Therapeutic Targets Database
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TTD Target ID: TTDS00420

Target Information
NameCytochrome P450 11B1, mitochondrial    
Type of targetSuccessful target    
SynonymsCYP11B1    
CYPXIB1    
P-450c11    
P450C11    
S11BH    
Steroid 11-beta-hydroxylase    
DiseaseAdrenocortical tumour
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[1]
Cushing's syndrome
[ICD9: 255.0   ICD10: E24]
[1]
Drug(s)MetyraponeApprovedCushing's syndrome (hypercortisolism)[2]
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.14.15.4
PathwayAndrogen and estrogen metabolism
C21-Steroid hormone metabolism
Metabolic pathways
UniProt IDP15538
SequenceMALRAKAEVCMAVPWLSLQRAQALGTRAARVPRTVLPFEAMPRRPGNRWLRLLQIWREQG YEDLHLEVHQTFQELGPIFRYDLGGAGMVCVMLPEDVEKLQQVDSLHPHRMSLEPWVAYR QHRGHKCGVFLLNGPEWRFNRLRLNPEVLSPNAVQRFLPMVDAVARDFSQALKKKVLQNA RGSLTLDVQPSIFHYTIEASNLALFGERLGLVGHSPSSASLNFLHALEVMFKSTVQLMFM PRSLSRWTSPKVWKEHFEAWDCIFQYGDNCIQKIYQELAFSRPQQYTSIVAELLLNAELS PDAIKANSMELTAGSVDTTVFPLLMTLFELARNPNVQQALRQESLAAAASISEHPQKATT ELPLLRAALKETLRLYPVGLFLERVASSDLVLQNYHIPAGTLVRVFLYSLGRNPALFPRP ERYNPQRWLDIRGSGRNFYHVPFGFGMRQCLGRRLAEAEMLLLLHHVLKHLQVETLTQED IKMVYSFILRPSMFPLLTFRAIN
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3-[3]
(4-[3]
1- (2-Phenoxy-ethyl)-1H-imidazole[4]
1- (3,4-dihydronaphthalen-2-yl)-1H-imidazole[5]
1- (3-Bromobenzyl)-1H-imidazole[3]
1- (3-Chlorobenzyl)-1H-imidazole[3]
1- (3-Fluorobenzyl)-1H-imidazole[3]
1- (3-Methoxy-naphthalen-2-yl)-1H-imidazole[6]
1- (4-Aminobenzyl)-1H-imidazole[3]
1- (4-Bromobenzyl)-1H-imidazole[3]
1- (4-Bromobenzyl)-5-phenyl-1H-imidazole[3]
1- (4-Chlorobenzyl)-5-phenyl-1H-imidazole[3]
1- (4-Cyanobenzyl)-1H-imidazole[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-[3]
1- (4-Cyanobenzyl)-5-bromo-1H-imidazole[3]
1- (4-Cyanobenzyl)-5-formyl-1H-imidazole[3]
1- (4-Cyanobenzyl)-5-hydroxymethyl-1H-imidazole[3]
1- (4-Cyanobenzyl)-5-methyl-1H-imidazole[3]
1- (4-Cyanobenzyl)-5-phenyl-1H-imidazole[3]
1- (4-Fluorobenzyl)-1H-imidazole[3]
1- (4-Fluorobenzyl)-5-phenyl-1H-imidazole[3]
1- (4-Methoxybenzyl)-5-phenyl-1H-imidazole[3]
1- (6-Methoxy-naphthalen-2-yl)-1H-imidazole[6]
1-Benzyl-5-phenyl-1H-imidazole[3]
1-Ethyl-3-imidazol-1-ylmethyl-1H-indole[7]
1-Naphthalen-2-yl-1H-imidazole[6]
1-Phenyl-2-pyridin-3-yl-propan-1-one[8]
2-Methyl-1,2-di-pyridin-3-yl-1-methoxypropane[8]
2-Methyl-1,2-di-pyridin-3-yl-propan-1-one oxime[8]
2-Methyl-1,2-di-pyridin-3-yl-propane[8]
2-Methyl-1,2-di-pyridin-3-yl-propylchloride[8]
2-Methyl-1,2-di-pyridin-3-yl-propyliodide[8]
2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-ol[8]
2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-one[8]
3- ([3]
3- (1,1-Dimethyl-2-phenyl-ethyl)-pyridine[8]
3- (1,2-dihydroacenaphthylen-3-yl)pyridine[9]
3- (1,2-dihydroacenaphthylen-5-yl)pyridine[9]
3- (1-Benzyl-1H-imidazol-5-yl)-1-propanol[3]
3- (1-Chloro-7-methoxy-naphthalen-2-yl)-pyridine[6]
3- (1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine[5]
3- (1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine[5]
3- (1H-inden-2-yl)pyridine[5]
3- (2,3-Dihydro-1,4-benzodioxin-6-yl)pyridine[10]
3- (2-Chloro-1,1-dimethyl-2-phenyl-ethyl)-pyridine[8]
3- (3,4-dihydronaphthalen-2-yl)pyridine[5]
3- (3-Benzyl-6-methoxynaphthalen-2-yl)pyridine[11]
3- (3-Benzylnaphthalen-2-yl)pyridine[11]
3- (3-methyl-3,4-dihydronaphthalen-2-yl)pyridine[5]
3- (4-ethyl-3,4-dihydronaphthalen-2-yl)pyridine[5]
3- (4-methyl-3,4-dihydronaphthalen-2-yl)pyridine[5]
3- (5,6,7,8-Tetrahydronaphthalen-2-yl)pyridine[10]
3- (5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine[6]
3- (5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine[6]
3- (5-methoxy-1H-inden-2-yl)pyridine[5]
3- (6-Bromo-naphthalen-2-yl)-pyridine[6]
3- (6-Ethoxy-naphthalen-2-yl)-pyridine[6]
3- (6-Methoxy-3-methylnaphthalen-2-yl)pyridine[12]
3- (6-Methoxynaphthalen-2-yl)-4-methylpyridine[12]
3- (6-Methoxynaphthalen-2-yl)-5-phenylpyridine[12]
3- (6-Methoxynaphthalen-2-yl)pyridin-4-amine[12]
3- (6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine[12]
3- (6-methoxynaphthalen-2-yl)pyridine[11]
3- (naphthalen-2-yl)pyridine[11]
3-Ethoxy-5- (6-methoxynaphthalen-2-yl)pyridine[12]
3-Fluoro-4'- (pyridin-4-ylmethyl)biphenyl-4-ol[13]
3-Imidazol-1-yl-quinoline[6]
3-Imidazol-1-ylmethyl-1H-indole[7]
3-Imidazol-1-ylmethyl-2-isopropyl-1H-indole[7]
3-Indan- (1E)-ylidenemethyl-pyridine[14]
3-Indan- (1Z)-ylidenemethyl-pyridine[14]
3-MeSO2-DDE[2]
3-Phenanthren-9-yl-pyridine[6]
3-[ (Z)-2-phenylvinyl]pyridine[5]
3-[1- (4-Bromobenzyl)-1H-imidazol-5-yl]-1-propanol[3]
3-[1- (4-Cyanobenzyl)-1H-imidazol-5-yl]-1-propanol[3]
3-[3- (4-Methoxybenzyl)naphthalen-2-yl]pyridine[11]
3-[4-Chloro-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[4-Chloro-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[4-Fluoro-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[4-Methyl-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Bromo-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Bromo-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[5-Chloro-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Chloro-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[5-Ethoxy-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Ethoxy-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[5-Fluoro-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Fluoro-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[5-Methoxy-indan- (1E)-ylidenemethyl]-pyridine[14]
3-[5-Methoxy-indan- (1Z)-ylidenemethyl]-pyridine[14]
3-[7-Methoxy-indan- (1E)-ylidenemethyl]-pyridine[14]
3-methoxy-5- (6-methoxynaphthalen-2-yl)pyridine[12]
4'- (Pyridin-4-ylmethyl)biphenyl-3,4-diamine[13]
4'- (Pyridin-4-ylmethyl)biphenyl-3,4-diol[13]
4'- (Pyridin-4-ylmethyl)biphenyl-3-amine[13]
4'- (Pyridin-4-ylmethyl)biphenyl-4-amine[13]
4- ([13]
4- (2-Imidazol-1-yl-ethoxy)-benzamide[4]
4- (4'-Fluoro-biphenyl-4-ylmethyl)pyridine[13]
4- (4-[13]
4- (4-[13]
4- (6-Methoxy-3-methylnaphthalen-2-yl)isoquinoline[12]
4- (6-Methoxynaphthalen-2-yl)isoquinoline[12]
4- (6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine[5]
4-Indan- (1Z)-ylidenemethyl-pyridine[14]
4-[ (3'-Hydroxybiphenyl-4-yl)methyl]pyridine[13]
4-[ (4'-Hydroxybiphenyl-4-yl)methyl]pyridine[13]
4-[5-Bromo-indan- (1E)-ylidenemethyl]-pyridine[14]
4-[5-Bromo-indan- (1Z)-ylidenemethyl]-pyridine[14]
4-[5-Chloro-indan- (1E)-ylidenemethyl]-pyridine[14]
4-[5-Chloro-indan- (1Z)-ylidenemethyl]-pyridine[14]
4-[5-Fluoro-indan- (1E)-ylidenemethyl]-pyridine[14]
4-[5-Fluoro-indan- (1Z)-ylidenemethyl]-pyridine[14]
5- (6-Methoxynaphthalen-2-yl)pyridin-3-ol[12]
5-Indan- (1E)-ylidenemethyl-1H-imidazole[15]
5-Indan- (1Z)-ylidenemethyl-1H-imidazole[15]
5-Naphthalen-2-yl-1H-imidazole[6]
5-Naphthalen-2-yl-oxazole[6]
5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one[10]
5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one[10]
5-[4- (Pyridin-4-ylmethyl)phenyl]-1H-indole[13]
5-[5-Bromo-indan- (1E)-ylidenemethyl]-1H-imidazole[15]
5-[5-Bromo-indan- (1Z)-ylidenemethyl]-1H-imidazole[15]
5-[5-Fluoro-indan- (1E)-ylidenemethyl]-pyrimidine[14]
6- (4-Methylpyridin-3-yl)-2-naphthonitrile[12]
6- (pyridin-3-yl)-2-naphthonitrile[12]
6-Isoquinolin-4-yl-3,4-dihydroquinolin-2 (1H)-one[10]
6-Pyridin-3-yl-1,2,3,4-tetrahydronaphthalen-2-ol[10]
6-Pyridin-3-yl-3,4-dihydronaphthalen-2 (1H)-one[10]
6-Pyridin-3-yl-3,4-dihydroquinolin-2 (1H)-on[10]
6-Pyridin-3-yl-3,4-dihydroquinoline-2 (1H)-thione[10]
6-Pyridin-3-yl-naphthalen-2-ol[6]
6-[4- (Pyridin-4-ylmethyl)phenyl]naphthalen-2-ol[13]
7- (1-[16]
7-Pyridin-3-yl-2H-1,4-benzothiazin-3 (4H)-one[10]
ABIRATERONE[17]
BENZYLIMIDAZOLE[3]
FADROZOLE[3]
FADROZOLE[10]
FADROZOLE HCL[18]
METYRAPOL[8]
Methyl 3- (1-Benzyl-1H-imidazol-5-yl)-propanoate[3]
Metyrapone[2]
N- (4'-Isonicotinoylbiphenyl-3-yl)acetamide[13]
R-fadrozole[3]
SL125[19]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. To Reference
Ref 2Effects of 3-MeSO2-DDE and some CYP inhibitors on glucocorticoid steroidogenesis in the H295R human adrenocortical carcinoma cell line. Toxicol In Vitro. 2002 Apr;16(2):113-21. To Reference
Ref 3J Med Chem. 2010 Feb 25;53(4):1712-25.Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2). To Reference
Ref 4J Med Chem. 1985 Oct;28(10):1427-32.Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles. To Reference
Ref 5J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis. To Reference
Ref 6J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. To Reference
Ref 7J Med Chem. 1986 Mar;29(3):342-6.Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues. To Reference
Ref 8J Med Chem. 1984 Jan;27(1):15-9.Structure-activity relationship study of the inhibition of adrenal cortical 11 beta-hydroxylase by new metyrapone analogues. To Reference
Ref 9Bioorg Med Chem Lett. 2006 Jan 1;16(1):25-30. Epub 2005 Oct 21.Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2). To Reference
Ref 10J Med Chem. 2008 Dec 25;51(24):8077-87.In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives. To Reference
Ref 11J Med Chem. 2008 Oct 9;51(19):6138-49. Epub 2008 Sep 3.Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach. To Reference
Ref 12J Med Chem. 2008 Aug 28;51(16):5064-74. Epub 2008 Aug 1.Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity. To Reference
Ref 13J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer. To Reference
Ref 14J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. To Reference
Ref 15J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. To Reference
Ref 16Bioorg Med Chem. 2008 Aug 15;16(16):7715-27. Epub 2008 Jul 9.Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17alpha-hydroxylase-17,20-lyase (CYP17)--part II: Core rigidification and influence of substituents at the methylene bridge. To Reference
Ref 17J Med Chem. 2010 Jul 8;53(13):5049-53.Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors. To Reference
Ref 18J Med Chem. 1991 Feb;34(2):725-36.Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. To Reference
Ref 19A novel therapeutic strategy for the treatment of congestive heart failure, mycardial fibrosis and hyperalderonism. ElexoPharm GmbH. 2006 To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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