyclopentylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(3-(benzylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3'',5''-dimethylphenylamino)-6-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(3-(3'',5''-dimethylphenylamino)-8-nitro-1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzenesulfonamide
2.3.1.5 0.03
-
pH and temperature not specified in the publication Homo sapiens N-(8-nitro-1,4-dioxo-3-(phenylamino)-1,4-dihydronaphthalen-2-yl)benzenesulfonamide