Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(1R)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
-
-
(1S)-2-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-1-phenylethanol
-
-
(5Z)-5-(1H-imidazol-5-ylmethylene)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
-
50% inhibition at 0.0069 mM, selective for CYP11B1
(R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile
FAD286; FAD286, CYP11B2 inhibitor, inhibited CYP11B2 and CYP11B1 activities
1-(1H-inden-2-yl)-1H-imidazole
-
CYP11B2 IC50: 448 nM, no inhibition of CYP11B1, recombinant enzymes
1-(3,4-dihydronaphthalen-2-yl)-1H-imidazole
-
CYP11B1 IC50: 639 nM, CYP11B2 IC50: 334 nM, recombinant enzymes
1-(3-bromobenzyl)-1H-imidazole
-
-
1-(3-chlorobenzyl)-1H-imidazole
-
-
1-(3-cyanobenzyl)-1H-imidazole
-
-
1-(3-fluorobenzyl)-1H-imidazole
-
-
1-(4-aminobenzyl)-1H-imidazole
-
-
1-(4-bromobenzyl)-1H-imidazole
-
-
1-(4-bromobenzyl)-5-phenyl-1H-imidazole
-
-
1-(4-chlorobenzyl)-1H-imidazole
-
-
1-(4-chlorobenzyl)-5-phenyl-1H-imidazole
-
-
1-(4-cyanobenzyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(2-fluorophenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(2-methylphenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(3-fluorophenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(3-methylphenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(4-fluorophenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(4-methylphenyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(4-pyridyl)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(methyl carboxylate)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-(methylene-acetate)-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-bromo-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-formyl-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-hydroxymethyl-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-methyl-1H-imidazole
-
-
1-(4-cyanobenzyl)-5-phenyl-1H-imidazole
-
-
1-(4-fluorobenzyl)-1H-imidazole
-
-
1-(4-fluorobenzyl)-5-phenyl-1H-imidazole
-
-
1-(4-methoxybenzyl)-5-phenyl-1H-imidazole
-
-
1-(6-methoxy-3,4-dihydronaphthalen-2-yl)-1H-imidazole
-
CYP11B1 IC50: 763 nM, CYP11B2 IC50: 411 nM, recombinant enzymes
1-benzyl-5-phenyl-1H-imidazole
-
-
11beta-hydroxy-dehydroepiandrosterone
-
50% inhibition at 0.0033 mM
11beta-hydroxy-progesterone
-
50% inhibition at 0.0004 mM
11beta-hydroxy-testosterone
-
50% inhibition at 0.0017 mM
18-vinyldeoxycorticosterone
-
deoxycorticosterone analog, very strong and reversible inhibitor for deoxycorticosterone and corticosterone oxidation, 0.001 mM leads to decrease in corticosterone production with 30% of total activity after 1 min, 100fold more efficient than 18-vinylprogesterone for inhibition of 11beta-hydroxylation step, only 6fold of more inhibition of 18-hydroxylation step
2,3-dichloro-N-(pyridin-3-yl)benzamide
-
51% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B22
2,4,5-trifluoro-N-(pyridin-3-yl)benzamide
-
70% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B23
2-(4-chlorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-(4-fluorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-benzyl-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-fluoro-N-(pyridin-3-yl)benzamide
-
34% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B19
2-[(1R)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(3-methoxy-2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(cyclopropylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(3-methyloxetan-3-yl)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(propan-2-yloxy)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
3,4-difluoro-N-(pyridin-3-yl)benzamide
-
83% inhibition of CYP11B2 at 0.5 mM, 6% inhibition of CYP11B20
3,4-dimethoxy-N-(pyridin-3-yl)benzamide
-
-
3-(1-benzyl-1H-imidazol-5-yl)-1-propanol
-
-
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine
-
CYP11B1 IC50: 2117 nM, CYP11B2 IC50: 30 nM, recombinant enzymes
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine
-
CYP11B1 IC50: 1268 nM, CYP11B2 IC50: 7 nM, recombinant enzymes
3-(1H-imidazol-1-ylmethyl)aniline
-
-
3-(3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B1 IC50: 1729 nM, CYP11B2 IC50: 7 nM, recombinant enzymes
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B1 IC50: 503 nM, CYP11B2 IC50: 5 nM, recombinant enzymes
3-(4-ethyl-3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B1 IC50: 1615 nM, CYP11B2 IC50: 176 nM, recombinant enzymes
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B1 IC50: 1291 nM, CYP11B2 IC50: 13 nM, recombinant enzymes
3-(6-methoxy-1H-inden-2-yl)pyridine
-
competitive, CYP11B1 IC50: 5684 nM, CYP11B2 IC50: 4 nM, recombinant enzymes
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine
-
competitive, CYP11B1 IC50: 578 nM, CYP11B2 IC50: 2 nM, recombinant enzymes
3-(7-methoxy-3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B2 IC50: 45 nM, no inhibition of CYP11B1, recombinant enzymes
3-chloro-N-(pyridin-3-yl)benzamide
-
26% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B18
3-fluoro-N-(pyridin-3-yl)benzamide
-
47% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B17
3-[(Z)-2,3-dihydro-1H-inden-1-ylidenemethyl]pyridine
-
50% inhibition at 0.087 mM
3-[(Z)-2-phenylvinyl]pyridine
-
CYP11B1 IC50: 288 nM, CYP11B2 IC50: 735 nM, no inhibition by the 3-[(E)-2-phenylvinyl]pyridine isomer, recombinant enzymes
3-[1-(4-bromobenzyl)-1H-imidazol-5-yl]-1-propanol
-
-
3-[1-(4-chlorobenzyl)-1H-imidazol-5-yl]-1-propanol
-
-
3-[1-(4-cyanobenzyl)-1H-imidazol-5-yl]-1-propanol
-
-
3-[1-(4-fluorobenzyl)-1H-imidazol-5-yl]-1-propanol
-
-
3-[1-(4-methoxybenzyl)-1H-imidazol-5-yl]-1-propanol
-
-
3-[2-[(1S)-1-(4-chlorophenyl)ethyl]-3,3-dioxido-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazin-4-yl]-2-methylpropan-1-ol
-
-
4-((5-phenyl-1H-imidazol-1-yl)methyl)benzonitrile
-
-
4-(2-methylpropyl)-2-(thiophen-2-ylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
4-(2-methylpropyl)-2-[4-(trifluoromethoxy)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
4-(2-methylpropyl)-2-[4-(trifluoromethyl)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide
-
-
4-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine
-
CYP11B1 IC50: 2529 nM, CYP11B2 IC50: 2834 nM, recombinant enzymes
4-(7-benzyl-6-oxo-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazin-5-yl)benzonitrile
-
-
4-bromo-N-(pyridin-3-yl)benzamide
-
64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B9
4-chloro-N-(pyridin-3-yl)benzamide
-
88% inhibition of CYP11B2 at 0.5 mM, 5% inhibition of CYP11B8
4-cyano-N-(pyridin-3-yl)benzamide
-
81% inhibition of CYP11B2 at 0.5 mM, 9% inhibition of CYP11B15
4-fluoro-N-(pyridin-3-yl)benzamide
-
86% inhibition of CYP11B2 at 0.5 mM, 7% inhibition of CYP11B7
4-methoxy-N-(pyridin-3-yl)benzamide
-
19% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B10
4-methyl-N-(pyridin-3-yl)benzamide
-
25% inhibition of CYP11B2 at 0.5 mM, no% inhibition of CYP11B13
4-nitro-N-(pyridin-3-yl)benzamide
-
64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B16
4-[(Z)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]pyridine
-
50% inhibition at 0.034 mM, selective for CYP11B1
5-bromo-N-(pyridin-3-yl)pyridine-3-carboxamide
-
29% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B5
5-[(1E)-1-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)ethyl]isoquinoline
-
50% inhibition at 0.096 mM
5-[(E)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]isoquinoline
-
50% inhibition at 0.058 mM, selective for CYP11B1
5-[(E)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]pyrimidine
-
50% inhibition at 0.027 mM, very selective for CYP11B1
5-[(Z)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]isoquinoline
-
50% inhibition at 0.026 mM, selective for CYP11B1
5-[(Z)-2,3-dihydro-1H-inden-1-ylidenemethyl]-1H-imidazole
-
50% inhibition at 0.0061 mM
5-[(Z)-3,4-dihydronaphthalen-1(2H)-ylidenemethyl]-1H-imidazole
-
50% inhibition at 0.0033 mM
6,6-dimethyl-8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
6-(5,8-dihydroisoquinolin-4-yl)-3,4-dihydroquinolin-2(1H)-one
-
94% inhibition of CYP11B2 at 0.5 mM, 91% inhibition of CYP11B1
6-methoxydihydronaphthalene
-
-
8-(1H-imidazol-1-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(2,3'-bipyridin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(5-ethoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(5-fluoropyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(5-hydroxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(5-methoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(5-phenylpyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one
-
-
8-(isoquinolin-4-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-4-thione
-
-
8-(pyrimidin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(2,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(2-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(2-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(3,4-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(3,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(3-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(3-hydroxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(3-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(4-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(4-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(propan-2-yloxy)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-(trifluoromethyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
8-[5-[3-(trifluoromethyl)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one
-
-
9-(5-methoxypyridin-3-yl)-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one
-
-
9-(pyridin-3-yl)-1,2,6,7-tetrahydro-5H-pyrido[ 3,2,1-ij]quinolin-3-one
-
-
9-[6-(isoquinolin-4-yl)pyridin-3-yl]-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one
-
-
acetone
-
10%, v/v, complete inhibition of hydroxylation
Anti-11beta-hydroxylase IgG
-
antiserum
-
produced by rabbits
-
ascorbate
-
without NADH, inhibition of aldosterone synthetase
atenolol
-
potent inhibition of CYP11B2, recombinant enzyme
clotrimazole
-
azole derivative, antimycotic drug, strong dose-dependent inhibition
corticosterone
-
competitive inhibition of 11beta-hydroxylase activity
deoxycorticosterone
-
competitive substrate inhibition
diphosphatidyl glycerol
-
cardiolipin, dipalmitoyl phasphatidylcholine vesicles, 50% inhibition with 4-5 mol%, complete inhibition at 15 mol%
erythromycin
-
potent inhibition of CYP11B2, recombinant enzyme
ethanol
-
10%, v/v, complete inhibition of hydroxylation
FAD286
-
inhibitor of 11-beta-hydroxylase CYP11B1
HgCl2
-
0.2 mM, 50% inhibition
iron-sulfur protein
-
adrenodoxin, at high concentrations, 25% inhibition
-
ketoprofene
-
potent inhibition of CYP11B2, recombinant enzyme
methanol
-
10%, v/v, complete inhibition of hydroxylation
methyl 3-(1-benzyl-1H-imidazol-5-yl)-propanoate
-
-
methyl 3-[1-(4-bromobenzyl)-1H-imidazol-5-yl]-propanoate
-
-
methyl 3-[1-(4-chlorobenzyl)-1H-imidazol-5-yl]-propanoate
-
-
methyl 3-[1-(4-cyanobenzyl)-1H-imidazol-5-yl]-propanoate
-
-
methyl 3-[1-(4-fluorobenzyl)-1H-imidazol-5-yl]-propanoate
-
-
methyl 3-[1-(4-methoxybenzyl)-1H-imidazol-5-yl]-propanoate
-
-
methyltrienolone
-
synthetic androgen, used as photoaffinity ligand and substrate analog, covalent binding, 0.1 mM inhibits cortisol synthesis, during photolabeling radioactivity incorporation via radioactive methyltrienolone is blocked by 11-deoxycorticosterone, so it binds to the conserved substrate binding region Trp428-Leu429-Asp430-Arg431 between beta3-sheet and the L-helix analysed by trypsin digest
metyrapol
-
11beta-hydroxylase inhibition, 40.8% by racemate, 38.1% by (+)-enantiomer and 33.8% by (-)-enantiomer, each 0.4 mM
miconazole
-
azole derivative, antimycotic drug, strong dose-dependent inhibition
N-(pyridin-3-yl)-4-(trifluoromethoxy)benzamide
-
-
N-(pyridin-3-yl)-4-(trifluoromethyl)benzamide
-
-
N-(pyridin-3-yl)benzamide
-
30% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B6
N-(pyridin-3-yl)biphenyl-4-carboxamide
-
-
N-(pyridin-3-yl)pyridine-3-carboxamide
-
8% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B3
N-(pyridin-3-yl)pyridine-4-carboxamide
-
39% inhibition of CYP11B2 at 0.5 mM, 4% inhibition of CYP11B4
norharman
-
beta-carboline, high affinity type II ligand to both cytochromes, progesterone binding to CYP17 competitively inhibited
p-chloromercuribenzoate
-
1 mM
PCMB
-
0.1 mM, 50% inhibition
phenazine methosulfate
-
1 mM, crude extract
phosphatidylcholine
-
unsaturated increasing dioleoyl/diphytanoyl phosphatidylcholine
progesterone
-
progesterone acts as a competitive inhibitor for 11beta-hydroxylase and aldosterone synthase, inhibits aldosterone production by wild-type CYP11B1 and chimeric mutant CYP11B1/B2 in HEK-293 cells. The wild-type is more strongly inhibited than the chimera
SKF 525A
-
little inhibition of the purified 11beta-hydroxylase, 18-hydroxylation and aldosterone synthesis of corticosterone are inhibited
sodium cholate
-
0.2% effect nearly 20% inhibition
spironolactone
-
diuretic and antihypertensive drug, competitive aldosterone antagonist, slight inhibition
sulfhydryl reagents
-
strongly
testosterone
-
potent inhibition of CYP11B2, recombinant enzyme
[3-(1H-imidazol-1-ylmethyl)phenyl]methanol
-
-
[4-(1H-imidazol-1-ylmethyl)phenyl]methanol
-
-
18-ethynylprogesterone
-
mechanism-based inhibition; weaker than 18-vinylprogesterone, inhibitor of aldosterone synthesis for both activities, stronger for 18-hydroxylation inhibition
18-ethynylprogesterone
-
mechanism-based inhibition; progesterone analog, time-dependent pseudo-first-order inactivation, concentration dependent
18-ethynylprogesterone
-
suicide-substrate of aldosterone biosythesis, inhibits more strongly the 18-hydroxylation step
18-vinylprogesterone
-
competitive, potent inhibitor of aldosterone synthesis for both activities, 18-hydroxylation more effected, 65% inhibition of corticosterone and 11-deoxy-18-hydroxycorticosterone production by 0.03 mM; mechanism-based inhibition
18-vinylprogesterone
-
mechanism-based inhibition; progesterone analog, with NADPH, time and concentration dependent, irreversible, pseudo-first-order process, covalent binding to and destruction of prosthetic heme group, 5fold more effective than its acetylenic analog 18-ethynylprogesterone
18-vinylprogesterone
-
with 0.001 mM no inhibition detectable, with 0.01 mM 23% decrease in corticosterone production, better suicide-substrate of aldosterone biosythesis than 18-ethynylprogesterone, inhibits more strongly the 18-hydroxylation step
Anti-11beta-hydroxylase IgG
-
polyclonal, raised in rabbits, inhibition of 11-beta/18-hydroxylation and aldosterone synthesis of corticosterone
-
Anti-11beta-hydroxylase IgG
-
cross-reaction with 51 kDa protein
-
CO
-
-
CO
-
affects 11beta-/19-hydroxylase reaction
fadrozole
-
50% inhibition at 0.001 mM
fadrozole
-
50% inhibition at 0.010 mM
fadrozole
-
CYP11B2 IC50: 1 nM, CYP11B1 IC50: 10 nM, recombinant enzymes
fadrozole
-
in vitro and in vivo inhibition
fadrozole
-
inhibitor of CYP11B2
fadrozole
isoform-selective inhibitor binding. Fadrozole binds to aldosterone synthase in the R-configuration, using part of the active site cavity pointing toward the egress channel
ketoconazole
-
-
ketoconazole
-
azole derivative, antimycotic drug, strong dose-dependent inhibition
ketoconazole
-
50% inhibition at 0.081 mM
ketoconazole
-
CYP11B2 IC50: 81 nM, CYP11B1 IC50: 224 nM, recombinant enzymes
Metyrapone
-
competitive substrate inhibition
Metyrapone
-
competitive with substrate, affects strongly 11beta-/18-hydroxylation and 11beta-/19-hydroxylation
Metyrapone
-
diagnostic inhibitor, strong inhibition, 0.02 mM complete inhibition
Metyrapone
-
79% inhibition of CYP11B2 at 0.5 mM, 94% inhibition of CYP11B2
Metyrapone
-
11beta-hydroxylase, 39.7% inhibition by 0.4 mM
Metyrapone
-
inhibition of the purified 11beta-hydroxylase, 18-hydroxylation and aldosterone synthesis of corticosterone are inhibited
additional information
-
development and analysis of inhibitory potency of diverse inhibitors by superimposition of active and non-active compounds, modelling based on two pyridyl substituted acenaphthene derivatives, IC50 values of good inhibitors below 100 nM and of weak inhibitors above 300 nM, overview
-
additional information
-
synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis, ligand-protein interactions, docking and molecular dynamics studies using homology-modeled CYP11B2 structure, overview
-
additional information
-
effects of enzyme inhibition of steroid biosynthesis and mineralcorticoid formation, overview
-
additional information
-
a sulfonamide-imidazole scaffold is a potent inhibitor of CYP11B2, the scaffold can achieve high levels of selectivity for CYP11B2 over CYP11B1, overview. Evaluation of a lactam series of derivatives of the R-enantiomer of fadrozole, FAD286, homology modelling, overview
-
additional information
-
synthesis of 23 N-(pyridin-3-yl)benzamides and evaluation for their potential to inhibit steroid-11beta-hydroxylase CYP11B1 and aldosterone synthase CYP11B2, overview. N-(Pyridin-3-yl)benzamides are a highly selective class of CYP11B2 inhibitors in vitro. No or poor inhibition of both isozymes by 3i, 3j, 3l, and 3s
-
additional information
-
three-dimensional modeling of CYP11B2 to model the binding modes of the natural substrate 18-hydroxycorticosterone and the CYP11B2 inhibitor R-fadrozole, overview. Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase, overview. Molecular docking in the CYP11B1 and CYP11B2 models
-
additional information
-
development of 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones and structurally related aldosterone synthase inhibitors, molecular modelling, overview. No inhibition of both isozymes by 32 and 15
-
additional information
structure homology modelling for inhibitor design, overview
-
additional information
structure homology modelling for inhibitor design, overview
-
additional information
-
structure homology modelling for inhibitor design, overview
-
additional information
-
estradiol has no effect on aldosterone production by wild-type CYP11B1 and chimeric mutant CYP11B1/B2 in HEK-293 cells
-
additional information
-
conversion of labelled steroid to labelled aldosterone is inhibited by the addition of an excess of the same unlabelled steroid
-
additional information
-
no inhibition with Harman, tetrahydronorharman and tetrahydroharman
-
additional information
-
dexamethasone represses the enzyme in nervous system tissues, overview
-