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(R)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (R)-tetralol
-
-
?
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH
-
i.e. (S)-tetralol
-
-
r
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADH + H+
i.e. (S)-tetralol
-
-
?
(S)-1,2,3,4-tetrahydro-1-naphthol + NAD+
3,4-dihydronaphthalen-1(2H)-one + NADPH + H+
i.e. (S)-tetralol
-
-
?
(S)-1,2,3,4-tetrahydro-1-naphthol + NADP+
3,4-dihydronaphthalen-1(2H)-one + NADPH + H+
i.e. (S)-tetralol
-
-
?
(S)-1-indanol + NAD+
2,3-dihydro-1H-inden-1-one + NADH + H+
(S)-alpha-tetralol + NADP+
alpha-tetralone + NADPH + H+
-
-
-
-
?
(S)-camphorquinone + NADH + H+
? + NAD+
(S)-camphorquinone + NADPH + H+
? + NADP+
-
-
-
?
(S)-tetralol + NADP+
? + NADPH
-
-
-
-
?
1-acenaphthenol + NAD+
acenaphthylen-1(2H)-one + NADH + H+
-
-
-
?
1-phenyl-1,2-propanedione + NADH + H+
? + NAD+
-
-
-
?
11alpha-hydroxytestosterone + NAD+
11alpha-hydroxyandrost-4-ene-3,17-dione + NADH
-
156% velocity compared to testosterone
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
15alpha-hydroxytestosterone + NAD+
15alpha-hydroxyandrost-4-ene-3,17-dione + NADH
-
131% velocity compared to testosterone
-
r
16-oxoestrone + NADH + H+
? + NAD+
-
-
-
?
17beta-estradiol + NAD+
? + NADH + H+
-
-
-
r
17beta-estradiol + NAD+
estrone + NADH + H+
17beta-hydroxy-1alpha-methyl-5alpha-androstan-3-one + NAD+
1alpha-methyl-5alpha-androstane-3,17-dione + NADH
-
192% velocity compared to testosterone
-
r
17beta-hydroxy-5beta-androstan-3-one + NAD+
5beta-androstane-3,17-dione + NADH
-
86% velocity compared to testosterone
-
r
2,3-butanedione + NADH + H+
? + NAD+
-
-
-
?
2-cyclohexen-1-ol + NAD+
2-cyclohexen-1-one + NADH + H+
2-[(2-bromoethyl)(2-[[(2-hydroxyethyl)amino]methyl]-4,6-dinitrophenyl)amino]ethyl methanesulfonate + 2 NADH + 2 H+
2-[(2-bromoethyl)[4-(hydroxyamino)-2-[[(2-hydroxyethyl)amino]methyl]-6-nitrophenyl]amino]ethyl methanesulfonate + 2 NAD+ + H2O
-
i.e. PR-104A, phosphate ester prodrug designed to exploit tumor hypoxia
i.e. PR-104H, enzyme acts as nitroreductase for activation of PR-104A
-
-
20alpha-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
3alpha-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
3beta-hydroxy-5alpha-androstane-17-one + NAD+
5alpha-androstane-3,17-dione + NADH
-
75% velocity compared to testosterone
-
r
3beta-hydroxyprogesterone + NADH + H+
? + NAD+
-
-
-
?
4-androstenedione + NADPH + H+
testosterone + NADP+
-
-
-
-
?
4-oxo-2-nonenal + NADPH + H+
4-hydroxy-2-nonenal + NADP+
-
-
-
-
?
4-pregnen-3alpha-ol-2-one + NAD+
4-pregnen-3,20-dione + NADH + H+
-
-
-
r
4-pregnen-3alpha-ol-20-one + NAD+
4-pregnen-3,20-dione + NADH + H+
-
-
-
?
5alpha-androstan-17beta-ol-3-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstan-3alpha,17beta-diol + NAD+
5alpha-androstan-3alpha-ol-17-one + NADH
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,20-dione + NADH + H+
-
-
-
?
5alpha-androstan-3beta-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstane-17beta-ol-3-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
r
5alpha-androstane-3,17-dione + NADH + H+
? + NAD+
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
5alpha-androstane-3alpha-ol-17-one + NADH
5alpha-androstane-3alpha,17beta-diol + NAD+
?
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NAD+
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
5alpha-androstane-3beta,17beta-diol + NAD+
5alpha-androstane-3beta-ol-17-one + NADH
5alpha-androstane-3beta,17beta-diol + NAD+
? + NAD+
-
-
-
?
5alpha-dihydrotestosterone + NAD+
5alpha-androstane-3,17-dione + NADH
-
133% velocity compared to testosterone
-
r
5alpha-dihydrotestosterone + NAD+
androstandione + NADH
-
-
-
r
5alpha-dihydrotestosterone + NAD+
androstanedione + NADH
5alpha-dihydrotestosterone + NADH + H+
testosterone + NADH + H+
-
-
-
?
5alpha-pregnan-20alpha-ol-3-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3,21alpha-diol-20-one + NAD+
5alpha-pregnan-21-ol-3,20-dione + NADH
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
5alpha-pregnan-3beta-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
5beta-androstan-3alpha,17beta-diol + NAD+
5beta-androstan-3alpha-ol-17-one + NADH
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
r
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
5beta-androstane-17beta-ol-3-one + NAD+
5beta-nbdrostan-3,17-dione + NADH + H+
-
-
-
r
5beta-androstane-3,17-dione + NADH + H+
? + NAD+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
5beta-androstane-3alpha-ol-17-one + NADH
-
57% velocity compared to testosterone
-
r
5beta-androstane-3alpha,17beta-diol + NAD+
?
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
? + NAD+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
5beta-androstane-3beta,17beta-diol + NAD+
? + NAD+
-
-
-
?
5beta-dihydrotestosterone + NAD+
androstanedione + NADH
-
50% initial velocity compared to testosterone
-
r
5beta-dihydrotestosterone + NAD+
testosterone + NADH + H+
-
-
-
?
5beta-pregnan-20alpha-ol-3-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha,21-diol-20-one + NAD+
5beta-pregnan-21-ol-3,20-dione + NADH
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
5beta-pregnan-3beta,21-diol-20-one + NAD+
?
-
-
-
?
5beta-pregnan-3beta-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one + NADH + H+
? + NAD+
-
-
-
?
6beta-hydroxytestosterone + NAD+
6beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
84% velocity compared to testosterone
-
r
9,10-phenanthrenequinone + NADH + H+
? + NAD+
-
-
-
?
alpha-3-hydroxyhexobarbital + NAD+
?
-
-
-
?
alpha-tetralone + NADH + H+
? + NAD+
-
-
-
?
androst-4-ene-3beta,17beta-diol + NAD+
androst-4-ene-3beta-ol-17-one + NADH
-
75% velocity compared to testosterone
-
r
androst-4-ene-3beta,17beta-diol + NAD+
androst-4-ene-3beta-ol-17-one + NADH + H+
-
-
-
-
?
androst-5-ene-3beta,17beta-diol + NAD+
androst-5-ene-3beta-ol-17-one + NADH
-
33% velocity compared to testosterone
-
r
androstandiol + NAD+
androsterone + NADH
-
-
-
r
androstanediol + NAD+
androsterone + NADH
-
-
-
r
benzene dihydrodiol + NAD+
?
-
-
-
?
benzene dihydrodiol + NAD+
? + NADH + H+
-
-
-
?
beta-3-hydroxyhexobarbital + NAD+
?
-
-
-
?
beta-ionol + NAD+
(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
cis-benzene dihydrodiol + NAD+
?
-
-
-
?
daunorubicin + NADPH + H+
daunorubicinol + NADP+
dehydroepiandrosterone + NAD+
? + NADH + H+
-
-
-
?
estradiol + NAD+
estrone + NADH
estrone + NADPH + H+
17beta-estradiol + NADP+
-
-
-
-
?
farnesol + NAD+
?
-
-
-
?
farnesol + NAD+
? + NADH + H+
-
-
-
?
farnesol + NAD+
farnesal + NADH + H+
-
-
-
?
geraniol + NAD+
?
-
-
-
?
geraniol + NAD+
? + NADH + H+
-
-
-
?
geraniol + NAD+
geranial + NADH + H+
-
-
-
?
geranylgeraniol + NAD+
?
-
-
-
?
geranylgeraniol + NAD+
? + NADH + H+
-
-
-
?
geranylgeraniol + NAD+
geranylgeranial + NADH + H+
-
-
-
?
glycochenodeoxycholic acid + NAD+
7alpha-hydroxy-3-oxo-5-beta-cholanoyl glycine + NADH
-
-
-
?
glycolithocholic acid + NAD+
3-oxo-5beta-cholanoyl glycine + NADH
-
-
-
?
isatin + NADH + H+
? + NAD+
-
-
-
?
lithocholic acid
5beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
-
lithocholic acid + NAD+
5-beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
?
lithocholic acid + NAD+
5beta-cholan-3-one-24-oic acid + NADH
-
-
-
?
lithocholic acid + NAD+
5beta-cholan-3-one-24-oic acid + NADH + H+
-
-
-
?
morphine + NAD+
morphinone + NADH + H+
reaction of EC 1.1.1.218
-
-
?
naphthalene dihydrodiol + NAD+
? + NADH + H+
-
-
-
?
nerol + NAD+
neral + NADH + H+
-
-
-
?
progesterone + NADPH + H+
20alpha-hydroxyprogesterone + NADP+
-
-
-
-
?
prostaglandin D2 + NADPH + H+
9alpha,11beta-prostaglandin F2 + NADP+
-
-
-
-
?
pyridine-3-aldehyde + NADH + H+
? + NAD+
-
-
-
?
testosterone + NAD+
4-androstenedione + NADPH + H+
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
testosterone + NAD+
androstenedione + NADH + H+
testosterone + NADP+
androst-4-ene-3,17-dione + NADPH + H+
-
NADP is 3fold less efficient as cofactor
-
r
testosterone + NADP+
androstenedione + NADPH + H+
-
-
-
r
trans-benzene dihydrodiol + NAD+
?
-
-
-
?
additional information
?
-
(S)-1-indanol + NAD+

2,3-dihydro-1H-inden-1-one + NADH + H+
-
-
-
?
(S)-1-indanol + NAD+
2,3-dihydro-1H-inden-1-one + NADH + H+
-
-
-
?
(S)-camphorquinone + NADH + H+

? + NAD+
-
-
-
?
(S)-camphorquinone + NADH + H+
? + NAD+
-
-
-
?
11beta-hydroxytestosterone + NAD+

11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
136% velocity compared to testosterone
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
-
-
r
11beta-hydroxytestosterone + NAD+
11beta-hydroxyandrost-4-ene-3,17-dione + NADH
-
76% of testosterone oxidation rate
-
r
17beta-estradiol + NAD+

estrone + NADH + H+
-
-
-
?
17beta-estradiol + NAD+
estrone + NADH + H+
-
-
-
?
2-cyclohexen-1-ol + NAD+

2-cyclohexen-1-one + NADH + H+
-
-
-
?
2-cyclohexen-1-ol + NAD+
2-cyclohexen-1-one + NADH + H+
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+

5alpha-androstan-3,17-dione + NADH + H+
-
-
-
?
5alpha-androstan-3alpha-ol-17-one + NAD+
5alpha-androstan-3,17-dione + NADH + H+
-
-
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+

5alpha-androstane-3alpha-ol-17-one + NADH
-
72% velocity compared to testosterone
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+
5alpha-androstane-3alpha-ol-17-one + NADH
-
204% velocity compared to testosterone
-
r
5alpha-androstane-3alpha,17beta-diol + NAD+

? + NADH + H+
-
-
-
?
5alpha-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
r
5alpha-androstane-3beta,17beta-diol + NAD+

5alpha-androstane-3beta-ol-17-one + NADH
-
72% velocity compared to testosterone
-
r
5alpha-androstane-3beta,17beta-diol + NAD+
5alpha-androstane-3beta-ol-17-one + NADH
-
17% velocity compared to testosterone
-
r
5alpha-dihydrotestosterone + NAD+

androstanedione + NADH
-
-
-
r
5alpha-dihydrotestosterone + NAD+
androstanedione + NADH
-
119% initial velocity compared to testosterone
-
r
5alpha-pregnan-3alpha-ol-20-one + NAD+

5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
?
5alpha-pregnan-3alpha-ol-20-one + NAD+
5alpha-pregnan-3,20-dione + NADH + H+
-
-
-
r
5beta-androstan-17beta-ol-3-one + NAD+

5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-17beta-ol-3-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+

5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstan-3alpha-ol-17-one + NAD+
5beta-androstan-3,17-dione + NADH + H+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+

? + NADH + H+
-
-
-
?
5beta-androstane-3alpha,17beta-diol + NAD+
? + NADH + H+
-
-
-
r
5beta-pregnan-3alpha-ol-20-one + NAD+

5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
?
5beta-pregnan-3alpha-ol-20-one + NAD+
5beta-pregnan-3,20-dione + NADH + H+
-
-
-
r
beta-ionol + NAD+

(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
-
-
-
?
beta-ionol + NAD+
(3E)-4-(2,6,6-trimethylcyclohex-1-en-1-yl)but-3-en-2-one + NADH + H+
-
-
-
?
daunorubicin + NADPH + H+

daunorubicinol + NADP+
-
inactivation of the anticancer drug
-
-
r
daunorubicin + NADPH + H+
daunorubicinol + NADP+
-
the enzyme reduces daunorubicin to its corresponding alcohol daunorubicinol using NADPH as the coenzyme
-
-
r
estradiol + NAD+

estrone + NADH
-
72% velocity compared to testosterone oxidation
-
r
estradiol + NAD+
estrone + NADH
-
-
-
r
estradiol + NAD+
estrone + NADH
-
46% of testosterone oxidation rate
-
r
estradiol + NAD+
estrone + NADH
-
15% velocity compared to testosterone oxidation
-
r
testosterone + NAD+

4-androstenedione + NADPH + H+
-
-
-
?
testosterone + NAD+
4-androstenedione + NADPH + H+
-
-
-
?
testosterone + NAD+

androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
r
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
?
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+
androst-4-ene-3,17-dione + NADH + H+
-
-
-
-
testosterone + NAD+

androstenedione + NADH + H+
-
-
-
-
r
testosterone + NAD+
androstenedione + NADH + H+
-
the enzyme shows LNCaP-AKR1C3 mediates formation of testosterone, conversion of 4-androstene-3,17-dione to testosterone
-
-
r
testosterone + NAD+
androstenedione + NADH + H+
-
-
-
r
additional information

?
-
the enzyme AKR1C34 shows 3alpha/17beta/20alpha-hydroxysteroid dehydrogenase activities, substrate specificity, detailed overview. Ala54 plays a critical role in non-/recognition of the steroidal substrates. Reaction products identification by thin-layer chromatography (TLC) and liquid chromatography/mass spectrometry (LC/MS). AKR1C34 also has morphine dehydrogenase activity, EC 1.1.1.218. No activity with cyclohexanol
-
-
-
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
-
additional information
?
-
J7M9D0;
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
-
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. AKR1C28 exhibits low dehydrogenase activity for 20alpha-hydroxysteroids, but does not oxidize 3beta-hydroxysteroids (5alpha/beta-androstan-3beta-ol-17-ones and 5alpha/beta-pregnan-3beta-ol-20-ones), 17alpha-hydroxysteroids (4-androsten-17alpha-ol-3-one and 17alpha-estradiol) and 20beta-hydroxysteroids (4-pregnene-17alpha/20beta-diol-3-one and 5alpha-pregnan-20beta-ol-3-one). In the NADH-linked reverse reaction, AKR1C28 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. AKR1C28 shows higher kcat/Km values for 17beta-hydroxy-C19-steroids than those for 3alpha-hydroxysteroids, and most efficiently oxidized 17beta-estradiol. Substrate specificity, overview
-
-
-
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
-
additional information
?
-
J7M9D0;
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
-
additional information
?
-
residues Tyr118 and Phe310 play key roles in ligand binding in AKR1C27 and AKR1C28, Glu276 that is a critical residue for the NAD+ specificity is conserved in the enzymes. In the reverse reaction, the enzymes reduces several a-dicarbonyl compounds including scamphorquinone using NADH as the coenzyme. The enzyme oxidizes 3alpha- and 17beta-hydroxysteroids and also shows S-tetralol dehydrogenase activity, cf. EC 1.1.1.121 and (S)-specific secondary alcohol dehydrogenase. In the NADH-linked reverse reaction, AKR1C27 highly reduces non-steroidal alpha-dicarbonyl compounds, and also exhibits moderate activities towards TBE, alpha-tetralone and pyridine-3-aldehyde. Substrate specificity, detailed overview
-
-
-
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
-
additional information
?
-
J7M9D0;
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
-
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, and 5alpha-pregnan-20alpha-ol-3-one
-
-
-
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
-
additional information
?
-
J7M9D0;
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
-
additional information
?
-
the enzyme show NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids. No or poor activity with naphthalene dihydrodiol, morphine, beta-ionol, geraniogeraniol, farnesol, 5alpha-androstane-3alpha,17beta-diol, 5alpha-pregnan-20alpha-ol-3-one, and 4-pregnen-20alpha-3-one
-
-
-
additional information
?
-
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
-
additional information
?
-
J7M9D0;
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
-
additional information
?
-
the enzyme shows NAD+-dependent dehydrogenase activity towards other nonsteroidal alicyclic alcohols and 3alpha/17beta-hydroxy-C18/C19/C21-steroids
-
-
-
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(2E)-3-(3,3-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)prop-2-enoate
-
-
(2E)-3-(4-bromophenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
-
93.3% inhibition at 0.1 mM
(2E)-3-(4-ethylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
-
89.1% inhibition at 0.1 mM
(2E)-3-(4-methylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
-
92.7% inhibition at 0.1 mM
(2E)-3-prop-2-enoic acid
-
-
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
-
-
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoic acid
-
i.e. baccharin, a component of Brazilian propolis, exhibits a high inhibitory potency and selectivity for AKR1C3 over other AKR1C isoforms. When the cinnamic acid group of baccharin is esterified, there is a dramatic decrease in potency and selectivity for AKR1C3 in comparison to baccharin. Low or submicromolar inhibition is observed when the 3-prenyl group of baccharin is removed, and the selectivity over AKR1C2 is low. Inhibition of NAD+ dependent oxidation of S-tetralol
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
-
-
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoic acid
-
-
(2E)-3-[4-(benzoyloxy)phenyl]prop-2-enoic acid
-
-
(2E)-3-[4-(methylsulfanyl)phenyl]-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
-
93.5% inhibition at 0.1 mM
(2E)-3-[4-(pyridine-4-carbonyloxy)phenyl]prop-2-enoic acid
-
-
(2E)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
-
37% inhibition at 0.010 mM
(4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone
-
-
(E)-3-(3-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
-
-
(Z/E)-3-(4-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
-
-
(Z/E)-tert-butyl 3-(4-(3-phenylpropanoyloxy)phenyl)acrylate
-
-
1-(4-[[(2R)-2-methylpiperidin-1-yl]sulfonyl]phenyl)-1,3-dihydro-2H-pyrrol-2-one
-
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 11 nM
1-(4-[[(2R,6S)-2,6-dimethylpiperidin-1-yl]sulfonyl]phenyl)pyrrolidin-2-one
-
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 22 nM
1-[4-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)phenyl]pyrrolidin-2-one
-
IC50 value in HCT-116 cells engineered to over-express AKR1C3 is 24 nM
17alpha-methyltestosterone
-
competitive inhibition
17beta-estradiol
-
0.175 mM, 25-40% inhibition of testosterone oxidation
2'-des-methyl-indomethacin
-
the cofactor binding cavity of AKR1C3 is not perturbed upon binding of the inhibitor
-
2-(2,4-dioxo-1,3-thiazolidin-5-yl)-N-(2-hydroxyphenyl)acetamide
-
inhibitor is about 1000times more selective for isoform AKR1C3 over AKR1C2, and selectivity is even higher when compared with AKR1C1 and AKR1C4
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide
-
-
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
-
-
2-[[(3-hydroxyphenyl)carbonyl]amino]-4,5-dimethoxybenzoic acid
-
-
2-[[(3-hydroxyphenyl)carbonyl]amino]-5-nitrobenzoic acid
-
-
21-hydroxypregn-4-ene-3,20-dione
-
0.010 mM, 73% inhibition
3-((4-nitronaphthalen-1-yl)amino)benzoic acid
-
inhibitor nanomolar potency and selective inhibition of isoform AKR1C3 but also acts as an androgen receptor antagonist. It inhibits 5alpha-dihydrotestosterone stimulated androgen receptor reporter gene activity with an IC50 value of 4.7 microM and produces a concentration dependent reduction in androgen receptor levels in prostate cancer cells
3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoate
-
-
3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid
-
-
3-(phenylamino)benzoic acid
-
-
3-phenoxybenzoic acid
-
inhibitor carboxylic acid binds to the oxyanion site, in which the carboxylate group very closely overlays the acetate molecule found in other AKR1C3 structures and forms hydrogen bonds to the enzyme catalytic residues His117 and Tyr55, as well as to a conserved water network located in and near the SP3 subpocket. The 3-phenoxy ring extends into the SP1 subpocket and makes van der Waals contacts with the aromatic residues Phe306, Phe311 and Tyr319 that line the pocket
3-[(4-nitrophenyl)amino]benzoic acid
-
94fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid
-
-
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
-
-
3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(5-chlorothiophene-2-sulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide
-
-
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid
-
-
3-[[4-(methoxymethyl)phenyl]amino]benzoic acid
-
360fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
3a-phenyl-2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-one
-
inhibitor shows 17fold and 30fold selectivity against isoforms AKR1C2 and AKR1C1, respectively, and much higher selectivity against AKR1C4
3beta-cyclohexylethyl-androsterone
-
potent inhibitor
3beta-n-hexyl-androsterone
-
potent inhibitor
3beta-phenylethyl-androsterone
-
potent inhibitor
4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid
-
-
5-bromo-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
-
5-chloro-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
-
-
5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid
-
-
5alpha-Androstan-3beta-ol-17-one
-
0.005 mM, 55% inhibition
5alpha-pregnan-3beta-ol-20-one
-
0.005 mM, 52% inhibition
5beta-androstan-3,17-dione
-
product inhibition, forward reaction
5beta-androstan-3beta-ol-17-one
-
0.005 mM, 87% inhibition
5beta-dihydrotestosterone
-
product inhibition, reverse reaction
5beta-Pregnan-3beta-ol-20-one
-
0.005 mM, 81% inhibition
6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
-
-
7-hydroxyflavone
-
0.007 mM, 50% inhibition, oxidation of androstandiol
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid
-
-
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
-
-
9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide
-
-
abietic acid
-
0.010 mM, 50% inhibition, oxidation of androstandiol
Ag+
-
0.1 mM, complete inhibition
biochain A
-
0.014 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.008 mM, oxidation of androstanediol
chrysin
-
0.010 mM, 50% inhibition, oxidation of androstandiol
coumestrol
-
0.005 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.011 mM, 50% inhibition, oxidation of androstanediol
CuCl2
-
1 mM, complete inhibition
dexamethasone
-
0.10 mM, 39% inhibition
Dienstrol
-
0.010 mM, 60% inhibition
FeCl3
-
10 mM, 46% inhibition
Hg2+
-
0.1 mM, complete inhibition
ikarisoside A
competitive; competitive
Medroxyprogesterone acetate
-
0.010 mM, 22% inhibition
methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate
-
-
methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate
-
-
methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate
-
-
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
-
-
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
-
-
N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
-
N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide
-
-
N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
-
N-(4-chlorobenzoyl)-melatonin
-
-
N-benzoylanthranilic acid
-
-
N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
-
-
NaCN
-
1 mM, 50% inhibition
naringenin
-
0.010 mM, 50% inhibition, oxidation of androstandiol
p-chloromercuribenzoate
-
0.1 mM, complete inhibition
Sodium amytal
-
10 mM, 25% inhibition
stilboestrol
-
0.010 mM, 61% inhibition
tert-butyl(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
-
-
Triton X-100
-
immediate loss of 60-70% activity, remaining activity is stable for 4 days, competitive vs. testosterone, non-competitive vs. NAD+
ZnCl2
-
10 mM, 10% inhibition
[1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid
-
-
[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid
-
-
[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
-
-
[1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid
-
-
[1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
-
-
[1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
-
-
[1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
-
-
[5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
-
[5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
-
-
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid

-
250fold selectivity for the inhibition of isoform AKR1C3 over AKR1C2
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
-
in complex with AKR1C3. Compound adopts a similar binding orientation as flufenamic acid, however, its phenylamino ring projects deeper into a subpocket and confers selectivity over the other AKR1C isoforms
Hexestrol

-
Hexestrol
competitive; competitive
Hexoestrol

-
0.010 mM, 62% inhibition
hinokitiol

-
hinokitiol
competitive; competitive
indomethacin

-
-
indomethacin
-
0.10 mM, 67% inhibition
kaempferol

-
0.008 mM, 50% inhibition, oxidation of androstandiol
Phenolphthalein

-
quercetin

-
0.009 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.005 mM, oxidation of androstanediol
zearalenone

-
0.004 mM, 50% inhibition, reduction of androst-4-ene-3,17-dione, 0.002 mM, oxidation of androstanediol
zearalenone
competitive; competitive
additional information

-
development of potent and selective indomethacin analogues for the inhibition of AKR1C3 in castrate-resistant prostate cancer, overview. Increasing the length of the aliphatic side chain of indomethacin from -ethyl to -propyl leads to a 2fold reduction in AKR1C3 potency, but the compound retained 257fold selectivity for AKR1C3 over AKR1C2
-
additional information
-
screening of baccharin analogues as selective inhibitors against type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3), selectivity versus AKR1C2
-
additional information
no or poor inhibition by 7-hydroxyflavone, chrysin, quercetin, genistein, galangin, lithocholic acid, and zearalenone
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.095
(R)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C, recombinant enzyme
0.004 - 0.25
(S)-1,2,3,4-tetrahydro-1-naphthol
0.014 - 0.181
(S)-1-indanol
0.0019 - 0.0067
(S)-camphorquinone
0.148
1-Acenaphthenol
pH 7.4, 25°C, recombinant enzyme
0.0008 - 0.005
1-phenyl-1,2-propanedione
0.0021 - 0.01
16-oxoestrone
0.0021 - 0.1
17beta-estradiol
0.19 - 0.371
2,3-Butanedione
0.035 - 0.67
2-Cyclohexen-1-ol
0.0031
4-oxo-2-nonenal
-
pH 7.4, 25°C
0.0057 - 0.081
4-pregnen-3alpha-ol-20-one
0.00067 - 0.13
5alpha-androstan-17beta-ol-3-one
0.0031
5alpha-androstan-3alpha,17beta-diol
-
-
0.0022 - 0.0092
5alpha-Androstan-3alpha-ol-17-one
0.0005 - 0.0078
5alpha-androstane-3alpha,17beta-diol
0.00067 - 0.0035
5alpha-pregnan-3alpha-ol-20-one
0.00067 - 0.03
5beta-androstan-17beta-ol-3-one
0.0066
5beta-androstan-3,17-dione
-
-
0.0048
5beta-Androstan-3alpha,17beta-diol
-
-
0.0015 - 0.0023
5beta-Androstan-3alpha-ol-17-one
0.0022 - 0.02
5beta-androstane-3alpha,17beta-diol
0.0038
5beta-pregnan-3,20-dione
-
-
0.0062
5beta-pregnan-3alpha,17beta-diol-20-one
-
-
0.0036 - 0.17
5beta-Pregnan-3alpha-ol-20-one
0.0021 - 0.101
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
0.0001 - 0.0002
9,10-phenanthrenequinone
0.03
alpha-3-hydroxyhexobarbital
pH 7.4, 25°C, recombinant enzyme
0.0038 - 0.15
alpha-tetralone
0.0016
androst-4-ene-3,17-dione
-
-
0.024
androstendione
-
reduction of androstendione, pH 7.0
0.027 - 1.11
benzene dihydrodiol
0.013
beta-3-hydroxyhexobarbital
pH 7.4, 25°C, recombinant enzyme
0.0006 - 0.0097
beta-ionol
0.63
cis-benzene dihydrodiol
pH 7.4, 25°C, recombinant enzyme
0.009
estrone
-
pH 7.0, 37°C
0.0007 - 0.0012
geranylgeraniol
0.0075
glycochenodeoxycholic acid
-
-
0.003
glycolithocholic acid
-
-
0.0005 - 0.14
lithocholic acid
0.52
morphine
pH 7.4, 25°C
1.38
NADP+
pH 7.4, 25°C, with substrate S-camphorquinone
0.027
Naphthalene dihydrodiol
pH 7.4, 25°C
0.162
nerol
pH 7.4, 25°C, recombinant enzyme
0.29 - 1.1
Pyridine-3-aldehyde
0.0016 - 0.25
testosterone
1
trans-benzene dihydrodiol
pH 7.4, 25°C, recombinant enzyme
additional information
additional information
-
0.004
(S)-1,2,3,4-tetrahydro-1-naphthol

pH 7.4, 25°C
0.022
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C
0.061
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C, recombinant enzyme
0.25
(S)-1,2,3,4-tetrahydro-1-naphthol
pH 7.4, 25°C
0.014
(S)-1-indanol

pH 7.4, 25°C
0.042
(S)-1-indanol
pH 7.4, 25°C
0.11
(S)-1-indanol
pH 7.4, 25°C
0.181
(S)-1-indanol
pH 7.4, 25°C, recombinant enzyme
0.0019
(S)-camphorquinone

pH 7.4, 25°C
0.0029
(S)-camphorquinone
pH 7.4, 25°C
0.0067
(S)-camphorquinone
pH 7.4, 25°C
0.0008
1-phenyl-1,2-propanedione

pH 7.4, 25°C
0.003
1-phenyl-1,2-propanedione
pH 7.4, 25°C
0.005
1-phenyl-1,2-propanedione
pH 7.4, 25°C
0.0021
16-oxoestrone

pH 7.4, 25°C
0.003
16-oxoestrone
pH 7.4, 25°C
0.01
16-oxoestrone
pH 7.4, 25°C
0.0021
17beta-estradiol

pH 7.4, 25°C
0.0064
17beta-estradiol
-
-
0.0139
17beta-estradiol
-
cofactor S-NAD+
0.021
17beta-estradiol
-
-
0.1
17beta-estradiol
pH 7.4, 25°C
0.19
2,3-Butanedione

pH 7.4, 25°C
0.21
2,3-Butanedione
pH 7.4, 25°C
0.371
2,3-Butanedione
pH 7.4, 25°C
0.035
2-Cyclohexen-1-ol

pH 7.4, 25°C
0.066
2-Cyclohexen-1-ol
pH 7.4, 25°C
0.569
2-Cyclohexen-1-ol
pH 7.4, 25°C, recombinant enzyme
0.67
2-Cyclohexen-1-ol
pH 7.4, 25°C
0.0057
4-pregnen-3alpha-ol-20-one

pH 7.4, 25°C
0.0073
4-pregnen-3alpha-ol-20-one
pH 7.4, 25°C
0.081
4-pregnen-3alpha-ol-20-one
pH 7.4, 25°C
0.00067
5alpha-androstan-17beta-ol-3-one

pH 7.4, 25°C
0.0078
5alpha-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.13
5alpha-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0022
5alpha-Androstan-3alpha-ol-17-one

pH 7.4, 25°C
0.0092
5alpha-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0005
5alpha-androstane-3alpha,17beta-diol

pH 7.4, 25°C
0.0078
5alpha-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.00067
5alpha-pregnan-3alpha-ol-20-one

pH 7.4, 25°C
0.0035
5alpha-pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.00067
5beta-androstan-17beta-ol-3-one

pH 7.4, 25°C
0.0049
5beta-androstan-17beta-ol-3-one
-
-
0.0076
5beta-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.03
5beta-androstan-17beta-ol-3-one
pH 7.4, 25°C
0.0015
5beta-Androstan-3alpha-ol-17-one

pH 7.4, 25°C
0.0023
5beta-Androstan-3alpha-ol-17-one
pH 7.4, 25°C
0.0022
5beta-androstane-3alpha,17beta-diol

pH 7.4, 25°C
0.02
5beta-androstane-3alpha,17beta-diol
pH 7.4, 25°C
0.0036
5beta-Pregnan-3alpha-ol-20-one

pH 7.4, 25°C
0.0037
5beta-Pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0046
5beta-Pregnan-3alpha-ol-20-one
-
-
0.17
5beta-Pregnan-3alpha-ol-20-one
pH 7.4, 25°C
0.0021
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one

pH 7.4, 25°C
0.0042
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
pH 7.4, 25°C
0.101
6-tert-butyl-2,3-epoxy-4-hydroxy-5-cyclohexen-1-one
pH 7.4, 25°C
0.0001
9,10-phenanthrenequinone

pH 7.4, 25°C; pH 7.4, 25°C
0.0002
9,10-phenanthrenequinone
pH 7.4, 25°C
0.0038
alpha-tetralone

pH 7.4, 25°C
0.06
alpha-tetralone
pH 7.4, 25°C
0.15
alpha-tetralone
pH 7.4, 25°C
0.027
benzene dihydrodiol

pH 7.4, 25°C
0.12
benzene dihydrodiol
pH 7.4, 25°C
1.11
benzene dihydrodiol
pH 7.4, 25°C
0.0006
beta-ionol

pH 7.4, 25°C
0.009
beta-ionol
pH 7.4, 25°C
0.0097
beta-ionol
pH 7.4, 25°C, recombinant enzyme
0.00074
farnesol

pH 7.4, 25°C
0.0025
farnesol
pH 7.4, 25°C
0.011
farnesol
pH 7.4, 25°C, recombinant enzyme
0.0042
geraniol

pH 7.4, 25°C
0.012
geraniol
pH 7.4, 25°C
0.076
geraniol
pH 7.4, 25°C, recombinant enzyme
0.57
geraniol
pH 7.4, 25°C
0.0007
geranylgeraniol

pH 7.4, 25°C
0.00083
geranylgeraniol
pH 7.4, 25°C
0.0012
geranylgeraniol
pH 7.4, 25°C, recombinant enzyme
0.0005
isatin

pH 7.4, 25°C
0.0008
isatin
pH 7.4, 25°C
0.0011
isatin
pH 7.4, 25°C
0.0005
lithocholic acid

-
-
0.012
lithocholic acid
pH 7.4, 25°C
0.14
lithocholic acid
pH 7.4, 25°C
0.0068
NAD+

-
reduction of androstendione, pH 7.0
0.0096
NAD+
pH 7.4, 25°C
0.013
NAD+
pH 7.4, 25°C, with substrate S-tetralol
0.0181
NAD+
-
enzyme activity in hepatic microsomes
0.0185
NAD+
-
enzyme avtivity in hepatic microsomes, one individual animal
0.1
NAD+
-
solubilized enzyme
0.1
NAD+
-
solubilized with Triton X-100
0.164
NAD+
-
membrane bound
0.198
NAD+
-
oxidation of testosterone, pH 10.0
0.215
NAD+
-
oxidation of testosterone, pH 7.4
0.0026
NADH

pH 7.4, 25°C
0.0043
NADH
pH 7.4, 25°C
0.013
NADH
pH 7.4, 25°C, with substrate S-camphorquinone
0.29
Pyridine-3-aldehyde

pH 7.4, 25°C
0.3
Pyridine-3-aldehyde
pH 7.4, 25°C
1.1
Pyridine-3-aldehyde
pH 7.4, 25°C
0.0016
testosterone

-
solubilized enzyme
0.00167
testosterone
pH 7.4, 25°C
0.0022
testosterone
-
membrane bound
0.0073
testosterone
-
solubilized with Triton X-100
0.009
testosterone
-
cofactor S-NAD+
0.0095
testosterone
-
oxidation of testosterone, pH 10.0
0.014
testosterone
-
oxidation of testosterone, pH 7.4
0.0174
testosterone
-
enzyme avtivity in hepatic microsomes, one individual animal
0.033
testosterone
-
approximate value, data fitted by eye
0.037
testosterone
pH 7.4, 25°C
0.25
testosterone
pH 7.4, 25°C
additional information
additional information

Michaelis-Menten kinetics; Michaelis-Menten kinetics; Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
J7M9D0;
Michaelis-Menten kinetics; Michaelis-Menten kinetics; Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
Michaelis-Menten kinetics; Michaelis-Menten kinetics; Michaelis-Menten kinetics of wild-type and mutant enzymes, overview
-
additional information
additional information
Michaelis-Menten kinetics
-
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0.021
(2E)-3-(3,3-dimethyl-3,4-dihydro-2H-1-benzopyran-6-yl)prop-2-enoate
Homo sapiens;
-
pH 7.0, 37°C
0.0136
(2E)-3-(4-bromophenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0136
(2E)-3-(4-ethylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0134
(2E)-3-(4-methylphenyl)-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0047
(2E)-3-prop-2-enoic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0001
(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0086
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
Homo sapiens;
-
pH 7.0, 37°C
0.00044
(2E)-3-[4-(acetyloxy)-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0063
(2E)-3-[4-(benzoyloxy)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0058
(2E)-3-[4-(methylsulfanyl)phenyl]-2-[4-(methylsulfonyl)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.068
(2E)-3-[4-(pyridine-4-carbonyloxy)phenyl]prop-2-enoic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0097
(2E)-3-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-enoate
Homo sapiens;
-
pH 7.0, 37°C
0.00356
(4-chlorophenyl)(5-methoxy-2-methyl-1H-indol-1-yl)methanone
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00096
(E)-3-(3-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
Homo sapiens;
-
pH 7.0, 37°C
0.0023
(Z/E)-3-(4-((3-phenylpropanoyl)oxy)phenyl)acrylic acid
Homo sapiens;
-
pH 7.0, 37°C
0.632
(Z/E)-tert-butyl 3-(4-(3-phenylpropanoyloxy)phenyl)acrylate
Homo sapiens;
-
pH 7.0, 37°C
0.000094
1-(4-[[(2R)-2-methylpiperidin-1-yl]sulfonyl]phenyl)-1,3-dihydro-2H-pyrrol-2-one
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000056
1-(4-[[(2R,6S)-2,6-dimethylpiperidin-1-yl]sulfonyl]phenyl)pyrrolidin-2-one
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000052
1-[4-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)phenyl]pyrrolidin-2-one
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000213
2-(2,4-dioxo-1,3-thiazolidin-5-yl)-N-(2-hydroxyphenyl)acetamide
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.00882
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(2-methylbenzene-1-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00111
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-cyanobenzene-1-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00786
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-fluorobenzene-1-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0058
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methoxybenzene-1-sulfonyl)acetamide
Homo sapiens;
-
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0124
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-methylbenzene-1-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00252
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(4-phenoxybenzene-1-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00373
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(5-chlorothiophene-2-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.012
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(methanesulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00119
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(naphthalene-2-sulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00021
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00265
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[3-(trifluoromethyl)benzene-1-sulfonyl]acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00634
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]acetamide
Homo sapiens;
-
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00207
2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00074
2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]-N-(trifluoromethanesulfonyl)acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0052
2-[[(3-hydroxyphenyl)carbonyl]amino]-4,5-dimethoxybenzoic acid
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.00084
2-[[(3-hydroxyphenyl)carbonyl]amino]-5-nitrobenzoic acid
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.08
3-((4-nitronaphthalen-1-yl)amino)benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.1
3-(5-methoxy-2-methyl-1H-indol-3-yl)propanoic acid
Homo sapiens;
-
above, 100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000036
3-[(4-nitrophenyl)amino]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00015
3-[1-(4-chlorobenzoyl)-2-ethyl-5-methoxy-1H-indol-3-yl]propanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007 - 0.00009
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
0.00029
3-[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]propanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00022
3-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]propanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00012
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00029
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-2-methylpropanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00325
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(2-methylbenzene-1-sulfonyl)propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00311
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(4-methylbenzene-1-sulfonyl)propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00553
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)-2-methylpropanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00034
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(methanesulfonyl)propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00254
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(naphthalene-2-sulfonyl)propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00144
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-(trifluoromethanesulfonyl)propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00469
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(propan-2-yl)benzene-1-sulfonyl]propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0025
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethoxy)benzene-1-sulfonyl]propanamide
Homo sapiens;
-
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00111
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]-N-[4-(trifluoromethyl)benzene-1-sulfonyl]propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00013
3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000054
3-[[4-(methoxymethyl)phenyl]amino]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000062
3-[[4-(trifluoromethyl)phenyl]amino]benzoic acid
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00546
3a-phenyl-2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-one
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.00015
4-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]butanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0019
5-bromo-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.0022
5-chloro-2-[[(3-hydroxyphenyl)carbonyl]amino]benzoic acid
Homo sapiens;
-
pH 7.0, temperature not specified in the publication
0.0024
5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.000279
6-methoxy-9-[3-(trifluoromethyl)benzoyl]-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00034
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-2-carboxylic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00016
9-(4-chlorobenzoyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxylic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00507
9-(4-chlorobenzoyl)-N-(methanesulfonyl)-6-methoxy-2,3,4,9-tetrahydro-1H-carbazole-3-carboxamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.021
ferulic acid
Homo sapiens;
-
pH 7.0, 37°C
0.00013 - 0.02
ikarisoside A
0.0001
indomethacin
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.086
m-coumaric acid
Homo sapiens;
-
pH 7.0, 37°C
0.02278
methyl 5-methoxy-3-(2-oxobutyl)-1H-indole-1-carboxylate
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.01134
methyl [1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetate
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00564
methyl [1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetate
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00224 - 0.00759
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
0.00754 - 0.01571
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
0.00209
N-(4-acetylbenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00265
N-(4-acetylbenzene-1-sulfonyl)-3-[1-(4-chlorobenzoyl)-5-methoxy-3-methyl-1H-indol-2-yl]propanamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00397
N-(4-bromobenzene-1-sulfonyl)-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00194
N-[2,5-bis(trifluoromethyl)benzene-1-sulfonyl]-2-[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetamide
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0022 - 0.015
noranhydroicaritin
0.199
p-coumaric acid
Homo sapiens;
-
pH 7.0, 37°C
0.00065 - 0.02
Phenolphthalein
607
tert-butyl(2E)-3-[3-(3-methylbut-2-en-1-yl)-4-[(3-phenylpropanoyl)oxy]phenyl]prop-2-enoate
Homo sapiens;
-
pH 7.0, 37°C
0.0091 - 0.05
zearalenone
0.0005
[1-(4-chlorobenzoyl)-5-fluoro-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00025
[1-(4-chlorobenzoyl)-5-fluoro-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00096
[1-(4-chlorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007
[1-(4-chlorobenzoyl)-5-methoxy-2-propyl-1H-indol-3-yl]acetic acid
Homo sapiens;
-
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00496
[1-(4-fluorobenzoyl)-5-methoxy-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00071
[1-(4-fluorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00012
[1-[4-(chloromethyl)benzoyl]-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00223
[5-fluoro-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00014
[5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00521
[5-methoxy-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens;
-
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00108
[5-methoxy-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens;
-
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00016
[5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00244
[5-methoxy-2-methyl-1-[3-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00027
[5-methoxy-2-methyl-1-[4-(trifluoromethyl)benzoyl]-1H-indol-3-yl]acetic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00007
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid

Homo sapiens;
-
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00009
3-[1-(4-chlorobenzoyl)-3-ethyl-5-methoxy-1H-indol-2-yl]propanoic acid
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.009
Hexestrol

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.013
Hexestrol
Mesocricetus auratus;
A0A097ZMY7
pH 7.4, 25°C, recombinant enzyme
0.05
Hexestrol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
above, pH 7.4, 25°C, recombinant wild-type and mutant enzymes; pH 7.4, 25°C, recombinant enzyme
0.073
Hexestrol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.002
hinokitiol

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0026
hinokitiol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant Y118F/F310I enzyme
0.0032
hinokitiol
Mesocricetus auratus;
A0A097ZMY7
pH 7.4, 25°C, recombinant enzyme
0.01
hinokitiol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant Y118F enzyme
0.013
hinokitiol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant F310I enzyme
0.037
hinokitiol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.042
hinokitiol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.017
icarisid II

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.021
icarisid II
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.05
icarisid II
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
above, pH 7.4, 25°C, recombinant enzyme
0.00013
ikarisoside A

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0004
ikarisoside A
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant Y118F/F310I enzyme
0.00049
ikarisoside A
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant Y118F enzyme
0.009
ikarisoside A
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme; pH 7.4, 25°C, recombinant wild-type enzyme
0.013
ikarisoside A
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.02
ikarisoside A
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant mutant F310I enzyme
0.015
kaempferol

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.02
kaempferol
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
above, pH 7.4, 25°C, recombinant enzyme; above, pH 7.4, 25°C, recombinant enzyme; pH 7.4, 25°C, recombinant enzyme
0.00224
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate

Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00759
methyl [5-methoxy-1-(4-methoxybenzoyl)-2-methyl-1H-indol-3-yl]acetate
Homo sapiens;
-
100 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.00754
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate

Homo sapiens;
-
110 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.01571
methyl [5-methoxy-2-methyl-1-(4-methylbenzoyl)-1H-indol-3-yl]acetate
Homo sapiens;
-
111 mM Tris-HCl buffer, 37°C, pH not specified in the publication
0.0022
noranhydroicaritin

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0064
noranhydroicaritin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.015
noranhydroicaritin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.00065
Phenolphthalein

Mesocricetus auratus;
A0A097ZMY7
pH 7.4, 25°C, recombinant enzyme
0.007
Phenolphthalein
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.017
Phenolphthalein
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.02
Phenolphthalein
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.012
quercetin

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.018
quercetin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.026
quercetin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0024
quercitrin

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0025
quercitrin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.04
quercitrin
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.0091
zearalenone

Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
pH 7.4, 25°C, recombinant enzyme
0.05
zearalenone
Oryctolagus cuniculus;
G1T465, J7M9D0, J7MBS9
above, pH 7.4, 25°C, recombinant enzyme; above, pH 7.4, 25°C, recombinant wild-type and mutant enzymesenzyme; pH 7.4, 25°C, recombinant enzyme
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