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Literature summary for 2.3.1.5 extracted from

  • Russell, A.J.; Westwood, I.M.; Crawford, M.H.; Robinson, J.; Kawamura, A.; Redfield, C.; Laurieri, N.; Lowe, E.D.; Davies, S.G.; Sim, E.
    Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2 (2009), Bioorg. Med. Chem., 17, 905-918.
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(5Z)-3-amino-5-(3-hydroxy-2,4-diiodobenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(2-methylbenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(3,4-dichlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(3-hydroxy-2,4-diiodobenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(3-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens
(5Z)-5-(4-chlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one inhibition of both recombinant enzyme and native enzyme in ZR-75 cell lysate, competitive Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozyme NAT1
-

Source Tissue

Source Tissue Comment Organism Textmining
ZR-75 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + 4-aminobenzoic acid
-
 Homo sapiens CoA + 4-(acetylamino)benzoic acid
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0006
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(3-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0011
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(2-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0011
-
 pH 8.0, 25°C Homo sapiens (5Z)-3-amino-5-(3-hydroxy-2,4-diiodobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0018
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(3-hydroxy-2,4-diiodobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0034
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(3,4-dichlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0039
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(2-methylbenzylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0047
-
 pH 8.0, 25°C Homo sapiens (5Z)-5-(4-chlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one