Target Information
Target General Infomation | |||||
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Target ID |
T84621
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Former ID |
TTDS00420
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Target Name |
Cytochrome P450 11B1, mitochondrial
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Gene Name |
CYP11B1
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Synonyms |
CYPXIB1; P-450c11; P450C11; S11BH; Steroid 11-beta-hydroxylase; CYP11B1
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Target Type |
Successful
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Disease | Breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
Cushing's disease [ICD9: 255; ICD10: E24.0] | |||||
Congestive heart failure; Myocardial fibrosis; Hyperaldosteronism [ICD9: 255.1, 425.0, 425.3, 428, 428.0, 709.2; ICD10: E26, I42.0, I42.5, I50, L90.5] | |||||
Function |
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochrome P450 XIB.
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BioChemical Class |
Oxidoreductases acting on paired donors
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Target Validation |
T84621
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UniProt ID | |||||
EC Number |
EC 1.14.15.4
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Sequence |
MALRAKAEVCMAVPWLSLQRAQALGTRAARVPRTVLPFEAMPRRPGNRWLRLLQIWREQG
YEDLHLEVHQTFQELGPIFRYDLGGAGMVCVMLPEDVEKLQQVDSLHPHRMSLEPWVAYR QHRGHKCGVFLLNGPEWRFNRLRLNPEVLSPNAVQRFLPMVDAVARDFSQALKKKVLQNA RGSLTLDVQPSIFHYTIEASNLALFGERLGLVGHSPSSASLNFLHALEVMFKSTVQLMFM PRSLSRWTSPKVWKEHFEAWDCIFQYGDNCIQKIYQELAFSRPQQYTSIVAELLLNAELS PDAIKANSMELTAGSVDTTVFPLLMTLFELARNPNVQQALRQESLAAAASISEHPQKATT ELPLLRAALKETLRLYPVGLFLERVASSDLVLQNYHIPAGTLVRVFLYSLGRNPALFPRP ERYNPQRWLDIRGSGRNFYHVPFGFGMRQCLGRRLAEAEMLLLLHHVLKHLQVETLTQED IKMVYSFILRPSMFPLLTFRAIN |
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Drugs and Mode of Action | |||||
Inhibitor | (3-((1H-imidazol-1-yl)methyl)phenyl)methanol | Drug Info | [530679] | ||
(4-((1H-imidazol-1-yl)methyl)phenyl)methanol | Drug Info | [530679] | |||
1-(2-Phenoxy-ethyl)-1H-imidazole | Drug Info | [533496] | |||
1-(3,4-dihydronaphthalen-2-yl)-1H-imidazole | Drug Info | [528109] | |||
1-(3-Bromobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(3-Chlorobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(3-Fluorobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole | Drug Info | [527801] | |||
1-(4-Aminobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Bromobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Bromobenzyl)-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Chlorobenzyl)-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(2-fluorophenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(2-methylphenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(3-fluorophenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(3-methylphenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(4-fluorophenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(4-methylphenyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-(4-pyridyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-bromo-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-formyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-hydroxymethyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Cyanobenzyl)-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-fluorobenzyl)-1H-imidazole | Drug Info | [530679] | |||
1-(4-Fluorobenzyl)-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-(4-Methoxybenzyl)-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-(6-Methoxy-naphthalen-2-yl)-1H-imidazole | Drug Info | [527801] | |||
1-Benzyl-5-phenyl-1H-imidazole | Drug Info | [530679] | |||
1-Ethyl-3-imidazol-1-ylmethyl-1H-indole | Drug Info | [533418] | |||
1-Naphthalen-2-yl-1H-imidazole | Drug Info | [527801] | |||
1-Phenyl-2-pyridin-3-yl-propan-1-one | Drug Info | [533562] | |||
2-Methyl-1,2-di-pyridin-3-yl-1-methoxypropane | Drug Info | [533562] | |||
2-Methyl-1,2-di-pyridin-3-yl-propan-1-one oxime | Drug Info | [533562] | |||
2-Methyl-1,2-di-pyridin-3-yl-propane | Drug Info | [533562] | |||
2-Methyl-1,2-di-pyridin-3-yl-propylchloride | Drug Info | [533562] | |||
2-Methyl-1,2-di-pyridin-3-yl-propyliodide | Drug Info | [533562] | |||
2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-ol | Drug Info | [533562] | |||
2-Methyl-1-phenyl-2-pyridin-3-yl-propan-1-one | Drug Info | [533562] | |||
3-((1H-imidazol-1-yl)methyl)aniline | Drug Info | [530679] | |||
3-(1,1-Dimethyl-2-phenyl-ethyl)-pyridine | Drug Info | [533562] | |||
3-(1,2-dihydroacenaphthylen-3-yl)pyridine | Drug Info | [527819] | |||
3-(1,2-dihydroacenaphthylen-5-yl)pyridine | Drug Info | [527819] | |||
3-(1-Benzyl-1H-imidazol-5-yl)-1-propanol | Drug Info | [530679] | |||
3-(1-Chloro-7-methoxy-naphthalen-2-yl)-pyridine | Drug Info | [527801] | |||
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | [528109] | |||
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | [528109] | |||
3-(1H-inden-2-yl)pyridine | Drug Info | [528109] | |||
3-(2,3-Dihydro-1,4-benzodioxin-6-yl)pyridine | Drug Info | [529834] | |||
3-(2-Chloro-1,1-dimethyl-2-phenyl-ethyl)-pyridine | Drug Info | [533562] | |||
3-(3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [528109] | |||
3-(3-Benzyl-6-methoxynaphthalen-2-yl)pyridine | Drug Info | [529667] | |||
3-(3-Benzylnaphthalen-2-yl)pyridine | Drug Info | [529667] | |||
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [528109] | |||
3-(4-ethyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [528109] | |||
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [528109] | |||
3-(5,6,7,8-Tetrahydronaphthalen-2-yl)pyridine | Drug Info | [529834] | |||
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | [527801] | |||
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | [527801] | |||
3-(5-methoxy-1H-inden-2-yl)pyridine | Drug Info | [528109] | |||
3-(6-Bromo-naphthalen-2-yl)-pyridine | Drug Info | [527801] | |||
3-(6-Ethoxy-naphthalen-2-yl)-pyridine | Drug Info | [527801] | |||
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [529624] | |||
3-(6-Methoxy-3-methylnaphthalen-2-yl)pyridine | Drug Info | [529624] | |||
3-(6-Methoxynaphthalen-2-yl)-4-methylpyridine | Drug Info | [529624] | |||
3-(6-Methoxynaphthalen-2-yl)-5-phenylpyridine | Drug Info | [529624] | |||
3-(6-Methoxynaphthalen-2-yl)pyridin-4-amine | Drug Info | [529624] | |||
3-(6-methoxynaphthalen-2-yl)pyridine | Drug Info | [529667] | |||
3-(naphthalen-2-yl)pyridine | Drug Info | [529667] | |||
3-Ethoxy-5-(6-methoxynaphthalen-2-yl)pyridine | Drug Info | [529624] | |||
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol | Drug Info | [531085] | |||
3-Imidazol-1-yl-quinoline | Drug Info | [527801] | |||
3-Imidazol-1-ylmethyl-1H-indole | Drug Info | [533418] | |||
3-Imidazol-1-ylmethyl-2-isopropyl-1H-indole | Drug Info | [533418] | |||
3-Indan-(1E)-ylidenemethyl-pyridine | Drug Info | [527456] | |||
3-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | [527456] | |||
3-MeSO2-DDE | Drug Info | [535383] | |||
3-methoxy-5-(6-methoxynaphthalen-2-yl)pyridine | Drug Info | [529624] | |||
3-Phenanthren-9-yl-pyridine | Drug Info | [527801] | |||
3-[(Z)-2-phenylvinyl]pyridine | Drug Info | [528109] | |||
3-[1-(4-Bromobenzyl)-1H-imidazol-5-yl]-1-propanol | Drug Info | [530679] | |||
3-[1-(4-Cyanobenzyl)-1H-imidazol-5-yl]-1-propanol | Drug Info | [530679] | |||
3-[3-(4-Methoxybenzyl)naphthalen-2-yl]pyridine | Drug Info | [529667] | |||
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diamine | Drug Info | [531085] | |||
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol | Drug Info | [531085] | |||
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine | Drug Info | [531085] | |||
4'-(Pyridin-4-ylmethyl)biphenyl-4-amine | Drug Info | [531085] | |||
4-((1H-imidazol-1-yl)methyl)benzonitrile | Drug Info | [530679] | |||
4-((3',4'-Difluorobiphenyl-4-yl)methyl)pyridine | Drug Info | [531085] | |||
4-(2-Imidazol-1-yl-ethoxy)-benzamide | Drug Info | [533496] | |||
4-(4'-Fluoro-biphenyl-4-ylmethyl)pyridine | Drug Info | [531085] | |||
4-(4-(thiophen-2-yl)benzyl)pyridine | Drug Info | [531085] | |||
4-(4-(thiophen-3-yl)benzyl)pyridine | Drug Info | [531085] | |||
4-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [528109] | |||
4-(6-Methoxy-3-methylnaphthalen-2-yl)isoquinoline | Drug Info | [529624] | |||
4-(6-Methoxynaphthalen-2-yl)isoquinoline | Drug Info | [529624] | |||
4-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | [527456] | |||
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | [531085] | |||
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | [531085] | |||
4-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [527456] | |||
5-(6-Methoxynaphthalen-2-yl)pyridin-3-ol | Drug Info | [529624] | |||
5-Indan-(1E)-ylidenemethyl-1H-imidazole | Drug Info | [527475] | |||
5-Indan-(1Z)-ylidenemethyl-1H-imidazole | Drug Info | [527475] | |||
5-Naphthalen-2-yl-1H-imidazole | Drug Info | [527801] | |||
5-Naphthalen-2-yl-oxazole | Drug Info | [527801] | |||
5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one | Drug Info | [529834] | |||
5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one | Drug Info | [529834] | |||
5-[4-(Pyridin-4-ylmethyl)phenyl]-1H-indole | Drug Info | [531085] | |||
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole | Drug Info | [527475] | |||
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole | Drug Info | [527475] | |||
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine | Drug Info | [527456] | |||
6-(4-Methylpyridin-3-yl)-2-naphthonitrile | Drug Info | [529624] | |||
6-(pyridin-3-yl)-2-naphthonitrile | Drug Info | [529624] | |||
6-Isoquinolin-4-yl-3,4-dihydroquinolin-2(1H)-one | Drug Info | [529834] | |||
6-Pyridin-3-yl-1,2,3,4-tetrahydronaphthalen-2-ol | Drug Info | [529834] | |||
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one | Drug Info | [529834] | |||
6-Pyridin-3-yl-3,4-dihydronaphthalen-2(1H)-one | Drug Info | [529834] | |||
6-Pyridin-3-yl-3,4-dihydroquinoline-2(1H)-thione | Drug Info | [529834] | |||
6-Pyridin-3-yl-naphthalen-2-ol | Drug Info | [527801] | |||
6-[4-(Pyridin-4-ylmethyl)phenyl]naphthalen-2-ol | Drug Info | [531085] | |||
7-(1-(1H-imidazol-1-yl)ethyl)-9H-fluoren-2-ol | Drug Info | [529625] | |||
7-Pyridin-3-yl-2H-1,4-benzothiazin-3(4H)-one | Drug Info | [529834] | |||
BENZYLIMIDAZOLE | Drug Info | [530679] | |||
FADROZOLE | Drug Info | [530679] | |||
Methyl 3-(1-Benzyl-1H-imidazol-5-yl)-propanoate | Drug Info | [530679] | |||
METYRAPOL | Drug Info | [533562] | |||
Metyrapone | Drug Info | [535383] | |||
N-(4'-Isonicotinoylbiphenyl-3-yl)acetamide | Drug Info | [531085] | |||
R-fadrozole | Drug Info | [530679] | |||
SL125 | Drug Info | [551088] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
BioCyc Pathway | Superpathway of steroid hormone biosynthesis | ||||
Glucocorticoid biosynthesis | |||||
Mineralocorticoid biosynthesis | |||||
KEGG Pathway | Steroid hormone biosynthesis | ||||
Metabolic pathways | |||||
PathWhiz Pathway | Steroidogenesis | ||||
Reactome | Glucocorticoid biosynthesis | ||||
Endogenous sterols | |||||
WikiPathways | Metapathway biotransformation | ||||
Oxidation by Cytochrome P450 | |||||
Metabolism of steroid hormones and vitamin D | |||||
Corticotropin-releasing hormone | |||||
References | |||||
Ref 468277 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5224). | ||||
Ref 538462 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 012911. | ||||
Ref 543063 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8311). | ||||
Ref 527456 | J 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. | ||||
Ref 527475 | J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase. | ||||
Ref 527801 | J 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. | ||||
Ref 527819 | Bioorg 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). | ||||
Ref 528109 | J 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. | ||||
Ref 529624 | J 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 onpotency and selectivity. | ||||
Ref 529625 | Bioorg 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. | ||||
Ref 529667 | J 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. | ||||
Ref 529834 | J 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. | ||||
Ref 530679 | J 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). | ||||
Ref 531085 | J 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. | ||||
Ref 533418 | J 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. | ||||
Ref 533496 | J Med Chem. 1985 Oct;28(10):1427-32.Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles. | ||||
Ref 533562 | J 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. |
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