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Literature summary extracted from

  • Higaki, Y.; Usami, N.; Shintani, S.; Ishikura, S.; El-Kabbani, O.; Hara, A.
    Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone (2003), Chem. Biol. Interact., 143-144, 503-513.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.149 1,10-phenanthroline 50% inhibition at 0.065 mM Homo sapiens
1.1.1.149 2-acetylbenzofuran 50% inhibition at 0.033 mM Homo sapiens
1.1.1.149 3',3'',5',5''-tetrabromophenolphthalein 50% inhibition at 33 nM Homo sapiens
1.1.1.149 3',3'',5',5''-tetrabromophenolphthalein diacetate 50% inhibition at 350 nM Homo sapiens
1.1.1.149 3',3'',5',5''-tetraiodophenolphthalein 50% inhibition at 120 nM Homo sapiens
1.1.1.149 3,5-dibromo-4-hydroxybenzoic acid methyl ester 50% inhibition at 0.099 mM Homo sapiens
1.1.1.149 benzbromarone 50% inhibition at 48 nM Homo sapiens
1.1.1.149 benzbromarone acetate 50% inhibition at 430 nM Homo sapiens
1.1.1.149 benzofuran 50% inhibition at 1.45 mM Homo sapiens
1.1.1.149 benzofuran-2-carboxylic acid 50% inhibition at 0.16 mM Homo sapiens
1.1.1.149 Bethamethasone 0.1 mM, 10% inhibition Homo sapiens
1.1.1.149 Bromophenol blue 50% inhibition at 0.011 mM Homo sapiens
1.1.1.149 cloxazolam 0.01 mM, 38% inhibition Homo sapiens
1.1.1.149 diazepam 50% inhibition at 0.0056 mM Homo sapiens
1.1.1.149 dibenzofuran 50% inhibition at 0.895 mM Homo sapiens
1.1.1.149 Flufenamic acid 50% inhibition at 0.0053 mM Homo sapiens
1.1.1.149 glycyrrhetinic acid 50% inhibition at 0.0022 mM Homo sapiens
1.1.1.149 Hexestrol 50% inhibition at 0.0083 mM Homo sapiens
1.1.1.149 indomethacin 50% inhibition at 0.13 mM Homo sapiens
1.1.1.149 lithocholic acid 50% inhibition at 0.022 mM Homo sapiens
1.1.1.149 medazepam 50% inhibition at 0.0047 mM Homo sapiens
1.1.1.149 Medroxyprogesterone acetate 50% inhibition at 700 nM Homo sapiens
1.1.1.149 o-cresolphthalein 50% inhibition at 140 nM Homo sapiens
1.1.1.149 Phenolphthalein 50% inhibition at 340 nM Homo sapiens
1.1.1.149 Ursodeoxycholic acid 50% inhibition at 0.34 mM Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.149 0.0007
-
 5alpha-pregnan-20alpha-ol-3-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0009
-
 5alpha-pregnane-3alpha,20alpha-diol pH 7.0, 25°C Homo sapiens
1.1.1.149 0.001
-
 5beta-pregnan-20alpha-ol-3-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0011
-
 5alpha-pregnane-3,20-dione pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0012
-
 5beta-pregnane-3,20-dione pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0012
-
 5alpha-pregnane-21-ol-3,20-dione pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0013
-
 progesterone pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0013
-
 5beta-pregnan-20alpha-ol-3-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0015
-
 5beta-pregnane-3alpha,20alpha-diol pH 7.0, 25°C Homo sapiens
1.1.1.149 0.002
-
 5alpha-pregnan-3alpha-ol-20-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0026
-
 2-amino-8-((2-fluoro-4-methoxybenzyl)thio)-1,9-dihydro-6H-purin-6-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0027
-
 5alpha-pregnan-20alpha-ol-3-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0033
-
 5beta-Pregnan-3alpha-ol-20-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0033
-
 5alpha-pregnan-3alpha-ol-20-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.0045
-
 5beta-Pregnan-3alpha-ol-20-one pH 7.0, 25°C Homo sapiens
1.1.1.149 0.016
-
 4-pregnen-20alpha-ol-3-one pH 7.0, 25°C Homo sapiens

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.149 2-amino-8-((2-fluoro-4-methoxybenzyl)thio)-1,9-dihydro-6H-purin-6-one + NADP+
-
 Homo sapiens ?
-
 r
1.1.1.149 4-pregnen-20alpha-ol-3-one + NAD(P)+
-
 Homo sapiens 4-pregnen-3,20-dione + NAD(P)H + H+
-
 r
1.1.1.149 5alpha-pregnan-20alpha-ol-3-one + NAD(P)+
-
 Homo sapiens 5alpha-pregnan-3,20-dione + NAD(P)H
-
 r
1.1.1.149 5alpha-pregnan-20alpha-ol-3-one + NAD(P)+
-
 Homo sapiens 5alpha-pregnane-3,20-dione + NAD(P)H
-
 r
1.1.1.149 5alpha-pregnan-3alpha-ol-20-one + NAD(P)H
-
 Homo sapiens 5alpha-pregnan-3alpha,20alpha-diol + NAD(P)+
-
 r
1.1.1.149 5alpha-pregnan-3alpha-ol-20-one + NAD(P)H + H+
-
 Homo sapiens 5alpha-pregnan-3alpha,20alpha-diol + NAD(P)+
-
 r
1.1.1.149 5alpha-pregnane-21-ol-3,20-dione + NAD(P)H
-
 Homo sapiens 5alpha-pregnane-20alpha,21-diol-3-one + NAD(P)+
-
 r
1.1.1.149 5alpha-pregnane-3,20-dione + NAD(P)H
-
 Homo sapiens 5alpha-pregnan-20alpha-ol-3-one + NAD(P)+
-
 r
1.1.1.149 5alpha-pregnane-3alpha,20alpha-diol + NAD(P)+
-
 Homo sapiens 3alpha-hydroxy-5alpha-pregnan-20-one + NAD(P)H + H+
-
 r
1.1.1.149 5alpha-pregnane-3alpha,21-diol-20-one + NAD(P)H + H+
-
 Homo sapiens 5alpha-pregnane-3alpha,20alpha,21-triol + NAD(P)+
-
 r
1.1.1.149 5beta-pregnan-20alpha-ol-3-one + NAD(P)+
-
 Homo sapiens 5beta-pregnan-3,20-dione + NAD(P)H
-
 r
1.1.1.149 5beta-pregnan-3alpha-ol-20-one + NAD(P)H
-
 Homo sapiens 5beta-pregnan-3alpha,20alpha-diol + NAD(P)+
-
 r
1.1.1.149 5beta-pregnan-3alpha-ol-20-one + NAD(P)H
-
 Homo sapiens 5beta-pregnane-3alpha,20alpha-diol + NAD(P)+
-
 r
1.1.1.149 5beta-pregnane-3,20-dione + NAD(P)H + H+
-
 Homo sapiens 5alpha-pregnan-20alpha-ol-3-one + NAD(P)+
-
 r
1.1.1.149 5beta-pregnane-3alpha,20alpha-diol + NAD(P)+
-
 Homo sapiens 5beta-pregnan-20alpha-ol-3-one + NAD(P)H + H+
-
 r
1.1.1.149 progesterone + NAD(P)H
-
 Homo sapiens 20alpha-hydroxyprogesterone + NAD(P)+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.1.1.149 AKR1C1
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.149 NADP+
-
 Homo sapiens
1.1.1.149 NADPH
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.149 0.0000007
-
 3',3'',5',5''-tetrabromophenolphthalein binding to NADPH-enzyme complex via ordered bi-bi-mechanism Homo sapiens