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0.000006
(+)-LY191704
-
-
0.000004
(-)-LY191704
-
-
0.00092
(10bR)-8-chloro-4,10b-dimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
-
isoform I
0.0011
(10bR)-8-chloro-4,5,10b-trimethyl-4a,5,6,10b-tetrahydrophenanthridin-2(1H)-one
-
isoform I
0.00026 - 0.0012
(4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid
0.000035
(5alpha,20-R)-4-Diazo-21-hydroxy-20-methylpregnan-3-one
-
at 25°C formation of the reversible EI complex is not rate-limiting for enzyme inactivation, and this is expressed as saturation kinetics for the inhibition reaction
0.000085
17-diisopropylcarbamoyl-2-androsten-3-carboxylate
-
-
0.000007 - 0.000018
17-diisopropylcarbamoyl-3,5-androstadien-3-carboxylate
-
-
0.00003
17-diisopropylcarbamoyl-3-androsten-3-carboxyate
-
-
0.0022
17-diisopropylcarbamoyl-androstan-3-carboxylate
-
-
0.0045
17-tert-butylcarbamoyl-3,5-androstadien-3-carbaldehyde
-
-
0.000033
17-tert-butylcarbamoyl-3,5-androstadien-3-carboxylate
-
-
0.0042
17-tert-butylcarbamoyl-3,5-androstadien-3-ol
-
-
0.000036 - 0.0093
17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
0.026 - 0.036
17beta-estradiol
0.146
17beta-hydroxyandrosta-1,4-diene-3-one
-
-
0.000315 - 0.01
2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.00006
20alpha-hydroxypregn-4-en-3-one
-
-
0.0049
4,16-androstadien-3-one
-
-
0.0000058
4,8-dimethyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I
0.0000062 - 0.0000118
4-Aza-4-methyl-5alpha-pregnane-3,20-dione
0.0126
4-bromo-17alpha-(p-fluorobenzoyloxy)-4-pregnene-3,20-dione
-
pH 6.0, 25°C
0.000002 - 0.0000084
4-methyl-azasteroid
0.000026 - 0.01
7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.00032 - 0.0025
7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
0.0000027
8-chloro-4-methyl-1,2,5,6-tetrahydro-3H-pyrido[1,2-a]quinolin-3-one
-
isoform I
0.0000003 - 0.0041
acylate episteride
-
0.0000043 - 0.000017
dutasteride
0.000001 - 0.005
finasteride
0.00048 - 0.0027
penta-O-galloyl-beta-D-glucose
0.0026 - 0.0065
theaflavin-3'-gallate
0.00036 - 0.0056
theaflavin-3,3'-digallate
additional information
additional information
-
0.00026
(4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid
-
isoform II, Ki,app-value
0.0012
(4aS)-7-chloro-4a-methyl-2,3,4,4a-tetrahydrophenanthrene-2-carboxylic acid
-
isoform I, Ki,app-value
0.000036
17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
-
pH 7.0, 30°C, low Km-isoform from prostate
0.0049
17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
-
pH 7.0, 30°C, high Km-isoform from prostate
0.0093
17beta-(N-tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
-
pH 7.0, 30°C, isoform from breast skin
0.026
17beta-estradiol
-
intercept inhibition constant
0.036
17beta-estradiol
-
slope inhibition constant
0.000315
2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform I, Ki,app-value
0.01
2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform II, Ki,app-value
0.0000062
4-Aza-4-methyl-5alpha-pregnane-3,20-dione
-
versus progesterone
0.0000118
4-Aza-4-methyl-5alpha-pregnane-3,20-dione
-
versus NADPH
0.000002
4-methyl-azasteroid
-
iosenzyme 2
0.000003
4-methyl-azasteroid
-
iosenzyme 1
0.000003
4-methyl-azasteroid
-
iosenzyme 1
0.000003
4-methyl-azasteroid
-
iosenzyme 2
0.000004
4-methyl-azasteroid
-
iosenzyme 2
0.000008
4-methyl-azasteroid
-
iosenzyme 1
0.0000084
4-methyl-azasteroid
-
-
0.000026
7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform I, Ki,app-value
0.01
7-bromo-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform II, Ki,app-value
0.00032
7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform I, Ki,app-value
0.0025
7-chloro-2,4a,9,10-tetrahydrophenanthrene-2-carboxylic acid
-
isoform II, Ki,app-value
0.0000003
acylate episteride
-
iosenzyme 2
-
0.0000005
acylate episteride
-
iosenzyme 2
-
0.000004
acylate episteride
-
iosenzyme 2
-
0.00002
acylate episteride
-
iosenzyme 1
-
0.0005
acylate episteride
-
iosenzyme 1
-
0.0041
acylate episteride
-
iosenzyme 1
-
0.0000043
dutasteride
-
wild-type, 30 min reaction time
0.000017
dutasteride
-
wild-type, 10 min reaction time
0.000001
finasteride
-
iosenzyme 2
0.000004
finasteride
-
iosenzyme 2
0.000005
finasteride
-
iosenzyme 2
0.000005
finasteride
-
isozyme 5alphaR-2
0.000006
finasteride
-
iosenzyme 1
0.000023
finasteride
-
wild-type, 30 min reaction time
0.00006
finasteride
-
wild-type, 10 min reaction time
0.00022
finasteride
-
iosenzyme 1
0.0003
finasteride
-
isozyme 5alphaR-1
0.001
finasteride
-
iosenzyme 1
0.0013
finasteride
-
pH 7.0, 30°C, low Km-isoform from prostate
0.00154
finasteride
-
pH 6.0, 25°C
0.0028
finasteride
-
pH 7.0, 30°C, high Km-isoform from prostate
0.005
finasteride
-
pH 7.0, 30°C, isoform from breast skin
0.0043
NADP+
-
versus NADPH
0.0319
NADP+
-
versus progesterone
0.00048
penta-O-galloyl-beta-D-glucose
-
pH 6.5, 37°C, versus NADPH
0.0027
penta-O-galloyl-beta-D-glucose
-
pH 6.5, 37°C, versus testosterone
0.0026
theaflavin-3'-gallate
-
pH 6.5, 37°C, versus NADPH
0.0065
theaflavin-3'-gallate
-
pH 6.5, 37°C, versus testosterone
0.00036
theaflavin-3,3'-digallate
-
pH 6.5, 37°C, versus NADPH
0.0056
theaflavin-3,3'-digallate
-
pH 6.5, 37°C, versus testosterone
additional information
additional information
-
inhibition kinetics
-
additional information
additional information
-
isozyme-specific IC50-values of diverse inhibitors, overview
-
additional information
additional information
-
the majority of the enzyme variants result in a reduction of the apparent Ki for both finasteride and dutasteride from 10 min to the 30 min reaction like the wild-type enzyme, but several variants result in an increase of the apparent Ki for each inhibitor or no significant change between the 10 min and 30 min reactions, thus exhibiting time independent inhibition
-