General Information of the Protein
Protein ID
PT02547
Protein Name
D-amino-acid oxidase
Gene Name
DAO
Secondarily
Gene Name
DAMOX
Sequence
MRVVVIGAGVIGLSTALCIHERYHSVLQPLDIKVYADRFTPLTTTDVAAGLWQPYLSDPNNPQEADWSQQTFDYLLSHVHSPNAENLGLFLISGYNLFHEAIPDPSWKDTVLGFRKLTPRELDMFPDYGYGWFHTSLILEGKNYLQWLTERLTERGVKFFQRKVESFEEVAREGADVIVNCTGVWAGALQRDPLLQPGRGQIMKVDAPWMKHFILTHDPERGIYNSPYIIPGTQTVTLGGIFQLGNWSELNNIQDHNTIWEGCCRLEPTLKNARIIGERTGFRPVRPQIRLEREQLRTGPSNTEVIHNYGHGGYGLTIHWGCALEAAKLFGRILEEKKLSRMPPSHL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Regulates the level of the neuromodulator D-serine in the brain. Has high activity towards D-DOPA and contributes to dopamine synthesis. Could act as a detoxifying agent which removes D-amino acids accumulated during aging. Acts on a variety of D-amino acids with a preference for those having small hydrophobic side chains followed by those bearing polar, aromatic, and basic groups. Does not act on acidic amino acids.
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Uniprot ID
Primary ID:
P14920

Secondarily ID:
B2R7I5
Q16758
Q8N6R2
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Ensembl ID
ENSG00000110887
HGNC ID
HGNC:2671
Subcellular Location
Peroxisome
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0200164
N-[4-[2-[4-(diaminomethylideneamino)phenyl]ethyl]-1,3-thiazol-2-yl]acetamide
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C14H17N5OS
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0840759
N-{4-[2-(4-{[Amino(imino)methyl]amino}phenyl)ethyl]-5-[4-(methylsulfonyl)benzyl]-1,3-thiazol-2-yl}acetamidehydrochloride
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C22H26ClN5O3S2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0205967
6-[2-(3-fluorophenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C12H11FN2O2
 2
1 IC50 = 1.4 nM
2 IC50 = 9.7 nM
CP0367093
6-[2-(3,5-difluorophenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C12H10F2N2O2
 2
1 IC50 = 1.5 nM
2 IC50 = 11 nM
CP0137018
6-[2-(2-fluorophenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C12H11FN2O2
 2
1 IC50 = 2 nM
2 IC50 = 13 nM
CP0265140
6-[2-(3-methoxyphenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C13H14N2O3
 1
1 IC50 = 2.1 nM
CP0174406
US10202399, Example 237
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C11H10N2O3
 1
1 IC50 = 2.2 nM
CP0265142
6-[2-[3-(trifluoromethyl)phenyl]ethyl]-1,2-dihydropyridazine-3,4-dione
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C13H11F3N2O2
 2
1 IC50 = 2.4 nM
2 IC50 = 16 nM
CP0137019
6-[2-(4-chlorophenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C12H11ClN2O2
 2
1 IC50 = 2.7 nM
2 IC50 = 13 nM
CP0186475
6-[2-(4-methoxyphenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C13H14N2O3
 1
1 IC50 = 2.9 nM
CP0137017
6-[2-(4-fluorophenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C12H11FN2O2
 2
1 IC50 = 3.1 nM
2 IC50 = 10 nM
CP0231655
6-(2-phenylethyl)-1,2-dihydropyridazine-3,4-dione
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C12H12N2O2
 2
1 IC50 = 3.8 nM
2 IC50 = 10 nM
CP0174493
3-hydroxy-5-(2-phenylethyl)-1H-pyridin-2-one
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C13H13NO2
 2
1 IC50 = 3.9 nM
2 IC50 = 140 nM
CP0205973
US9212147, 40
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C12H18N2O2
 2
1 IC50 = 4.7 nM
2 IC50 = 31 nM
CP0121086
6-(1-phenylethyl)-1,2-dihydropyridazine-3,4-dione
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C12H12N2O2
 2
1 IC50 = 4.9 nM
2 IC50 = 32 nM
CP0176014
3-hydroxyquinolin-2(1H)-one, 2
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C9H7NO2
 3
1 IC50 = 6.9 nM
2 IC50 = 43 nM
3 Kd = 13 nM
CP0129275
6-[2-[2-(trifluoromethyl)phenyl]ethyl]-1,2-dihydropyridazine-3,4-dione
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C13H11F3N2O2
 2
1 IC50 = 8.4 nM
2 IC50 = 45 nM
CP0574281
5-[(3R)-7-chloro-3-methyl-2H-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C13H11ClN2O3S
 1
1 IC50 = 9 nM
CP0579643
5-[(3R)-3-methyl-7-(trifluoromethyl)-2H-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C14H11F3N2O3S
 1
1 IC50 = 9 nM
CP0184745
6-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,2-dihydropyridazine-3,4-dione
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C13H11F3N2O2
 2
1 IC50 = 12 nM
2 IC50 = 19 nM
CP0129278
US10463663, Example 40
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C11H9ClN2O2
 2
1 IC50 = 12 nM
2 IC50 = 17 nM
CP0164978
6-(3-phenylpropyl)-1,2-dihydropyridazine-3,4-dione
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C13H14N2O2
 1
1 IC50 = 13 nM
CP0231654
6-[2-(3,5-dimethoxyphenyl)ethyl]-1,2-dihydropyridazine-3,4-dione
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C14H16N2O4
 1
1 IC50 = 13 nM
CP0441581
US10202399, Example 21
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C12H10F2N2O2
 1
1 IC50 = 13 nM
CP0578758
5-[(3R)-7-(difluoromethyl)-2,3-dihydro-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C13H10F2N2O3S
 1
1 IC50 = 13 nM
CP0546648
(3R)-3-(5,6-dioxo-1,4-dihydropyrazin-2-yl)-2,3-dihydro-1,4-benzoxathiine-7-carbonitrile
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C13H9N3O3S
 1
1 IC50 = 20 nM
CP0579480
(3R)-3-(5,6-dioxo-1,4-dihydropyrazin-2-yl)-3-methyl-2H-1,4-benzoxathiine-7-carbonitrile
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C14H11N3O3S
 1
1 IC50 = 20 nM
CP0546647
5-[(3R)-7-chloro-2,3-dihydro-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C12H9ClN2O3S
 1
1 IC50 = 21 nM
CP0576992
5-[7-(trifluoromethyl)-2,3-dihydro-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C13H9F3N2O3S
 1
1 IC50 = 25 nM
CP0576993
5-[(3R)-7-methylsulfonyl-2,3-dihydro-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C13H12N2O5S2
 1
1 IC50 = 25 nM
CP0572801
4-[(5,6-dioxo-1,4-dihydropyrazin-2-yl)sulfanylmethyl]benzonitrile
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C12H9N3O2S
 1
1 IC50 = 43 nM
CP0546666
4-[(5,6-dioxo-1,4-dihydropyrazin-2-yl)methylsulfanyl]-2-fluorobenzonitrile
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C12H8FN3O2S
 1
1 IC50 = 46 nM
CP0546649
5-[(3R)-3-methyl-7-methylsulfonyl-2H-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C14H14N2O5S2
 1
1 IC50 = 51 nM
CP0578757
4-[(5,6-dioxo-1,4-dihydropyrazin-2-yl)sulfanylmethyl]-2-fluorobenzonitrile
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C12H8FN3O2S
 1
1 IC50 = 54 nM
CP0121087
6-[2-[3,5-bis(trifluoromethyl)phenyl]ethyl]-1,2-dihydropyridazine-3,4-dione
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C14H10F6N2O2
 2
1 IC50 = 57 nM
2 IC50 = 63 nM
CP0579837
5-[[4-(difluoromethyl)phenyl]methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C12H10F2N2O2S
 1
1 IC50 = 70 nM
CP0546650
5-[[4-(difluoromethyl)phenyl]sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C12H10F2N2O2S
 1
1 IC50 = 72 nM
CP0579106
5-[[4-(pentafluoro-lambda6-sulfanyl)phenyl]sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C11H9F5N2O2S2
 1
1 IC50 = 80 nM
CP0568248
5-[(4-methylsulfonylphenyl)sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C12H12N2O4S2
 1
1 IC50 = 82 nM
CP0579836
5-[(7-chloroquinolin-3-yl)sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C14H10ClN3O2S
 1
1 IC50 = 87 nM
CP0576368
5-[(4-methylsulfonylphenyl)methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C12H12N2O4S2
 1
1 IC50 = 90 nM
CP0546645
5-[[4-(trifluoromethyl)phenyl]methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C12H9F3N2O2S
 1
1 IC50 = 91 nM
CP0579104
5-[[4-(trifluoromethyl)phenyl]sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C12H9F3N2O2S
 1
1 IC50 = 92 nM
CP0578767
5-(3-methyl-2H-1,4-benzoxathiin-3-yl)-1,4-dihydropyrazine-2,3-dione
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C13H12N2O3S
 1
1 IC50 = 93 nM
CP0570422
5-[(3R)-7-fluoro-2,3-dihydro-1,4-benzoxathiin-3-yl]-1,4-dihydropyrazine-2,3-dione
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C12H9FN2O3S
 1
1 IC50 = 94 nM
CP0569387
5-[[4-(pentafluoro-lambda6-sulfanyl)phenyl]methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C11H9F5N2O2S2
 1
1 IC50 = 97 nM
CP0546651
2-chloro-4-[(5,6-dioxo-1,4-dihydropyrazin-2-yl)methylsulfanyl]benzonitrile
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C12H8ClN3O2S
 1
1 IC50 = 98 nM
CP0717824
(E)-6-(4-chlorostyryl)-4-hydroxypyridazin-3(2H)-one
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C12H9ClN2O2
 1
1 IC50 = 120 nM
CP0579105
5-[(4-chlorophenyl)sulfanylmethyl]-1,4-dihydropyrazine-2,3-dione
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C11H9ClN2O2S
 1
1 IC50 = 130 nM
CP0044110
4H-furo[3,2-b]pyrrole-5-carboxylic acid
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C7H5NO3
 5
1 IC50 = 141 nM
2 Kd = 3.1 nM
3 Kd = 14 nM
4 Kd = 29 nM
5 Kd = 37 nM
CP0569386
5-[(4-chlorophenyl)methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C11H9ClN2O2S
 1
1 IC50 = 150 nM
CP0569412
4-[2-(5,6-dioxo-1,4-dihydropyrazin-2-yl)ethyl]-2-fluorobenzonitrile
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C13H10FN3O2
 1
1 IC50 = 180 nM
CP0579102
5-[2-(3-chlorophenyl)ethyl]-1,4-dihydropyrazine-2,3-dione
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C12H11ClN2O2
 1
1 IC50 = 190 nM
CP0569210
5-[[6-(trifluoromethyl)pyridin-3-yl]methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C11H8F3N3O2S
 1
1 IC50 = 250 nM
CP0579103
5,6-dioxo-3-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,4-dihydropyrazine-2-carbonitrile
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C14H10F3N3O2
 1
1 IC50 = 250 nM
CP0164975
6-Cyclohexyl-4-hydroxypyridazin-3(2H)-one
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C10H14N2O2
 1
1 IC50 = 300 nM
CP0579835
5-[(3,4-difluorophenyl)methylsulfanyl]-1,4-dihydropyrazine-2,3-dione
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C11H8F2N2O2S
 1
1 IC50 = 300 nM
CP0546642
5-[2-[3-fluoro-4-(5-oxo-1,2-dihydropyrazol-3-yl)phenyl]ethyl]-1,4-dihydropyrazine-2,3-dione
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C15H13FN4O3
 1
1 IC50 = 320 nM
CP0546654
5-(2,3-dihydro-1,4-benzoxathiin-3-yl)-1,4-dihydropyrazine-2,3-dione
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C12H10N2O3S
 1
1 IC50 = 406 nM
CP0544878
3-[(5,6-dioxo-1,4-dihydropyrazin-2-yl)sulfanylmethyl]benzonitrile
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C12H9N3O2S
 1
1 IC50 = 440 nM
CP0569385
5-(2-quinolin-6-ylethyl)-1,4-dihydropyrazine-2,3-dione
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C15H13N3O2
 1
1 IC50 = 580 nM
CP0443179
6-(3,3-dimethylbutyl)-1,2-dihydropyridazine-3,4-dione
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C10H16N2O2
 1
1 IC50 = 670 nM
CP0579479
5-[2-[6-(difluoromethoxy)pyridin-3-yl]ethyl]-1,4-dihydropyrazine-2,3-dione
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C12H11F2N3O3
 1
1 IC50 = 670 nM
CP0576029
5-chloro-6-[2-[4-(trifluoromethyl)phenyl]ethyl]-1,4-dihydropyrazine-2,3-dione
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C13H10ClF3N2O2
 1
1 IC50 = 1500 nM
CP0183257
2-methyl-1,2,4-triazinane-3,5,6-trione
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C4H5N3O3
 1
1 IC50 = 3100 nM
CP0570177
4-[2-(5,6-dioxo-1,4-dihydropyrazin-2-yl)ethyl]benzonitrile
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C13H11N3O2
 1
1 IC50 = 5800 nM
CP0281664
naphthyridinone analog.,18
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C8H6N2O2
 1
1 Kd = 2 nM
CP0044107
3-hydroxyquinolin-2(1H)-one, 10
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C9H6ClNO2
 2
1 Kd = 2.5 nM
2 Kd = 7 nM
CP0203193
3-hydroxyquinolin-2(1H)-one, 26
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C9H5ClFNO2
 2
1 Kd = 4.6 nM
2 Kd = 5.5 nM
CP0296215
3-hydroxyquinolin-2(1H)-one, 5
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C9H6FNO2
 1
1 Kd = 17 nM
CP0281665
3-hydroxyquinolin-2(1H)-one, 6
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C9H6FNO2
 1
1 Kd = 18 nM
CP0296216
3-hydroxyquinolin-2(1H)-one, 15
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C11H11NO2
 1
1 Kd = 25 nM
CP0371190
3-hydroxyquinolin-2(1H)-one, 4
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C9H6FNO2
 1
1 Kd = 38 nM
Clinical Information about the Protein
Target 1 ( D-amino acid oxidase (DAO) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Friedreich's ataxia [ICD-11: 8A03.10]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 TAK-831 Phase 2
Friedreich's ataxia