General Information of the Protein
Protein ID
PT02047
Protein Name
cGMP-dependent 3',5'-cyclic phosphodiesterase
Secondarily
Protein Name
Cyclic GMP-stimulated phosphodiesterase
Gene Name
PDE2A
Sequence
MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDISGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCNGLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAVEKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDLDASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVVEDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTDEDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITEARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPDAYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAFSIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYSSEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 2
>
Phosphodiesterase 2A
Function
cGMP-activated cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes (PubMed:9210593, PubMed:29392776, PubMed:15938621). Has a higher efficiency with cGMP compared to cAMP (PubMed:15938621). Plays a role in cell growth and migration (PubMed:24705027).
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Uniprot ID
Primary ID:
O00408

Secondarily ID:
B2R646
B3KRV5
E9PGI1
F6W5Z0
Q5J791
Q5J792
Q5J793
Q6ZMR1
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Ensembl ID
ENSG00000186642
HGNC ID
HGNC:8777
Subcellular Location
Cell membrane
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: CL000012 , Sf21
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0218066
 Compound Info 
US8598155, 13
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C20H18F3N7
  1
1
IC50 = 0.3 nM
 Bioactivity Info 
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CP0071226
 Compound Info 
2-(3,4-Dimethoxy-benzyl)-7-[(R)-1-((R)-1-hydroxy-ethyl)-4-phenyl-butyl]-5-methyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one
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C27H32N4O4
  1
1
IC50 = 0.5 nM
 Bioactivity Info 
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CP0057278
 Compound Info 
4-(3-fluoroazetidin-1-yl)-7-methyl-5-[1-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazine
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C20H17F4N7
  1
1
IC50 = 0.53 nM
 Bioactivity Info 
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CP0508501
 Compound Info 
US8598155, 8
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C21H23N7O
  1
1
IC50 = 0.58 nM
 Bioactivity Info 
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CP0346271
 Compound Info 
US8598155, 36
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C20H20FN7O
  1
1
IC50 = 0.82 nM
 Bioactivity Info 
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CP0109700
 Compound Info 
US11419874, PF-05180999
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C19H17F3N8
  2
1
IC50 = 1 nM
 Bioactivity Info 
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2
IC50 = 1.6 nM
 Bioactivity Info 
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CP0365601
 Compound Info 
US8598155, 55
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C20H19F2N7O
  1
1
IC50 = 1.08 nM
 Bioactivity Info 
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CP0389403
 Compound Info 
7-methyl-5-[1-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazin-4-amine
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C17H14F3N7
  1
1
IC50 = 1.3 nM
 Bioactivity Info 
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CP0118848
 Compound Info 
US11419874, Example 15
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C20H18F3N7
  2
1
IC50 = 1.6 nM
 Bioactivity Info 
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2
IC50 = 2.3 nM
 Bioactivity Info 
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CP0945317
 Compound Info 
5-[5-(4-Chloro-2-fluorophenyl)-1-methyl-1H-pyrazol-4-yl]-4-(3-fluoroazetidin-1-yl)-7-methylimidazo[5,1-f][1,2,4]triazine
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C19H16ClF2N7
  1
1
IC50 = 1.72 nM
 Bioactivity Info 
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CP0125532
 Compound Info 
US8829010, 9
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C21H23N7
  1
1
IC50 = 2 nM
 Bioactivity Info 
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CP0477919
 Compound Info 
US8598155, 53
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C21H19F4N7O
  1
1
IC50 = 2.01 nM
 Bioactivity Info 
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CP0523499
 Compound Info 
1-(2,5-dichlorophenyl)-8-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C17H12Cl2N4O
  1
1
IC50 = 3.31 nM
 Bioactivity Info 
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CP0425174
 Compound Info 
US8829010, 33
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C22H23N7
  1
1
IC50 = 3.4 nM
 Bioactivity Info 
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CP0508422
 Compound Info 
US8829010, 17
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C23H26N8O2
  1
1
IC50 = 3.6 nM
 Bioactivity Info 
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CP0567196
 Compound Info 
US8829010, 7
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C24H30N8
  1
1
IC50 = 4.9 nM
 Bioactivity Info 
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CP0397671
 Compound Info 
8-chloro-1-(2,5-dichlorophenyl)-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C16H9Cl3N4
  1
1
IC50 = 5.31 nM
 Bioactivity Info 
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CP0459888
 Compound Info 
US8829010, 40
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C22H25N7O
  1
1
IC50 = 5.8 nM
 Bioactivity Info 
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CP0425177
 Compound Info 
3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C20H22N6O
  1
1
IC50 = 7.1 nM
 Bioactivity Info 
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CP0425176
 Compound Info 
3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methyl-4-pyrrolidin-1-ylpyrazolo[3,4-d]pyrimidine
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C22H25N7
  1
1
IC50 = 7.8 nM
 Bioactivity Info 
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CP0325892
 Compound Info 
US8598155, 5
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C18H17ClN8
  1
1
IC50 = 8.2 nM
 Bioactivity Info 
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CP0455777
 Compound Info 
US8829010, 4
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C19H17F3N8
  2
1
IC50 = 8.9 nM
 Bioactivity Info 
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2
IC50 = 9 nM
 Bioactivity Info 
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CP0479685
 Compound Info 
US8829010, 37
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C21H22N8
  1
1
IC50 = 8.9 nM
 Bioactivity Info 
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CP0465365
 Compound Info 
6-fluoro-1-(2-fluoro-5-methoxyphenyl)-8-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C18H14F2N4O2
  1
1
IC50 = 9.3 nM
 Bioactivity Info 
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CP0539078
 Compound Info 
3-[1-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C19H17F3N6O
  1
1
IC50 = 9.7 nM
 Bioactivity Info 
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CP0558877
 Compound Info 
7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazin-4-amine
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C16H13F3N8
  1
1
IC50 = 11 nM
 Bioactivity Info 
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CP0389405
 Compound Info 
1-[1-methyl-3-[1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]pyrazol-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]azetidin-3-ol
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C19H17F3N8O
  1
1
IC50 = 12 nM
 Bioactivity Info 
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CP0539077
 Compound Info 
US8829010, 1
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C20H21N7
  1
1
IC50 = 17.7 nM
 Bioactivity Info 
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CP0548141
 Compound Info 
5-[2-(2-methoxyphenyl)ethoxy]-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-[1,2,4]triazolo[4,3-a]pyrazine
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C24H19F3N6O2
  1
1
IC50 = 24.4 nM
 Bioactivity Info 
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CP0459875
 Compound Info 
3-[1-methyl-5-(4-methylphenyl)pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C19H20N6O
  1
1
IC50 = 27.7 nM
 Bioactivity Info 
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CP0139294
 Compound Info 
1-(2-chlorophenyl)-6,8-dimethoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C18H15ClN4O2
  1
1
IC50 = 30.3 nM
 Bioactivity Info 
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CP0405134
 Compound Info 
6-fluoro-8-methoxy-1-(5-methoxypyridin-3-yl)-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C17H14FN5O2
  1
1
IC50 = 39.4 nM
 Bioactivity Info 
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CP0447308
 Compound Info 
4-[3-(4-methoxyphenoxy)azetidin-1-yl]-1-methyl-3-(2-methylpropyl)pyrazolo[3,4-d]pyrimidine
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C20H25N5O2
  1
1
IC50 = 66.6 nM
 Bioactivity Info 
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CP0552624
 Compound Info 
3-[[1-methyl-3-[1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]pyrazol-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]amino]propanoic acid
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C19H17F3N8O2
  1
1
IC50 = 72 nM
 Bioactivity Info 
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CP0391296
 Compound Info 
6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-phenylmethoxyimidazo[5,1-c][1,2,4]benzotriazine
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C24H21N5O2
  1
1
IC50 = 80.6 nM
 Bioactivity Info 
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CP0448768
 Compound Info 
3-[5-(4-methoxyphenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C19H20N6O2
  1
1
IC50 = 108.5 nM
 Bioactivity Info 
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CP0536918
 Compound Info 
5-propoxy-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-[1,2,4]triazolo[4,3-a]pyrazine
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C18H15F3N6O
  1
1
IC50 = 115 nM
 Bioactivity Info 
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CP0412958
 Compound Info 
4-(1,3-dihydroisoindol-2-yl)-1-methyl-3-(2-methylpropyl)pyrazolo[3,4-d]pyrimidine
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C18H21N5
  1
1
IC50 = 146.4 nM
 Bioactivity Info 
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CP0425175
 Compound Info 
4-(azetidin-1-yl)-1-methyl-3-(1-methyl-5-phenylpyrazol-4-yl)pyrazolo[3,4-d]pyrimidine
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C19H19N7
  1
1
IC50 = 188.7 nM
 Bioactivity Info 
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CP0075285
 Compound Info 
2-methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazine
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C15H18N4O
  1
1
IC50 = 239 nM
 Bioactivity Info 
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CP0508405
 Compound Info 
3-[5-(4-fluorophenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C18H17FN6O
  1
1
IC50 = 240.8 nM
 Bioactivity Info 
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CP0508406
 Compound Info 
3-[5-(4-methylphenyl)-1H-pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C18H18N6O
  1
1
IC50 = 297.8 nM
 Bioactivity Info 
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CP0139291
 Compound Info 
6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazine
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C18H14F3N5O
  1
1
IC50 = 346.5 nM
 Bioactivity Info 
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CP0425178
 Compound Info 
5-[2-(2-methoxyphenyl)ethoxy]-3-(2-methylpropyl)-[1,2,4]triazolo[4,3-a]pyrazine
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C18H22N4O2
  1
1
IC50 = 389.6 nM
 Bioactivity Info 
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CP0508421
 Compound Info 
4-[3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methylpyrazolo[3,4-d]pyrimidin-4-yl]morpholine
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C22H25N7O
  1
1
IC50 = 423 nM
 Bioactivity Info 
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CP0558296
 Compound Info 
3-(1-methyl-5-phenylpyrazol-4-yl)-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C18H18N6O
  1
1
IC50 = 566.1 nM
 Bioactivity Info 
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CP0447309
 Compound Info 
4-(azetidin-1-yl)-3-[5-(5-cyclopropylpyrimidin-2-yl)-1-methylpyrazol-4-yl]-1-methylpyrazolo[3,4-d]pyrimidine
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C20H21N9
  1
1
IC50 = 1012.7 nM
 Bioactivity Info 
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CP0301299
 Compound Info 
8-fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C18H14F2N4O
  1
1
IC50 = 1150 nM
 Bioactivity Info 
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CP0454560
 Compound Info 
3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methyl-4-(4-methylpiperazin-1-yl)pyrazolo[3,4-d]pyrimidine
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C23H28N8
  1
1
IC50 = 1407 nM
 Bioactivity Info 
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CP0548142
 Compound Info 
3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-[1,2,4]triazolo[4,3-a]pyrazine
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C15H9F3N6
  1
1
IC50 = 2107.4 nM
 Bioactivity Info 
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CP0558297
 Compound Info 
3-(2-methylpropyl)-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine
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C12H18N4O
  1
1
IC50 = 5323.8 nM
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Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0071226
 Compound Info 
2-(3,4-Dimethoxy-benzyl)-7-[(R)-1-((R)-1-hydroxy-ethyl)-4-phenyl-butyl]-5-methyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one
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C27H32N4O4
  5
1 IC50 = 0.03 nM
2 IC50 = 0.86 nM
3 IC50 = 2 nM
4 IC50 = 4.7 nM
5 IC50 = 4.8 nM
CP0218066
 Compound Info 
US8598155, 13
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C20H18F3N7
  1
1 IC50 = 0.303 nM
CP0508501
 Compound Info 
US8598155, 8
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C21H23N7O
  1
1 IC50 = 0.578 nM
CP0057278
 Compound Info 
4-(3-fluoroazetidin-1-yl)-7-methyl-5-[1-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazine
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C20H17F4N7
  1
1 IC50 = 0.633 nM
CP0346271
 Compound Info 
US8598155, 36
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C20H20FN7O
  1
1 IC50 = 0.825 nM
CP0109700
 Compound Info 
US11419874, PF-05180999
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C19H17F3N8
  2
1 IC50 = 1 nM
2 IC50 = 1.61 nM
CP0365601
 Compound Info 
US8598155, 55
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C20H19F2N7O
  1
1 IC50 = 1.08 nM
CP0118848
 Compound Info 
US11419874, Example 15
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C20H18F3N7
  1
1 IC50 = 1.6 nM
CP0125532
 Compound Info 
US8829010, 9
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C21H23N7
  1
1 IC50 = 2 nM
CP0477919
 Compound Info 
US8598155, 53
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C21H19F4N7O
  1
1 IC50 = 2.01 nM
CP0383857
 Compound Info 
4-cyclobutyl-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)pyridin-2-yl]pyrazol-4-yl]imidazo[5,1-f][1,2,4]triazine
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C20H18F3N7
  1
1 IC50 = 2.3 nM
CP0304264
 Compound Info 
3-(2-chlorophenyl)-12-methoxy-5-methyl-2,4,7,8,13-pentazatricyclo[7.4.0.02,6]trideca-1(9),3,5,7,10,12-hexaene
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C16H12ClN5O
  2
1 IC50 = 4 nM
2 IC50 = 4.3 nM
CP0325892
 Compound Info 
US8598155, 5
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C18H17ClN8
  1
1 IC50 = 8.19 nM
CP0090153
 Compound Info 
4-[[1-(5-butoxypyridin-3-yl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxalin-8-yl]methyl]morpholine
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C24H28N6O2
  1
1 IC50 = 10 nM
CP0225130
 Compound Info 
1-(2-chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline
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C16H11ClN4
  1
1 IC50 = 21 nM
CP0139294
 Compound Info 
1-(2-chlorophenyl)-6,8-dimethoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C18H15ClN4O2
  1
1 IC50 = 30.3 nM
CP0147040
 Compound Info 
US11419874, Example 28
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C15H10ClN5
  1
1 IC50 = 69 nM
CP0075285
 Compound Info 
2-methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazine
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C15H18N4O
  3
1 IC50 = 239 nM
2 IC50 = 270 nM
3 IC50 = 2160 nM
CP0139291
 Compound Info 
6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazine
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C18H14F3N5O
  1
1 IC50 = 346.5 nM
CP0301299
 Compound Info 
8-fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine
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C18H14F2N4O
  1
1 IC50 = 1150 nM
CP0059743
 Compound Info 
1-methyl-3-(2-methylpropyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione
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C10H14N4O2
  1
1 IC50 = 12000 nM
CP0010658
 Compound Info 
5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
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C22H30N6O4S
  2
1 IC50 = 63000 nM
2 IC50 > 10000 nM
CP0000847
 Compound Info 
(2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione
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C22H19N3O4
  1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Phosphodiesterase 2A (PDE2A) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Irritable bowel syndrome [ICD-11: DD91.0]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Tofisopam
 Drug Info 
Phase 2
Irritable bowel syndrome
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT00681 Phosphodiesterase Macaca mulatta, Rhesus macaque
 Protein Info