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Literature summary for 1.1.1.149 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
Search for more literature for 1.1.1.149

Inhibitors

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

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
AKR1C1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
 Homo sapiens
NADPH
-
 Homo sapiens

Ki Value [mM]

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