Target Information
Target General Infomation | |||||
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Target ID |
T16117
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Former ID |
TTDC00063
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Target Name |
Nitric-oxide synthase, brain
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Gene Name |
NOS1
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Synonyms |
BNOS; Constitutive NOS; N-NOS; NC-NOS; NNOS; NOS, type I; Neuronal NOS; NOS1
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Target Type |
Clinical Trial
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Disease | Headache [ICD9: 339, 784.0; ICD10: G43-G44, R51] | ||||
Function |
Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In the brain and peripheral nervous system, NO displays many properties of a neurotransmitter. Probably has nitrosylase activity and mediates cysteine S-nitrosylation of cytoplasmic target proteins such SRR.
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BioChemical Class |
Oxidoreductases acting on paired donors
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Target Validation |
T16117
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UniProt ID | |||||
EC Number |
EC 1.14.13.39
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Sequence |
MEDHMFGVQQIQPNVISVRLFKRKVGGLGFLVKERVSKPPVIISDLIRGGAAEQSGLIQA
GDIILAVNGRPLVDLSYDSALEVLRGIASETHVVLILRGPEGFTTHLETTFTGDGTPKTI RVTQPLGPPTKAVDLSHQPPAGKEQPLAVDGASGPGNGPQHAYDDGQEAGSLPHANGLAP RPPGQDPAKKATRVSLQGRGENNELLKEIEPVLSLLTSGSRGVKGGAPAKAEMKDMGIQV DRDLDGKSHKPLPLGVENDRVFNDLWGKGNVPVVLNNPYSEKEQPPTSGKQSPTKNGSPS KCPRFLKVKNWETEVVLTDTLHLKSTLETGCTEYICMGSIMHPSQHARRPEDVRTKGQLF PLAKEFIDQYYSSIKRFGSKAHMERLEEVNKEIDTTSTYQLKDTELIYGAKHAWRNASRC VGRIQWSKLQVFDARDCTTAHGMFNYICNHVKYATNKGNLRSAITIFPQRTDGKHDFRVW NSQLIRYAGYKQPDGSTLGDPANVQFTEICIQQGWKPPRGRFDVLPLLLQANGNDPELFQ IPPELVLEVPIRHPKFEWFKDLGLKWYGLPAVSNMLLEIGGLEFSACPFSGWYMGTEIGV RDYCDNSRYNILEEVAKKMNLDMRKTSSLWKDQALVEINIAVLYSFQSDKVTIVDHHSAT ESFIKHMENEYRCRGGCPADWVWIVPPMSGSITPVFHQEMLNYRLTPSFEYQPDPWNTHV WKGTNGTPTKRRAIGFKKLAEAVKFSAKLMGQAMAKRVKATILYATETGKSQAYAKTLCE IFKHAFDAKVMSMEEYDIVHLEHETLVLVVTSTFGNGDPPENGEKFGCALMEMRHPNSVQ EERKSYKVRFNSVSSYSDSQKSSGDGPDLRDNFESAGPLANVRFSVFGLGSRAYPHFCAF GHAVDTLLEELGGERILKMREGDELCGQEEAFRTWAKKVFKAACDVFCVGDDVNIEKANN SLISNDRSWKRNKFRLTFVAEAPELTQGLSNVHKKRVSAARLLSRQNLQSPKSSRSTIFV RLHTNGSQELQYQPGDHLGVFPGNHEDLVNALIERLEDAPPVNQMVKVELLEERNTALGV ISNWTDELRLPPCTIFQAFKYYLDITTPPTPLQLQQFASLATSEKEKQRLLVLSKGLQEY EEWKWGKNPTIVEVLEEFPSIQMPATLLLTQLSLLQPRYYSISSSPDMYPDEVHLTVAIV SYRTRDGEGPIHHGVCSSWLNRIQADELVPCFVRGAPSFHLPRNPQVPCILVGPGTGIAP FRSFWQQRQFDIQHKGMNPCPMVLVFGCRQSKIDHIYREETLQAKNKGVFRELYTAYSRE PDKPKKYVQDILQEQLAESVYRALKEQGGHIYVCGDVTMAADVLKAIQRIMTQQGKLSAE DAGVFISRMRDDNRYHEDIFGVTLRTYEVTNRLRSESIAFIEESKKDTDEVFSS |
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Drugs and Mode of Action | |||||
Inhibitor | ((E)-7-But-2-enyl)-azepan-(2Z)-ylideneamine | Drug Info | [526140] | ||
(+/-)-2-Methyl-1-(1-phenylethyl)-1H-imidazole | Drug Info | [531201] | |||
(4S,5R)-4,5-Diethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
(4S,5R)-4,5-Dimethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
(4S,5S)-4,5-Diethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
(5-Imino-[1,4]thiazepan-3-yl)-methanol | Drug Info | [527266] | |||
(5S,6R)-[Octahydro-quinolin-(2E)-ylidene]amine | Drug Info | [527502] | |||
(5S,6S)-[Octahydro-quinolin-(2E)-ylidene]amine | Drug Info | [527502] | |||
(6r,1'r,2's)-5,6,7,8 Tetrahydrobiopterin | Drug Info | [551393] | |||
(R)-3-Propyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
(S)-2-Amino-5-(N-methyl-guanidino)-pentanoic acid | Drug Info | [534097] | |||
(S)-3-Propyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
(S)-6-Amino-2-(2-imino-ethylamino)-hexanoic acid | Drug Info | [527266] | |||
1-(2-amino-benzothiazol-5-yl)-2-ethyl-isothiourea | Drug Info | [528695] | |||
1-(2-amino-benzothiazol-6-yl)-2-ethyl-isothiourea | Drug Info | [528695] | |||
1-(Benzhydrylamino)ethaniminium bromide | Drug Info | [531201] | |||
1-Benzyl-2-methyl-1H-imidazole | Drug Info | [531201] | |||
1-[(3-Methoxybenzyl)amino]ethaniminium chloride | Drug Info | [531201] | |||
2'-Monophosphoadenosine 5'-Diphosphoribose | Drug Info | [551393] | |||
2-(2-Amino-ethyl)-7-imino-azepane | Drug Info | [526140] | |||
2-amino-4,6-dimethylpyridine | Drug Info | [530216] | |||
2-Amino-5-(N-nitro-guanidino)-pentanoic acid | Drug Info | [534097] | |||
2-aminopyridine | Drug Info | [530216] | |||
2-Methyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
3,4-Dihydro-1H-quinolin-(2E)-ylideneamine | Drug Info | [527502] | |||
3,4-Dimethyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
3-(2-Amino-ethyl)-5-imino-[1,4]oxazepane | Drug Info | [526140] | |||
3-(2-Nitro-ethyl)-[1,4]oxazepan-(5Z)-ylideneamine | Drug Info | [526140] | |||
3-Bromo-1H-indazole-7-carbonitrile | Drug Info | [529494] | |||
3-bromo-7-nitro-1H-indazole | Drug Info | [530315] | |||
3-Bromo-7-Nitroindazole | Drug Info | [551393] | |||
3-Butyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
3-Ethyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
3-Isobutyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
3-Methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
3-Methyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
3-Propyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
4,5,6,7-tetrafluoro-3-methyl-1H-indazole | Drug Info | [530315] | |||
4,5-Dimethyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-bromo-1H-indazole | Drug Info | [528763] | |||
4-Butyl-thiazolidin-(2E)-ylideneamine | Drug Info | [527210] | |||
4-chloro-1H-indazole | Drug Info | [528763] | |||
4-Ethyl-3-methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-Ethyl-5-methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-Ethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
4-Ethyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-iodo-1H-indazole | Drug Info | [528763] | |||
4-Isopropyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-Methyl-5-propyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-methyl-6-propylpyridin-2-amine | Drug Info | [529745] | |||
4-Methyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
4-Methyl-piperidin-(2E)-ylideneamine | Drug Info | [527502] | |||
4-Methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
4-methylpyridin-2-amine | Drug Info | [529745] | |||
4-[(2-Methyl-1H-imidazol-1-yl)methyl]pyridine | Drug Info | [531201] | |||
5-bromo-1H-indazole | Drug Info | [528763] | |||
5-Bromomethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
5-chloro-1H-indazole | Drug Info | [528763] | |||
5-Ethyl-3-methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
5-Ethyl-4-methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
5-Ethyl-4-propyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
5-Ethyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
5-iodo-1H-indazole | Drug Info | [528763] | |||
5-Methyl-oxazolidin-(2Z)-ylideneamine | Drug Info | [526912] | |||
5-Methyl-pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
5-N-Allyl-Arginine | Drug Info | [551393] | |||
6-(2-Fluoropropyl)-4-methylpyridin-2-amine | Drug Info | [530039] | |||
6-(3-Fluoropropyl)-4-methylpyridin-2-amine | Drug Info | [530039] | |||
6-bromo-1H-indazole | Drug Info | [528763] | |||
6-chloro-1H-indazole | Drug Info | [528763] | |||
6-isobutyl-4-methylpyridin-2-amine | Drug Info | [530039] | |||
7-(2-Nitro-ethyl)-azepan-(2Z)-ylideneamine | Drug Info | [526140] | |||
7-bromo-1H-indazole | Drug Info | [528763] | |||
7-Butyl-azepan-(2Z)-ylideneamine | Drug Info | [526140] | |||
7-chloro-1H-indazole | Drug Info | [528763] | |||
7-Methoxy-1H-indazole | Drug Info | [526052] | |||
7-Methyl-[1,4]thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
7-nitro-1H-indazole | Drug Info | [530315] | |||
Acetate Ion | Drug Info | [551393] | |||
Alpha-D-Mannose | Drug Info | [551393] | |||
AR-C102222 | Drug Info | [529745] | |||
AR-C133057XX | Drug Info | [529745] | |||
Azepan-(2Z)-ylideneamine | Drug Info | [526140] | |||
Azocan-(2Z)-ylideneamine | Drug Info | [526140] | |||
Azonan-(2Z)-ylideneamine | Drug Info | [534097] | |||
EUSYNSTYELAMIDE B | Drug Info | [530193] | |||
Eusynstyelamide C | Drug Info | [530193] | |||
Flavin-Adenine Dinucleotide | Drug Info | [551393] | |||
Formic Acid | Drug Info | [551393] | |||
Heme | Drug Info | [551374] | |||
Hexahydro-cyclopenta[b]pyrrol-(2Z)-ylideneamine | Drug Info | [527210] | |||
Hexahydro-cyclopenta[c]pyrrol-(1Z)-ylideneamine | Drug Info | [527210] | |||
Hexahydro-pyrrolizin-(3E)-ylideneamine | Drug Info | [527210] | |||
L-NIL | Drug Info | [529159] | |||
L-NIO | Drug Info | [529811] | |||
L-Nw-nitroarginine | Drug Info | [531224] | |||
N*1*-(5-Methyl-2-nitro-phenyl)-butane-1,4-diamine | Drug Info | [534663] | |||
N-(3-(aminomethyl)-benzyl)acetamidine | Drug Info | [531201] | |||
N-(3-(Aminomethyl)Benzyl)Acetamidine | Drug Info | [551374] | |||
N-(5-Amino-6-oxo-heptyl)-acetamidine | Drug Info | [527210] | |||
N-Butyl-N'-Hydroxyguanidine | Drug Info | [551393] | |||
N-Isopropyl-N'-Hydroxyguanidine | Drug Info | [551393] | |||
N-omega-allyl-L-arginine | Drug Info | [529811] | |||
N-Omega-Hydroxy-L-Arginine | Drug Info | [551393] | |||
N-omega-propargyl-L-arginine | Drug Info | [529811] | |||
N-Omega-Propyl-L-Arginine | Drug Info | [551393] | |||
N5-(1-Imino-3-Butenyl)-L-Ornithine | Drug Info | [551393] | |||
N5-(1-iminobut-3-enyl)-L-ornithine | Drug Info | [529811] | |||
N5-(1-iminobutyl)-L-ornithine | Drug Info | [529811] | |||
N5-(1-iminopent-3-enyl)-L-ornithine | Drug Info | [529811] | |||
N5-(1-iminopropyl)-L-ornithine | Drug Info | [529811] | |||
Nitroarginine | Drug Info | [551396] | |||
NXN-462 | Drug Info | [524159] | |||
Octahydro-isoindol-(1Z)-ylideneamine | Drug Info | [527210] | |||
Piperidin-(2E)-ylideneamine | Drug Info | [527502] | |||
Pyrrolidin-(2Z)-ylideneamine | Drug Info | [527210] | |||
S-Ethyl-N-Phenyl-Isothiourea | Drug Info | [551374] | |||
S-Ethyl-N-[4-(Trifluoromethyl)Phenyl]Isothiourea | Drug Info | [551374] | |||
Tetrahydro-pyrimidin-2-ylideneamine | Drug Info | [534097] | |||
Thiazolidin-(2E)-ylideneamine | Drug Info | [527210] | |||
THIOCITRULLINE | Drug Info | [527563] | |||
[1,3]Oxazinan-(2E)-ylideneamine | Drug Info | [534097] | |||
[1,3]Thiazinan-(2E)-ylideneamine | Drug Info | [534097] | |||
[1,4]Oxazepan-(3E)-ylideneamine | Drug Info | [527266] | |||
[1,4]Oxazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
[1,4]Thiazepan-(3E)-ylideneamine | Drug Info | [527266] | |||
[1,4]Thiazepan-(5E)-ylideneamine | Drug Info | [527266] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
BioCyc Pathway | Citrulline-nitric oxide cycle | ||||
KEGG Pathway | Arginine and proline metabolism | ||||
Metabolic pathways | |||||
Calcium signaling pathway | |||||
Phagosome | |||||
Circadian entrainment | |||||
Long-term depression | |||||
Salivary secretion | |||||
Alzheimer' | |||||
s disease | |||||
Amyotrophic lateral sclerosis (ALS) | |||||
NetPath Pathway | EGFR1 Signaling Pathway | ||||
PANTHER Pathway | CCKR signaling map ST | ||||
PathWhiz Pathway | Arginine and Proline Metabolism | ||||
Reactome | ROS production in response to bacteria | ||||
Nitric oxide stimulates guanylate cyclase | |||||
WikiPathways | Monoamine Transport | ||||
Myometrial Relaxation and Contraction Pathways | |||||
Amyotrophic lateral sclerosis (ALS) | |||||
Quercetin and Nf-kB/ AP-1 Induced Cell Apoptosis | |||||
Spinal Cord Injury | |||||
Alzheimers Disease | |||||
Effects of Nitric Oxide | |||||
Serotonin Transporter Activity | |||||
References | |||||
Ref 524159 | ClinicalTrials.gov (NCT01748877) Efficacy, Tolerability, and Safety of NXN-462 in Patients With Post-Herpetic Neuralgia. U.S. National Institutes of Health. | ||||
Ref 526052 | Bioorg Med Chem Lett. 2001 May 7;11(9):1153-6.Inhibition of neuronal nitric oxide synthase by 7-methoxyindazole and related substituted indazoles. | ||||
Ref 526140 | Bioorg Med Chem Lett. 2001 Oct 8;11(19):2651-3.Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase. | ||||
Ref 526912 | Bioorg Med Chem Lett. 2004 Jan 19;14(2):313-6.4,5-Disubstituted-1,3-oxazolidin-2-imine derivatives: a new class of orally bioavailable nitric oxide synthase inhibitor. | ||||
Ref 527210 | Bioorg Med Chem Lett. 2004 Sep 6;14(17):4539-44.Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase. | ||||
Ref 527266 | Bioorg Med Chem Lett. 2004 Dec 6;14(23):5907-11.Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases. | ||||
Ref 527502 | Bioorg Med Chem Lett. 2005 Apr 15;15(8):1997-2001.Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase. | ||||
Ref 527563 | Bioorg Med Chem Lett. 2005 Jun 2;15(11):2881-5. Epub 2005 Apr 25.Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes. | ||||
Ref 528695 | Bioorg Med Chem Lett. 2007 May 1;17(9):2540-4. Epub 2007 Feb 8.Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors. | ||||
Ref 528763 | Bioorg Med Chem Lett. 2007 Jun 1;17(11):3177-80. Epub 2007 Mar 14.4-substituted indazoles as new inhibitors of neuronal nitric oxide synthase. | ||||
Ref 529159 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):336-43. Epub 2007 Oct 25.Discovery of a series of aminopiperidines as novel iNOS inhibitors. | ||||
Ref 529494 | Bioorg Med Chem. 2008 Jun 1;16(11):5962-73. Epub 2008 Apr 26.Inhibitory effects of a series of 7-substituted-indazoles toward nitric oxide synthases: particular potency of 1H-indazole-7-carbonitrile. | ||||
Ref 529745 | Nat Chem Biol. 2008 Nov;4(11):700-7. Epub 2008 Oct 12.Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase. | ||||
Ref 529811 | Bioorg Med Chem. 2008 Dec 15;16(24):10205-9. Epub 2008 Oct 29.Structure-activity relationship of novel and known inhibitors of human dimethylarginine dimethylaminohydrolase-1: alkenyl-amidines as new leads. | ||||
Ref 530039 | J Med Chem. 2009 Apr 23;52(8):2443-53.Design and synthesis of 2-amino-4-methylpyridine analogues as inhibitors for inducible nitric oxide synthase and in vivo evaluation of [18F]6-(2-fluoropropyl)-4-methyl-pyridin-2-amine as a potential PET tracer for inducible nitric oxide synthase. | ||||
Ref 530193 | J Nat Prod. 2009 Jun;72(6):1115-20.Eusynstyelamides A, B, and C, nNOS inhibitors, from the ascidian Eusynstyela latericius. | ||||
Ref 530216 | J Med Chem. 2009 Jul 23;52(14):4533-7.L337H mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors. | ||||
Ref 530315 | Bioorg Med Chem. 2009 Sep 1;17(17):6180-7. Epub 2009 Aug 6.Fluorinated indazoles as novel selective inhibitors of nitric oxide synthase (NOS): synthesis and biological evaluation. | ||||
Ref 531201 | Bioorg Med Chem Lett. 2010 Nov 15;20(22):6495-9. Epub 2010 Sep 17.N-Substituted acetamidines and 2-methylimidazole derivatives as selective inhibitors of neuronal nitric oxide synthase. | ||||
Ref 531224 | J Med Chem. 2010 Nov 11;53(21):7804-24.Exploration of the active site of neuronal nitric oxide synthase by the design and synthesis of pyrrolidinomethyl 2-aminopyridine derivatives. | ||||
Ref 534097 | J Med Chem. 1996 Feb 2;39(3):669-72.2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms. | ||||
Ref 534663 | J Med Chem. 1998 Jul 2;41(14):2636-42.Nitroaromatic amino acids as inhibitors of neuronal nitric oxide synthase. |
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