General Information of the Protein
Protein ID
PT03334
Protein Name
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
Secondarily
Protein Name
cGMP phosphodiesterase 6C
Gene Name
PDE6C
Secondarily
Gene Name
PDEA2
Sequence
MGEINQVAVEKYLEENPQFAKEYFDRKLRVEVLGEIFKNSQVPVQSSMSFSELTQVEESALCLELLWTVQEEGGTPEQGVHRALQRLAHLLQADRCSMFLCRSRNGIPEVASRLLDVTPTSKFEDNLVGPDKEVVFPLDIGIVGWAAHTKKTHNVPDVKKNSHFSDFMDKQTGYVTKNLLATPIVVGKEVLAVIMAVNKVNASEFSKQDEEVFSKYLNFVSIILRLHHTSYMYNIESRRSQILMWSANKVFEELTDVERQFHKALYTVRSYLNCERYSIGLLDMTKEKEFYDEWPIKLGEVEPYKGPKTPDGREVNFYKIIDYILHGKEEIKVIPTPPADHWTLISGLPTYVAENGFICNMMNAPADEYFTFQKGPVDETGWVIKNVLSLPIVNKKEDIVGVATFYNRKDGKPFDEHDEYITETLTQFLGWSLLNTDTYDKMNKLENRKDIAQEMLMNQTKATPEEIKSILKFQEKLNVDVIDDCEEKQLVAILKEDLPDPRSAELYEFRFSDFPLTEHGLIKCGIRLFFEINVVEKFKVPVEVLTRWMYTVRKGYRAVTYHNWRHGFNVGQTMFTLLMTGRLKKYYTDLEAFAMLAAAFCHDIDHRGTNNLYQMKSTSPLARLHGSSILERHHLEYSKTLLQDESLNIFQNLNKRQFETVIHLFEVAIIATDLALYFKKRTMFQKIVDACEQMQTEEEAIKYVTVDPTKKEIIMAMMMTACDLSAITKPWEVQSQVALMVANEFWEQGDLERTVLQQQPIPMMDRNKRDELPKLQVGFIDFVCTFVYKEFSRFHKEITPMLSGLQNNRVEWKSLADEYDAKMKVIEEEAKKQEGGAEKAAEDSGGGDDKKSKTCLML
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 6
>
Phosphodiesterase 6C
Function
As cone-specific cGMP phosphodiesterase, it plays an essential role in light detection and cone phototransduction by rapidly decreasing intracellular levels of cGMP.
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Uniprot ID
Primary ID:
P51160

Secondarily ID:
A6NCR6
Q5VY29
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HGNC ID
HGNC:8787
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0087426
21-methyl-3,13,21-triazapentacyclo[11.8.0.02,10.04,9.015,20]henicosa-2(10),4,6,8,15,17,19-heptaen-14-one
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C19H17N3O
 1
1
EC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0955774
(S)-4-Methoxy-14-methyl-7,8,13b,14-tetrahydroindolo-[2',3':3,4]pyrido[2,1-b]quinazolin-5(13H)-one
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C20H19N3O2
 1
1
EC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0959864
4-Methoxyevodiamine
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C20H19N3O2
 1
1
EC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0385143
2-[4-[4-ethoxy-3-(3-ethyl-1-methyl-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenoxy]piperidin-1-yl]-N-hydroxypyrimidine-5-carboxamide
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C26H30N8O5
 1
1
IC50 = 0.13 nM
   TI
   LI
   LO
   TS
CP0411277
(3S)-3-(5-ethylthiophen-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5OS
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0391810
(3S)-3-(5-ethylfuran-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5O2
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
   TS
CP0175962
3-(5-ethylfuran-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5O2
 1
1
IC50 = 2.3 nM
   TI
   LI
   LO
   TS
CP0007669
3-[[4-ethoxy-3-(3-ethyl-1-methyl-7-oxo-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxycyclobutane-1-carboxamide
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C22H27N5O4
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0457227
3-(5-ethylthiophen-2-yl)-2-pyrimidin-2-yl-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C21H18N4OS
 1
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0383136
(3R)-3-(5-ethylfuran-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5O2
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0117113
3-(5-ethylthiophen-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5OS
 1
1
IC50 = 4.8 nM
   TI
   LI
   LO
   TS
CP0383137
3-(5-ethylfuran-2-yl)-2-pyrimidin-2-yl-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C21H18N4O2
 1
1
IC50 = 6.2 nM
   TI
   LI
   LO
   TS
CP0392075
(10R,15R)-13-ethyl-10-(5-ethylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0440103
(10S,15S)-13-ethyl-10-(3-methylthiophen-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C20H19N3O2S
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0384486
N-[3-(4,5-diethyl-6-oxo-1H-pyrimidin-2-yl)-4-propoxyphenyl]-2-(4-methylpiperazin-1-yl)acetamide
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C24H35N5O3
 1
1
IC50 = 19.8 nM
   TI
   LI
   LO
   TS
CP0411276
(3R)-3-(5-ethylthiophen-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one
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C26H21N5OS
 1
1
IC50 = 34.1 nM
   TI
   LI
   LO
   TS
CP0010658
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
IC50 = 36.42 nM
   TI
   LI
   LO
   TS
CP0157969
(10S,15S)-13-ethyl-10-(5-ethylthiophen-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O2S
 1
1
IC50 = 56 nM
   TI
   LI
   LO
   TS
CP0157968
(10S,15S)-13-ethyl-10-(5-methylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C20H19N3O3
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0392073
(10S,15S)-13-butyl-10-(5-ethylthiophen-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C23H25N3O2S
 1
1
IC50 = 107 nM
   TI
   LI
   LO
   TS
CP0257911
(10S,15S)-13-ethyl-10-(5-ethylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O3
 1
1
IC50 = 127 nM
   TI
   LI
   LO
   TS
CP0109248
(2S,8R)-2-(5-bromothiophen-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C19H16BrN3O2S
 1
1
IC50 = 136 nM
   TI
   LI
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CP0392076
2-[5-(3,4-dimethoxyphenyl)pyrimidin-2-yl]-1-(5-ethylthiophen-2-yl)-3,9-dihydro-1H-pyrido[3,4-b]indol-4-one
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C29H26N4O3S
 1
1
IC50 = 253 nM
   TI
   LI
   LO
   TS
CP0438006
2-[5-(3,4-dimethoxyphenyl)pyrimidin-2-yl]-1-(5-ethylfuran-2-yl)-3,9-dihydro-1H-pyrido[3,4-b]indol-4-one
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C29H26N4O4
 1
1
IC50 = 288 nM
   TI
   LI
   LO
   TS
CP0000847
(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
 2
1
IC50 = 402 nM
   TI
   LI
   LO
   TS
2
IC50 > 10000 nM
   TI
   LI
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CP0176508
[4-[3-(3-fluoro-4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C29H31FN4O2
 1
1
IC50 > 10000 nM
   TI
   LI
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CP0365459
[4-[5-tert-butyl-3-(3,5-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C26H32F2N4O2
 1
1
IC50 > 10000 nM
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CP0419692
N-(2-hydroxyethyl)-4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]benzamide
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C26H27N3O3
 1
1
IC50 > 10000 nM
   TI
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CP0419693
[4-[5-tert-butyl-3-(2,3-difluoro-4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C26H32F2N4O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
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CP0444327
[4-[3-(4-methoxyphenyl)-5-(2-methylphenyl)-3,4-dihydropyrazol-2-yl]phenyl]-(4-methylpiperazin-1-yl)methanone
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C29H32N4O2
 1
1
IC50 > 10000 nM
   TI
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CP0833740
(S)-4,9-Dimethoxy-14-methyl-7,8,13b,14-tetrahydroindolo-[2',3':3,4]pyrido[2,1-b]quinazolin-5(13H)-one
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C21H21N3O3
 1
1
IC50 > 40000 nM
   TI
   LI
   LO
   TS
CP0109250
(2S,8R)-6-methyl-2-(5-methylthiophen-2-yl)-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C20H19N3O2S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0144390
(2S,8R)-2-(5-ethylfuran-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C21H21N3O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0164472
(10S,15R)-13-ethyl-10-(5-ethylthiophen-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O2S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0168902
(10S,15R)-13-ethyl-10-(5-ethylfuran-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C21H21N3O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0268684
(2S,8R)-2-(5-ethylthiophen-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C21H21N3O2S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0392491
(2R,8S)-2-(5-ethylthiophen-2-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
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C21H21N3O2S
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0432292
(10S,15R)-13-butyl-10-(5-ethylthiophen-2-yl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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C23H25N3O2S
 1
1
IC50 > 1000 nM
   TI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0010658
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
 3
1 IC50 = 24 nM
2 IC50 = 39.2 nM
3 IC50 = 160 nM