1.14.15.4 (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 - 83196 1.14.15.4 (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 - 83197 1.14.15.4 (5Z)-5-(1H-imidazol-5-ylmethylene)-5,6,7,8-tetrahydronaphthalene-2-carbonitrile 50% inhibition at 0.0069 mM, selective for CYP11B1 122840 1.14.15.4 (R)-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile FAD286; FAD286, CYP11B2 inhibitor, inhibited CYP11B2 and CYP11B1 activities 14623 1.14.15.4 1-(1H-inden-2-yl)-1H-imidazole CYP11B2 IC50: 448 nM, no inhibition of CYP11B1, recombinant enzymes 62196 1.14.15.4 1-(3,4-dihydronaphthalen-2-yl)-1H-imidazole CYP11B1 IC50: 639 nM, CYP11B2 IC50: 334 nM, recombinant enzymes 36305 1.14.15.4 1-(3-bromobenzyl)-1H-imidazole - 40998 1.14.15.4 1-(3-chlorobenzyl)-1H-imidazole - 40997 1.14.15.4 1-(3-cyanobenzyl)-1H-imidazole - 40995 1.14.15.4 1-(3-fluorobenzyl)-1H-imidazole - 40996 1.14.15.4 1-(4-aminobenzyl)-1H-imidazole - 40994 1.14.15.4 1-(4-bromobenzyl)-1H-imidazole - 11729 1.14.15.4 1-(4-bromobenzyl)-5-phenyl-1H-imidazole - 41016 1.14.15.4 1-(4-chlorobenzyl)-1H-imidazole - 14037 1.14.15.4 1-(4-chlorobenzyl)-5-phenyl-1H-imidazole - 41015 1.14.15.4 1-(4-cyanobenzyl)-1H-imidazole - 40992 1.14.15.4 1-(4-cyanobenzyl)-5-(2-fluorophenyl)-1H-imidazole - 41025 1.14.15.4 1-(4-cyanobenzyl)-5-(2-methylphenyl)-1H-imidazole - 41026 1.14.15.4 1-(4-cyanobenzyl)-5-(3-fluorophenyl)-1H-imidazole - 41027 1.14.15.4 1-(4-cyanobenzyl)-5-(3-methylphenyl)-1H-imidazole - 41028 1.14.15.4 1-(4-cyanobenzyl)-5-(4-fluorophenyl)-1H-imidazole - 41029 1.14.15.4 1-(4-cyanobenzyl)-5-(4-methylphenyl)-1H-imidazole - 41030 1.14.15.4 1-(4-cyanobenzyl)-5-(4-pyridyl)-1H-imidazole - 41024 1.14.15.4 1-(4-cyanobenzyl)-5-(methyl carboxylate)-1H-imidazole - 41019 1.14.15.4 1-(4-cyanobenzyl)-5-(methylene-acetate)-1H-imidazole - 41018 1.14.15.4 1-(4-cyanobenzyl)-5-bromo-1H-imidazole - 41021 1.14.15.4 1-(4-cyanobenzyl)-5-formyl-1H-imidazole - 41022 1.14.15.4 1-(4-cyanobenzyl)-5-hydroxymethyl-1H-imidazole - 41023 1.14.15.4 1-(4-cyanobenzyl)-5-methyl-1H-imidazole - 41020 1.14.15.4 1-(4-cyanobenzyl)-5-phenyl-1H-imidazole - 41013 1.14.15.4 1-(4-fluorobenzyl)-1H-imidazole - 14738 1.14.15.4 1-(4-fluorobenzyl)-5-phenyl-1H-imidazole - 41014 1.14.15.4 1-(4-methoxybenzyl)-5-phenyl-1H-imidazole - 41017 1.14.15.4 1-(6-methoxy-3,4-dihydronaphthalen-2-yl)-1H-imidazole CYP11B1 IC50: 763 nM, CYP11B2 IC50: 411 nM, recombinant enzymes 36306 1.14.15.4 1-benzyl-5-phenyl-1H-imidazole - 18919 1.14.15.4 11beta-hydroxy-dehydroepiandrosterone 50% inhibition at 0.0033 mM 124967 1.14.15.4 11beta-hydroxy-progesterone 50% inhibition at 0.0004 mM 124966 1.14.15.4 11beta-hydroxy-testosterone 50% inhibition at 0.0017 mM 23292 1.14.15.4 18-ethynylprogesterone mechanism-based inhibition; weaker than 18-vinylprogesterone, inhibitor of aldosterone synthesis for both activities, stronger for 18-hydroxylation inhibition 16593 1.14.15.4 18-ethynylprogesterone mechanism-based inhibition; progesterone analog, time-dependent pseudo-first-order inactivation, concentration dependent 16593 1.14.15.4 18-ethynylprogesterone suicide-substrate of aldosterone biosythesis, inhibits more strongly the 18-hydroxylation step 16593 1.14.15.4 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 104363 1.14.15.4 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 16594 1.14.15.4 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 16594 1.14.15.4 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 16594 1.14.15.4 2,3-dichloro-N-(pyridin-3-yl)benzamide 51% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B22 162884 1.14.15.4 2,4,5-trifluoro-N-(pyridin-3-yl)benzamide 70% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B23 40991 1.14.15.4 2-(4-chlorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83184 1.14.15.4 2-(4-fluorobenzyl)-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 162886 1.14.15.4 2-benzyl-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83185 1.14.15.4 2-fluoro-N-(pyridin-3-yl)benzamide 34% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B19 162882 1.14.15.4 2-[(1R)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83189 1.14.15.4 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83190 1.14.15.4 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(3-methoxy-2-methylpropyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83193 1.14.15.4 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-(cyclopropylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83195 1.14.15.4 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 - 83192 1.14.15.4 2-[(1S)-1-(4-chlorophenyl)ethyl]-4-[(propan-2-yloxy)methyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83194 1.14.15.4 3,4-difluoro-N-(pyridin-3-yl)benzamide 83% inhibition of CYP11B2 at 0.5 mM, 6% inhibition of CYP11B20 40990 1.14.15.4 3,4-dimethoxy-N-(pyridin-3-yl)benzamide - 162883 1.14.15.4 3-(1-benzyl-1H-imidazol-5-yl)-1-propanol - 41007 1.14.15.4 3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine CYP11B1 IC50: 2117 nM, CYP11B2 IC50: 30 nM, recombinant enzymes 36300 1.14.15.4 3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine CYP11B1 IC50: 1268 nM, CYP11B2 IC50: 7 nM, recombinant enzymes 36299 1.14.15.4 3-(1H-imidazol-1-ylmethyl)aniline - 41000 1.14.15.4 3-(3,4-dihydronaphthalen-2-yl)pyridine CYP11B1 IC50: 1729 nM, CYP11B2 IC50: 7 nM, recombinant enzymes 36296 1.14.15.4 3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine CYP11B1 IC50: 503 nM, CYP11B2 IC50: 5 nM, recombinant enzymes 36301 1.14.15.4 3-(4-ethyl-3,4-dihydronaphthalen-2-yl)pyridine CYP11B1 IC50: 1615 nM, CYP11B2 IC50: 176 nM, recombinant enzymes 36303 1.14.15.4 3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine CYP11B1 IC50: 1291 nM, CYP11B2 IC50: 13 nM, recombinant enzymes 36302 1.14.15.4 3-(6-methoxy-1H-inden-2-yl)pyridine competitive, CYP11B1 IC50: 5684 nM, CYP11B2 IC50: 4 nM, recombinant enzymes 36297 1.14.15.4 3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine competitive, CYP11B1 IC50: 578 nM, CYP11B2 IC50: 2 nM, recombinant enzymes 36298 1.14.15.4 3-(7-methoxy-3,4-dihydronaphthalen-2-yl)pyridine CYP11B2 IC50: 45 nM, no inhibition of CYP11B1, recombinant enzymes 62195 1.14.15.4 3-chloro-N-(pyridin-3-yl)benzamide 26% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B18 162881 1.14.15.4 3-fluoro-N-(pyridin-3-yl)benzamide 47% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B17 162880 1.14.15.4 3-[(Z)-2,3-dihydro-1H-inden-1-ylidenemethyl]pyridine 50% inhibition at 0.087 mM 122832 1.14.15.4 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 36307 1.14.15.4 3-[1-(4-bromobenzyl)-1H-imidazol-5-yl]-1-propanol - 41011 1.14.15.4 3-[1-(4-chlorobenzyl)-1H-imidazol-5-yl]-1-propanol - 41010 1.14.15.4 3-[1-(4-cyanobenzyl)-1H-imidazol-5-yl]-1-propanol - 41008 1.14.15.4 3-[1-(4-fluorobenzyl)-1H-imidazol-5-yl]-1-propanol - 41009 1.14.15.4 3-[1-(4-methoxybenzyl)-1H-imidazol-5-yl]-1-propanol - 41012 1.14.15.4 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 - 83191 1.14.15.4 4-((5-phenyl-1H-imidazol-1-yl)methyl)benzonitrile - 41106 1.14.15.4 4-(2-methylpropyl)-2-(thiophen-2-ylmethyl)-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83188 1.14.15.4 4-(2-methylpropyl)-2-[4-(trifluoromethoxy)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83186 1.14.15.4 4-(2-methylpropyl)-2-[4-(trifluoromethyl)benzyl]-1,2-dihydroimidazo[5,1-d][1,2,5]thiadiazine 3,3-dioxide - 83187 1.14.15.4 4-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine CYP11B1 IC50: 2529 nM, CYP11B2 IC50: 2834 nM, recombinant enzymes 36304 1.14.15.4 4-(7-benzyl-6-oxo-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazin-5-yl)benzonitrile - 162885 1.14.15.4 4-bromo-N-(pyridin-3-yl)benzamide 64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B9 40987 1.14.15.4 4-chloro-N-(pyridin-3-yl)benzamide 88% inhibition of CYP11B2 at 0.5 mM, 5% inhibition of CYP11B8 40986 1.14.15.4 4-cyano-N-(pyridin-3-yl)benzamide 81% inhibition of CYP11B2 at 0.5 mM, 9% inhibition of CYP11B15 40988 1.14.15.4 4-fluoro-N-(pyridin-3-yl)benzamide 86% inhibition of CYP11B2 at 0.5 mM, 7% inhibition of CYP11B7 40985 1.14.15.4 4-methoxy-N-(pyridin-3-yl)benzamide 19% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B10 162875 1.14.15.4 4-methyl-N-(pyridin-3-yl)benzamide 25% inhibition of CYP11B2 at 0.5 mM, no% inhibition of CYP11B13 162878 1.14.15.4 4-nitro-N-(pyridin-3-yl)benzamide 64% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B16 40989 1.14.15.4 4-[(Z)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]pyridine 50% inhibition at 0.034 mM, selective for CYP11B1 122833 1.14.15.4 5-bromo-N-(pyridin-3-yl)pyridine-3-carboxamide 29% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B5 162873 1.14.15.4 5-[(1E)-1-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)ethyl]isoquinoline 50% inhibition at 0.096 mM 122837 1.14.15.4 5-[(E)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]isoquinoline 50% inhibition at 0.058 mM, selective for CYP11B1 122835 1.14.15.4 5-[(E)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]pyrimidine 50% inhibition at 0.027 mM, very selective for CYP11B1 122834 1.14.15.4 5-[(Z)-(5-fluoro-2,3-dihydro-1H-inden-1-ylidene)methyl]isoquinoline 50% inhibition at 0.026 mM, selective for CYP11B1 122836 1.14.15.4 5-[(Z)-2,3-dihydro-1H-inden-1-ylidenemethyl]-1H-imidazole 50% inhibition at 0.0061 mM 122839 1.14.15.4 5-[(Z)-3,4-dihydronaphthalen-1(2H)-ylidenemethyl]-1H-imidazole 50% inhibition at 0.0033 mM 122838 1.14.15.4 6,6-dimethyl-8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 162888 1.14.15.4 6-(5,8-dihydroisoquinolin-4-yl)-3,4-dihydroquinolin-2(1H)-one 94% inhibition of CYP11B2 at 0.5 mM, 91% inhibition of CYP11B1 40984 1.14.15.4 6-methoxydihydronaphthalene - 63003 1.14.15.4 8-(1H-imidazol-1-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41043 1.14.15.4 8-(2,3'-bipyridin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 162887 1.14.15.4 8-(5-ethoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41035 1.14.15.4 8-(5-fluoropyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41038 1.14.15.4 8-(5-hydroxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41037 1.14.15.4 8-(5-methoxypyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41033 1.14.15.4 8-(5-phenylpyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]-quinolin-4-one - 41044 1.14.15.4 8-(isoquinolin-4-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41040 1.14.15.4 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41031 1.14.15.4 8-(pyridin-3-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinoline-4-thione - 41057 1.14.15.4 8-(pyrimidin-5-yl)-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41042 1.14.15.4 8-[5-(2,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41048 1.14.15.4 8-[5-(2-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41045 1.14.15.4 8-[5-(2-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41051 1.14.15.4 8-[5-(3,4-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41049 1.14.15.4 8-[5-(3,5-difluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41050 1.14.15.4 8-[5-(3-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41046 1.14.15.4 8-[5-(3-hydroxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41054 1.14.15.4 8-[5-(3-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41052 1.14.15.4 8-[5-(4-fluorophenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41047 1.14.15.4 8-[5-(4-methoxyphenyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41053 1.14.15.4 8-[5-(propan-2-yloxy)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41036 1.14.15.4 8-[5-(trifluoromethyl)pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41039 1.14.15.4 8-[5-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41055 1.14.15.4 8-[5-[3-(trifluoromethyl)phenyl]pyridin-3-yl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one - 41056 1.14.15.4 9-(5-methoxypyridin-3-yl)-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one - 41034 1.14.15.4 9-(pyridin-3-yl)-1,2,6,7-tetrahydro-5H-pyrido[ 3,2,1-ij]quinolin-3-one - 41032 1.14.15.4 9-[6-(isoquinolin-4-yl)pyridin-3-yl]-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinolin-5-one - 41041 1.14.15.4 acetone 10%, v/v, complete inhibition of hydroxylation 333 1.14.15.4 Anti-11beta-hydroxylase IgG polyclonal, raised in rabbits, inhibition of 11-beta/18-hydroxylation and aldosterone synthesis of corticosterone 46649 1.14.15.4 Anti-11beta-hydroxylase IgG cross-reaction with 51 kDa protein 46649 1.14.15.4 antiserum produced by rabbits 31371 1.14.15.4 ascorbate without NADH, inhibition of aldosterone synthetase 94 1.14.15.4 atenolol potent inhibition of CYP11B2, recombinant enzyme 62194 1.14.15.4 clotrimazole azole derivative, antimycotic drug, strong dose-dependent inhibition 1496 1.14.15.4 CO - 176 1.14.15.4 CO affects 11beta-/19-hydroxylase reaction 176 1.14.15.4 CO strongly 176 1.14.15.4 corticosterone competitive inhibition of 11beta-hydroxylase activity 1103 1.14.15.4 Cu2+ - 19 1.14.15.4 deoxycorticosterone competitive substrate inhibition 1753 1.14.15.4 diphosphatidyl glycerol cardiolipin, dipalmitoyl phasphatidylcholine vesicles, 50% inhibition with 4-5 mol%, complete inhibition at 15 mol% 48292 1.14.15.4 EDTA 10 mM 21 1.14.15.4 erythromycin potent inhibition of CYP11B2, recombinant enzyme 5148 1.14.15.4 ethanol 10%, v/v, complete inhibition of hydroxylation 69 1.14.15.4 FAD286 inhibitor of 11-beta-hydroxylase CYP11B1 163009 1.14.15.4 fadrozole 50% inhibition at 0.001 mM 6216 1.14.15.4 fadrozole 50% inhibition at 0.010 mM 6216 1.14.15.4 fadrozole CYP11B2 IC50: 1 nM, CYP11B1 IC50: 10 nM, recombinant enzymes 6216 1.14.15.4 fadrozole in vitro and in vivo inhibition 6216 1.14.15.4 fadrozole inhibitor of CYP11B2 6216 1.14.15.4 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 6216 1.14.15.4 HgCl2 0.2 mM, 50% inhibition 110 1.14.15.4 iron-sulfur protein adrenodoxin, at high concentrations, 25% inhibition 106336 1.14.15.4 KCl total inactivation 79 1.14.15.4 KCN slight inhibitor 161 1.14.15.4 ketoconazole azole derivative, antimycotic drug, strong dose-dependent inhibition 483 1.14.15.4 ketoconazole - 483 1.14.15.4 ketoconazole 50% inhibition at 0.081 mM 483 1.14.15.4 ketoconazole CYP11B2 IC50: 81 nM, CYP11B1 IC50: 224 nM, recombinant enzymes 483 1.14.15.4 ketoprofene potent inhibition of CYP11B2, recombinant enzyme 135254 1.14.15.4 methanol 10%, v/v, complete inhibition of hydroxylation 83 1.14.15.4 methyl 3-(1-benzyl-1H-imidazol-5-yl)-propanoate - 41001 1.14.15.4 methyl 3-[1-(4-bromobenzyl)-1H-imidazol-5-yl]-propanoate - 41005 1.14.15.4 methyl 3-[1-(4-chlorobenzyl)-1H-imidazol-5-yl]-propanoate - 41004 1.14.15.4 methyl 3-[1-(4-cyanobenzyl)-1H-imidazol-5-yl]-propanoate - 41002 1.14.15.4 methyl 3-[1-(4-fluorobenzyl)-1H-imidazol-5-yl]-propanoate - 41003 1.14.15.4 methyl 3-[1-(4-methoxybenzyl)-1H-imidazol-5-yl]-propanoate - 41006 1.14.15.4 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 49207 1.14.15.4 metyrapol 11beta-hydroxylase inhibition, 40.8% by racemate, 38.1% by (+)-enantiomer and 33.8% by (-)-enantiomer, each 0.4 mM 21634 1.14.15.4 Metyrapone 2 mM 990 1.14.15.4 Metyrapone competitive substrate inhibition 990 1.14.15.4 Metyrapone competitive with substrate, affects strongly 11beta-/18-hydroxylation and 11beta-/19-hydroxylation 990 1.14.15.4 Metyrapone - 990 1.14.15.4 Metyrapone inhibition of the purified 11beta-hydroxylase, 18-hydroxylation and aldosterone synthesis of corticosterone are inhibited 990 1.14.15.4 Metyrapone 11beta-hydroxylase, 39.7% inhibition by 0.4 mM 990 1.14.15.4 Metyrapone diagnostic inhibitor, strong inhibition, 0.02 mM complete inhibition 990 1.14.15.4 Metyrapone 79% inhibition of CYP11B2 at 0.5 mM, 94% inhibition of CYP11B2 990 1.14.15.4 Mg2+ - 6 1.14.15.4 miconazole azole derivative, antimycotic drug, strong dose-dependent inhibition 1206 1.14.15.4 Mn2+ - 11 1.14.15.4 additional information conversion of labelled steroid to labelled aldosterone is inhibited by the addition of an excess of the same unlabelled steroid 2 1.14.15.4 additional information no inhibition with Harman, tetrahydronorharman and tetrahydroharman 2 1.14.15.4 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 2 1.14.15.4 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 2 1.14.15.4 additional information effects of enzyme inhibition of steroid biosynthesis and mineralcorticoid formation, overview 2 1.14.15.4 additional information dexamethasone represses the enzyme in nervous system tissues, overview 2 1.14.15.4 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 2 1.14.15.4 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 2 1.14.15.4 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 2 1.14.15.4 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 2 1.14.15.4 additional information structure homology modelling for inhibitor design, overview 2 1.14.15.4 additional information estradiol has no effect on aldosterone production by wild-type CYP11B1 and chimeric mutant CYP11B1/B2 in HEK-293 cells 2 1.14.15.4 N-(pyridin-3-yl)-4-(trifluoromethoxy)benzamide - 162876 1.14.15.4 N-(pyridin-3-yl)-4-(trifluoromethyl)benzamide - 162877 1.14.15.4 N-(pyridin-3-yl)benzamide 30% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B6 162874 1.14.15.4 N-(pyridin-3-yl)biphenyl-4-carboxamide - 162879 1.14.15.4 N-(pyridin-3-yl)pyridine-3-carboxamide 8% inhibition of CYP11B2 at 0.5 mM, no inhibition of CYP11B3 162871 1.14.15.4 N-(pyridin-3-yl)pyridine-4-carboxamide 39% inhibition of CYP11B2 at 0.5 mM, 4% inhibition of CYP11B4 162872 1.14.15.4 norharman beta-carboline, high affinity type II ligand to both cytochromes, progesterone binding to CYP17 competitively inhibited 2303 1.14.15.4 p-chloromercuribenzoate 1 mM 43 1.14.15.4 PCMB 0.1 mM, 50% inhibition 78 1.14.15.4 phenazine methosulfate 1 mM, crude extract 287 1.14.15.4 phosphate - 16 1.14.15.4 phosphatidylcholine unsaturated increasing dioleoyl/diphytanoyl phosphatidylcholine 215 1.14.15.4 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 286 1.14.15.4 R-fadrozole - 41104 1.14.15.4 S-fadrozole - 41105 1.14.15.4 SKF 525A little inhibition of the purified 11beta-hydroxylase, 18-hydroxylation and aldosterone synthesis of corticosterone are inhibited 9271 1.14.15.4 sodium cholate 0.2% effect nearly 20% inhibition 1209 1.14.15.4 spironolactone diuretic and antihypertensive drug, competitive aldosterone antagonist, slight inhibition 13224 1.14.15.4 Stilbestrol - 10783 1.14.15.4 sulfhydryl reagents strongly 978 1.14.15.4 testosterone potent inhibition of CYP11B2, recombinant enzyme 284 1.14.15.4 Zn2+ - 14 1.14.15.4 [3-(1H-imidazol-1-ylmethyl)phenyl]methanol - 40999 1.14.15.4 [4-(1H-imidazol-1-ylmethyl)phenyl]methanol - 40993