General Information of the Protein
Protein ID
PT02485
Protein Name
cGMP-specific 3',5'-cyclic phosphodiesterase
Secondarily
Protein Name
cGMP-binding cGMP-specific phosphodiesterase
Gene Name
PDE5A
Secondarily
Gene Name
Pde5
Sequence
MLPFGDKTRDMVNAWFSERVHNIPVCKEGIRAHTESCSCSLPQSPHADNTTPGAPARKISASEFDRPLRPIVVKDSEGTVSFLSDSGKKEQMPLTSPRFDSDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSKDKFLVSRLFDVAEGSTLEEASNNCIRLEWNKGIVGHVAAFGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCPDSFSRVFQMEWEEVGKSSEPLTREHDANKINYMYAQYVKNTMEPLNIPDVTKDNRFPWTNENMGHINTHCIRSLLCTPIKNGKKNKVIGVCQLVNKMEEKTGKIKAFNQNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQALAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLETLALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSTMEHHHFDQCLMVLNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNEFSFEDPLQKELFLAMLMTACDLSAITKPWPIQQRIAELVAAEFFDQGDRERKELNMEPADLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCLPLLDGCRKNRQKWQALADQQEKTLLNGESGQAKRD
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Organism
Rattus norvegicus, Rat
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 5
>
Phosphodiesterase 5A
Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP. Specifically regulates nitric-oxide-generated cGMP.
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Uniprot ID
O54735
Ensembl ID
ENSG00000138735
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: CL000070 , RFL-6
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0381670
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-(5-pyridin-2-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H21N5O2
  1
1
IC50 = 0.4 nM
 Bioactivity Info 
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CP0376603
 Compound Info 
3-Benzo[1,3]dioxol-5-yl-2-(4-imidazol-1-yl-phenyl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C27H20N4O3
  1
1
IC50 = 1.75 nM
 Bioactivity Info 
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CP0509609
 Compound Info 
2-(5-Bromo-pyrimidin-2-yl)-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C23H17BrN4O2
  1
1
IC50 = 1.9 nM
 Bioactivity Info 
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CP0554268
 Compound Info 
(R)-3-(2,3-Dihydro-benzofuran-5-yl)-2-(5-pyridin-2-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H21N5O2
  1
1
Ki = 0.019 nM
 Bioactivity Info 
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CP0381660
 Compound Info 
(R)-3-(2,3-Dihydro-benzofuran-5-yl)-2-pyridin-2-yl-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C24H19N3O2
  1
1
Ki = 0.12 nM
 Bioactivity Info 
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CP0496997
 Compound Info 
2-[2,3'']Bipyridinyl-6''-yl-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C29H22N4O2
  1
1
Ki = 0.15 nM
 Bioactivity Info 
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CP0502715
 Compound Info 
2-[5-(3-Benzyl-3H-imidazol-4-yl)-pyridin-2-yl]-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C34H27N5O2
  1
1
Ki = 0.17 nM
 Bioactivity Info 
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CP0393282
 Compound Info 
3-Benzofuran-5-yl-2-(5-pyridin-2-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H19N5O2
  1
1
Ki = 0.19 nM
 Bioactivity Info 
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CP0393260
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-(5-pyridin-4-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H21N5O2
  1
1
Ki = 0.22 nM
 Bioactivity Info 
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CP0430100
 Compound Info 
2-[5-(3-Benzyl-2-methyl-3H-imidazol-4-yl)-pyrimidin-2-yl]-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C34H28N6O2
  1
1
Ki = 0.24 nM
 Bioactivity Info 
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CP0508226
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-[5-(2,3-dimethyl-3H-imidazol-4-yl)-pyrimidin-2-yl]-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H24N6O2
  1
1
Ki = 0.24 nM
 Bioactivity Info 
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CP0496995
 Compound Info 
3-Benzo[1,3]dioxol-5-yl-2-(5-pyridin-3-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C27H19N5O3
  1
1
Ki = 0.29 nM
 Bioactivity Info 
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CP0500747
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-[5-(3-methyl-3H-imidazol-4-yl)-pyridin-2-yl]-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H23N5O2
  1
1
Ki = 0.33 nM
 Bioactivity Info 
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CP0430102
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-(5-pyridin-3-yl-pyrimidin-2-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H21N5O2
  1
1
Ki = 0.36 nM
 Bioactivity Info 
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CP0501159
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-(4-imidazol-1-yl-phenyl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C28H22N4O2
  1
1
Ki = 0.51 nM
 Bioactivity Info 
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CP0244408
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-[5-(4-methoxy-phenyl)-pyrimidin-2-yl]-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-on
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C30H24N4O3
  1
1
Ki = 0.52 nM
 Bioactivity Info 
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CP0277224
 Compound Info 
2-{5-[4-(2-Diethylamino-ethoxy)-phenyl]-pyrimidin-2-yl}-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C35H35N5O3
  1
1
Ki = 0.53 nM
 Bioactivity Info 
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CP0497305
 Compound Info 
3-(2,3-Dihydro-benzofuran-5-yl)-2-pyridin-2-yl-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C24H19N3O2
  1
1
Ki = 0.65 nM
 Bioactivity Info 
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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
  1
1
Ki = 1.8 nM
 Bioactivity Info 
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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
Ki = 5 nM
 Bioactivity Info 
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CP0502519
 Compound Info 
2-[2,2'']Bipyridinyl-5-yl-3-(2,3-dihydro-benzofuran-5-yl)-1,2,3,4-tetrahydro-pyrrolo[3,4-b]quinolin-9-one
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C29H22N4O2
  1
1
Ki = 6.43 nM
 Bioactivity Info 
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Biochemical Assays
Compound ID Compound Name Compound Formula
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 EC50 = 78 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 = 0.3 nM
2 IC50 = 2 nM