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Literature summary for 1.1.1.146 extracted from

  • Studzinska, R.; Kolodziejska, R.; Kupczyk, D.; Plazinski, W.; Kosmalski, T.
    A novel derivatives of thiazol-4(5H)-one and their activity in the inhibition of 11beta-hydroxysteroid dehydrogenase type 1 (2018), Bioorg. Chem., 79, 115-121 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one 38.03% inhibition of isoform 11beta-HSD1 at 0.01 mM, 22.6% inhibition of isoform 11beta-HSD2 at 0.01 mM Homo sapiens
2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one 71.27% inhibition of isoform 11beta-HSD1 at 0.01 mM, 23.97% inhibition of isoform 11beta-HSD2 at 0.01 mM Homo sapiens
2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one 13.46% inhibition of isoform 11beta-HSD1 at 0.01 mM, 1.34% inhibition of isoform 11beta-HSD2 at 0.01 mM Homo sapiens
additional information not inhibited by 2-(allylamino)thiazol-4(5H)-one, 2-(allylamino)-5-methylthiazol-4(5H)-one, 2-(allylamino)-5-ethylthiazol-4(5H)-one, 2-(allylamino)-5-propylthiazol-4(5H)-one, 2-(allylamino)-5-isopropylthiazol-4(5H)-one, 2-(allylamino)-5,5-dimethylthiazol-4(5H)-one, and 2-(allylamino)-5-phenylthiazol-4(5H)-one Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens
-
cortisol + NADP+
-
ir

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adipose tissue
-
Homo sapiens
-
brain
-
Homo sapiens
-
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
ir

Synonyms

Synonyms Comment Organism
11beta-HSD1 isoform Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0025
-
isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one
0.036
-
isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one
0.05
-
IC50 above 0.05 mM, isoform 11beta-HSD1, at pH 7.4 and 37°C Homo sapiens 2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one