General Information of the Protein
Protein ID
PT01856
Protein Name
Nitric oxide synthase 3
Secondarily
Protein Name
Constitutive NOS
EC-NOS
NOS type III
Nitric oxide synthase
endothelial
Gene Name
NOS3
Sequence
MGNLKSVAQEPGPPCGLGLGLGLGLCGKQGPATPAPEPSRAPASLLPPAPEHSPPSSPLTQPPEGPKFPRVKNWEVGSITYDTLSAQAQQDGPCTPRRCLGSLVFPRKLQGRPSPGPPAPEQLLSQARDFINQYYSSIKRSGSQAHEQRLQEVEAEVAATGTYQLRESELVFGAKQAWRNAPRCVGRIQWGKLQVFDARDCRSAQEMFTYICNHIKYATNRGNLRSAITVFPQRCPGRGDFRIWNSQLVRYAGYRQQDGSVRGDPANVEITELCIQHGWTPGNGRFDVLPLLLQAPDDPPELFLLPPELVLEVPLEHPTLEWFAALGLRWYALPAVSNMLLEIGGLEFPAAPFSGWYMSTEIGTRNLCDPHRYNILEDVAVCMDLDTRTTSSLWKDKAAVEINVAVLHSYQLAKVTIVDHHAATASFMKHLENEQKARGGCPADWAWIVPPISGSLTPVFHQEMVNYFLSPAFRYQPDPWKGSAAKGTGITRKKTFKEVANAVKISASLMGTVMAKRVKATILYGSETGRAQSYAQQLGRLFRKAFDPRVLCMDEYDVVSLEHETLVLVVTSTFGNGDPPENGESFAAALMEMSGPYNSSPRPEQHKSYKIRFNSISCSDPLVSSWRRKRKESSNTDSAGALGTLRFCVFGLGSRAYPHFCAFARAVDTRLEELGGERLLQLGQGDELCGQEEAFRGWAQAAFQAACETFCVGEDAKAAARDIFSPKRSWKRQRYRLSAQAEGLQLLPGLIHVHRRKMFQATIRSVENLQSSKSTRATILVRLDTGGQEGLQYQPGDHIGVCPPNRPGLVEALLSRVEDPPAPTEPVAVEQLEKGSPGGPPPGWVRDPRLPPCTLRQALTFFLDITSPPSPQLLRLLSTLAEEPREQQELEALSQDPRRYEEWKWFRCPTLLEVLEQFPSVALPAPLLLTQLPLLQPRYYSVSSAPSTHPGEIHLTVAVLAYRTQDGLGPLHYGVCSTWLSQLKPGDPVPCFIRGAPSFRLPPDPSLPCILVGPGTGIAPFRGFWQERLHDIESKGLQPTPMTLVFGCRCSQLDHLYRDEVQNAQQRGVFGRVLTAFSREPDNPKTYVQDILRTELAAEVHRVLCLERGHMFVCGDVTMATNVLQTVQRILATEGDMELDEAGDVIGVLRDQQRYHEDIFGLTLRTQEVTSRIRTQSFSLQERQLRGAVPWAFDPPGSDTNSP
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Produces nitric oxide (NO) which is implicated in vascular smooth muscle relaxation through a cGMP-mediated signal transduction pathway (PubMed:1378832). NO mediates vascular endothelial growth factor (VEGF)-induced angiogenesis in coronary vessels and promotes blood clotting through the activation of platelets.
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Uniprot ID
Primary ID:
P29474

Secondarily ID:
A0S0A7
A0S0A8
A8KA63
B2RCQ1
E9PFR2
Q13662
Q14251
Q14434
Q548C1
Q6GSL5
Q9UDC6
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Ensembl ID
ENSG00000164867
HGNC ID
HGNC:7876
Subcellular Location
Cell membrane
Membrane
Caveola
Cytoplasm
Cytoskeleton
Golgi apparatus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000749 , HUVEC-C
Compound ID Compound Name Compound Formula
CP0376504
5-Cyclopropyl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C10H12N2S
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0425444
5-Ethynyl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
   Show/Hide
C9H8N2S
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0536715
6-Ethynyl-6,7-dihydro-thieno[3,2-c]pyridin-4-ylamine
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C9H8N2S
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0506680
8-Fluoro-3-(4-fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H12F2N2
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0454759
4,5-Dihydro-thieno[2,3-c]pyridin-7-ylamine
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C7H8N2S
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0053263
(2S)-2-azaniumyl-5-[(N'-methylcarbamimidoyl)amino]pentanoate
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C7H16N4O2
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0383554
6-Cyclopropyl-6,7-dihydro-thieno[3,2-c]pyridin-4-ylamine
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C10H12N2S
 1
1
IC50 = 750 nM
   TI
   LI
   LO
   TS
CP0507314
3-Ethynyl-3,4-dihydro-isoquinolin-1-ylamine
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C11H10N2
 1
1
IC50 = 900 nM
   TI
   LI
   LO
   TS
CP0380179
5-Furan-2-yl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C11H10N2OS
 1
1
IC50 = 920 nM
   TI
   LI
   LO
   TS
CP0402943
5-Thiophen-2-yl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C11H10N2S2
 1
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0464414
3,4-Dihydro-isoquinolin-1-ylamine
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C9H10N2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0044041
(L-N6-1-iminoethyl)lysine
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C8H17N3O2
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0043950
(S)-methyl 2-amino-5-(amino(nitroamino)methyleneamino)pentanoate
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C7H15N5O4
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0375487
3-Cyclopropyl-3,4-dihydro-isoquinolin-1-ylamine
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C12H14N2
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0463597
3-Methyl-3,4-dihydro-isoquinolin-1-ylamine
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C10H12N2
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0383447
5-Phenyl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C13H12N2S
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0466769
8-Chloro-3-(4-fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H12ClFN2
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0565395
3-Furan-2-yl-3,4-dihydro-isoquinolin-1-ylamine
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C13H12N2O
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0463500
5-Prop-1-ynyl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C10H10N2S
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0540144
8-Chloro-3-phenyl-3,4-dihydro-isoquinolin-1-ylamine
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C15H13ClN2
 1
1
IC50 = 6000 nM
   TI
   LI
   LO
   TS
CP0439003
3-Thiophen-2-yl-3,4-dihydro-isoquinolin-1-ylamine
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C13H12N2S
 1
1
IC50 = 8000 nM
   TI
   LI
   LO
   TS
CP0375511
3-Phenyl-3,4-dihydro-isoquinolin-1-ylamine
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C15H14N2
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0380411
3-(3-Fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H13FN2
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0466341
6-Phenyl-6,7-dihydro-thieno[3,2-c]pyridin-4-ylamine
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C13H12N2S
 1
1
IC50 = 9500 nM
   TI
   LI
   LO
   TS
CP0437466
5-Ethynyl-2-methyl-4,5-dihydro-thieno[2,3-c]pyridin-7-ylamine
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C10H10N2S
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0533020
4,5-Dihydro-3H-benzo[c]azepin-1-ylamine
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C10H12N2
 1
1
IC50 = 12000 nM
   TI
   LI
   LO
   TS
CP0416781
3-Thiazol-2-yl-3,4-dihydro-isoquinolin-1-ylamine
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C12H11N3S
 1
1
IC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0403965
3-(4-Fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H13FN2
 1
1
IC50 = 40000 nM
   TI
   LI
   LO
   TS
CP0496468
3-(2-Fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H13FN2
 1
1
IC50 = 44000 nM
   TI
   LI
   LO
   TS
CP0518313
5-Fluoro-3-(4-fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H12F2N2
 1
1
IC50 = 44000 nM
   TI
   LI
   LO
   TS
CP0503502
7-Fluoro-3-(4-fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H12F2N2
 1
1
IC50 = 55000 nM
   TI
   LI
   LO
   TS
CP0055850
Aminoguanidine
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CH6N4
 1
1
IC50 = 72000 nM
   TI
   LI
   LO
   TS
CP0466928
8-Fluoro-3-phenyl-3,4-dihydro-isoquinolin-1-ylamine
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C15H13FN2
 1
1
IC50 = 80000 nM
   TI
   LI
   LO
   TS
CP0492145
3-(4-Chloro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H13ClN2
 1
1
IC50 = 86000 nM
   TI
   LI
   LO
   TS
CP0404434
6-Fluoro-3-(4-fluoro-phenyl)-3,4-dihydro-isoquinolin-1-ylamine
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C15H12F2N2
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0053263
(2S)-2-azaniumyl-5-[(N'-methylcarbamimidoyl)amino]pentanoate
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C7H16N4O2
 7
1 IC50 = 540 nM
2 IC50 = 650 nM
3 IC50 = 3500 nM
4 IC50 = 5900 nM
5 IC50 = 6000 nM
6 IC50 = 8700 nM
7 Ki = 400 nM
CP0043950
(S)-methyl 2-amino-5-(amino(nitroamino)methyleneamino)pentanoate
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C7H15N5O4
 2
1 IC50 = 1500 nM
2 IC50 = 2700 nM
CP0047550
7-nitro-1H-indazole
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C7H5N3O2
 2
1 IC50 = 1890 nM
2 IC50 = 2500 nM
CP0044041
(L-N6-1-iminoethyl)lysine
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C8H17N3O2
 5
1 IC50 = 2400 nM
2 IC50 = 2600 nM
3 IC50 = 7900 nM
4 IC50 = 38000 nM
5 IC50 > 100000 nM
CP0223802
N'-[[3-(aminomethyl)phenyl]methyl]ethanimidamide
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C10H15N3
 1
1 IC50 = 51200 nM
CP0055850
Aminoguanidine
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CH6N4
 1
1 IC50 = 100000 nM
CP0040036
(S)-5-Acetimidoylamino-2-amino-pent
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C7H15N3O2
 1
1 Ki = 810 nM
Clinical Information about the Protein
Target 1 ( Nitric-oxide synthase endothelial (NOS3) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Coronary artery disease [ICD-11: BA80]
2 Hypertension [ICD-11: BA00-BA04]
3 Myocardial infarction [ICD-11: BA41-BA43]
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 ACCLAIM Phase 2
Coronary artery disease
2 L-NAME Phase 2
Hypertension
3 Tilarginine acetate Phase 3
Myocardial infarction
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01594 Nitric oxide synthase 3 Bos taurus, Bovine
PT04155 Nitric oxide synthase 3 Rattus norvegicus, Rat