Protein Information

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 Show/Hide
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). Show/Hide
Uniprot ID	Primary ID: O00408 Secondarily ID: B2R646 B3KRV5 E9PGI1 F6W5Z0 Q5J791 Q5J792 Q5J793 Q6ZMR1 Show/Hide
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 Show/Hide	C20H18F3N7	1
1	IC50 = 0.3 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C27H32N4O4	1
1	IC50 = 0.5 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C20H17F4N7	1
1	IC50 = 0.53 nM Bioactivity Info	TI LI LO TS
CP0508501 Compound Info	US8598155, 8 Show/Hide	C21H23N7O	1
1	IC50 = 0.58 nM Bioactivity Info	TI LI LO TS
CP0346271 Compound Info	US8598155, 36 Show/Hide	C20H20FN7O	1
1	IC50 = 0.82 nM Bioactivity Info	TI LI LO TS
CP0109700 Compound Info	US11419874, PF-05180999 Show/Hide	C19H17F3N8	2
1	IC50 = 1 nM Bioactivity Info	TI LI LO TS
2	IC50 = 1.6 nM Bioactivity Info	TI LI LO TS
CP0365601 Compound Info	US8598155, 55 Show/Hide	C20H19F2N7O	1
1	IC50 = 1.08 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C17H14F3N7	1
1	IC50 = 1.3 nM Bioactivity Info	TI LI LO TS
CP0118848 Compound Info	US11419874, Example 15 Show/Hide	C20H18F3N7	2
1	IC50 = 1.6 nM Bioactivity Info	TI LI LO TS
2	IC50 = 2.3 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C19H16ClF2N7	1
1	IC50 = 1.72 nM Bioactivity Info	TI LI LO TS
CP0125532 Compound Info	US8829010, 9 Show/Hide	C21H23N7	1
1	IC50 = 2 nM Bioactivity Info	TI LI LO TS
CP0477919 Compound Info	US8598155, 53 Show/Hide	C21H19F4N7O	1
1	IC50 = 2.01 nM Bioactivity Info	TI LI LO TS
CP0523499 Compound Info	1-(2,5-dichlorophenyl)-8-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C17H12Cl2N4O	1
1	IC50 = 3.31 nM Bioactivity Info	TI LI LO TS
CP0425174 Compound Info	US8829010, 33 Show/Hide	C22H23N7	1
1	IC50 = 3.4 nM Bioactivity Info	TI LI LO TS
CP0508422 Compound Info	US8829010, 17 Show/Hide	C23H26N8O2	1
1	IC50 = 3.6 nM Bioactivity Info	TI LI LO TS
CP0567196 Compound Info	US8829010, 7 Show/Hide	C24H30N8	1
1	IC50 = 4.9 nM Bioactivity Info	TI LI LO TS
CP0397671 Compound Info	8-chloro-1-(2,5-dichlorophenyl)-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C16H9Cl3N4	1
1	IC50 = 5.31 nM Bioactivity Info	TI LI LO TS
CP0459888 Compound Info	US8829010, 40 Show/Hide	C22H25N7O	1
1	IC50 = 5.8 nM Bioactivity Info	TI LI LO TS
CP0425177 Compound Info	3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C20H22N6O	1
1	IC50 = 7.1 nM Bioactivity Info	TI LI LO TS
CP0425176 Compound Info	3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methyl-4-pyrrolidin-1-ylpyrazolo[3,4-d]pyrimidine Show/Hide	C22H25N7	1
1	IC50 = 7.8 nM Bioactivity Info	TI LI LO TS
CP0325892 Compound Info	US8598155, 5 Show/Hide	C18H17ClN8	1
1	IC50 = 8.2 nM Bioactivity Info	TI LI LO TS
CP0455777 Compound Info	US8829010, 4 Show/Hide	C19H17F3N8	2
1	IC50 = 8.9 nM Bioactivity Info	TI LI LO TS
2	IC50 = 9 nM Bioactivity Info	TI LI LO TS
CP0479685 Compound Info	US8829010, 37 Show/Hide	C21H22N8	1
1	IC50 = 8.9 nM Bioactivity Info	TI LI LO TS
CP0465365 Compound Info	6-fluoro-1-(2-fluoro-5-methoxyphenyl)-8-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H14F2N4O2	1
1	IC50 = 9.3 nM Bioactivity Info	TI LI LO TS
CP0539078 Compound Info	3-[1-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C19H17F3N6O	1
1	IC50 = 9.7 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C16H13F3N8	1
1	IC50 = 11 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C19H17F3N8O	1
1	IC50 = 12 nM Bioactivity Info	TI LI LO TS
CP0539077 Compound Info	US8829010, 1 Show/Hide	C20H21N7	1
1	IC50 = 17.7 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C24H19F3N6O2	1
1	IC50 = 24.4 nM Bioactivity Info	TI LI LO TS
CP0459875 Compound Info	3-[1-methyl-5-(4-methylphenyl)pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C19H20N6O	1
1	IC50 = 27.7 nM Bioactivity Info	TI LI LO TS
CP0139294 Compound Info	1-(2-chlorophenyl)-6,8-dimethoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H15ClN4O2	1
1	IC50 = 30.3 nM Bioactivity Info	TI LI LO TS
CP0405134 Compound Info	6-fluoro-8-methoxy-1-(5-methoxypyridin-3-yl)-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C17H14FN5O2	1
1	IC50 = 39.4 nM Bioactivity Info	TI LI LO TS
CP0447308 Compound Info	4-[3-(4-methoxyphenoxy)azetidin-1-yl]-1-methyl-3-(2-methylpropyl)pyrazolo[3,4-d]pyrimidine Show/Hide	C20H25N5O2	1
1	IC50 = 66.6 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C19H17F3N8O2	1
1	IC50 = 72 nM Bioactivity Info	TI LI LO TS
CP0391296 Compound Info	6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-phenylmethoxyimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C24H21N5O2	1
1	IC50 = 80.6 nM Bioactivity Info	TI LI LO TS
CP0448768 Compound Info	3-[5-(4-methoxyphenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C19H20N6O2	1
1	IC50 = 108.5 nM Bioactivity Info	TI LI LO TS
CP0536918 Compound Info	5-propoxy-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C18H15F3N6O	1
1	IC50 = 115 nM Bioactivity Info	TI LI LO TS
CP0412958 Compound Info	4-(1,3-dihydroisoindol-2-yl)-1-methyl-3-(2-methylpropyl)pyrazolo[3,4-d]pyrimidine Show/Hide	C18H21N5	1
1	IC50 = 146.4 nM Bioactivity Info	TI LI LO TS
CP0425175 Compound Info	4-(azetidin-1-yl)-1-methyl-3-(1-methyl-5-phenylpyrazol-4-yl)pyrazolo[3,4-d]pyrimidine Show/Hide	C19H19N7	1
1	IC50 = 188.7 nM Bioactivity Info	TI LI LO TS
CP0075285 Compound Info	2-methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazine Show/Hide	C15H18N4O	1
1	IC50 = 239 nM Bioactivity Info	TI LI LO TS
CP0508405 Compound Info	3-[5-(4-fluorophenyl)-1-methylpyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C18H17FN6O	1
1	IC50 = 240.8 nM Bioactivity Info	TI LI LO TS
CP0508406 Compound Info	3-[5-(4-methylphenyl)-1H-pyrazol-4-yl]-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C18H18N6O	1
1	IC50 = 297.8 nM Bioactivity Info	TI LI LO TS
CP0139291 Compound Info	6-methoxy-3-methyl-1-(3-methylpyridin-4-yl)-8-(trifluoromethyl)imidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H14F3N5O	1
1	IC50 = 346.5 nM Bioactivity Info	TI LI LO TS
CP0425178 Compound Info	5-[2-(2-methoxyphenyl)ethoxy]-3-(2-methylpropyl)-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C18H22N4O2	1
1	IC50 = 389.6 nM Bioactivity Info	TI LI LO TS
CP0508421 Compound Info	4-[3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methylpyrazolo[3,4-d]pyrimidin-4-yl]morpholine Show/Hide	C22H25N7O	1
1	IC50 = 423 nM Bioactivity Info	TI LI LO TS
CP0558296 Compound Info	3-(1-methyl-5-phenylpyrazol-4-yl)-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C18H18N6O	1
1	IC50 = 566.1 nM Bioactivity Info	TI LI LO TS
CP0447309 Compound Info	4-(azetidin-1-yl)-3-[5-(5-cyclopropylpyrimidin-2-yl)-1-methylpyrazol-4-yl]-1-methylpyrazolo[3,4-d]pyrimidine Show/Hide	C20H21N9	1
1	IC50 = 1012.7 nM Bioactivity Info	TI LI LO TS
CP0301299 Compound Info	8-fluoro-1-(3-fluoro-2-methylphenyl)-6-methoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H14F2N4O	1
1	IC50 = 1150 nM Bioactivity Info	TI LI LO TS
CP0454560 Compound Info	3-[5-(4-ethylphenyl)-1-methylpyrazol-4-yl]-1-methyl-4-(4-methylpiperazin-1-yl)pyrazolo[3,4-d]pyrimidine Show/Hide	C23H28N8	1
1	IC50 = 1407 nM Bioactivity Info	TI LI LO TS
CP0548142 Compound Info	3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C15H9F3N6	1
1	IC50 = 2107.4 nM Bioactivity Info	TI LI LO TS
CP0558297 Compound Info	3-(2-methylpropyl)-5-propoxy-[1,2,4]triazolo[4,3-a]pyrazine Show/Hide	C12H18N4O	1
1	IC50 = 5323.8 nM Bioactivity Info	TI LI LO TS

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 Show/Hide	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 Show/Hide	C20H18F3N7	1
1	IC50 = 0.303 nM
CP0508501 Compound Info	US8598155, 8 Show/Hide	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 Show/Hide	C20H17F4N7	1
1	IC50 = 0.633 nM
CP0346271 Compound Info	US8598155, 36 Show/Hide	C20H20FN7O	1
1	IC50 = 0.825 nM
CP0109700 Compound Info	US11419874, PF-05180999 Show/Hide	C19H17F3N8	2
1	IC50 = 1 nM
2	IC50 = 1.61 nM
CP0365601 Compound Info	US8598155, 55 Show/Hide	C20H19F2N7O	1
1	IC50 = 1.08 nM
CP0118848 Compound Info	US11419874, Example 15 Show/Hide	C20H18F3N7	1
1	IC50 = 1.6 nM
CP0125532 Compound Info	US8829010, 9 Show/Hide	C21H23N7	1
1	IC50 = 2 nM
CP0477919 Compound Info	US8598155, 53 Show/Hide	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 Show/Hide	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 Show/Hide	C16H12ClN5O	2
1	IC50 = 4 nM
2	IC50 = 4.3 nM
CP0325892 Compound Info	US8598155, 5 Show/Hide	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 Show/Hide	C24H28N6O2	1
1	IC50 = 10 nM
CP0225130 Compound Info	1-(2-chlorophenyl)-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline Show/Hide	C16H11ClN4	1
1	IC50 = 21 nM
CP0139294 Compound Info	1-(2-chlorophenyl)-6,8-dimethoxy-3-methylimidazo[5,1-c][1,2,4]benzotriazine Show/Hide	C18H15ClN4O2	1
1	IC50 = 30.3 nM
CP0147040 Compound Info	US11419874, Example 28 Show/Hide	C15H10ClN5	1
1	IC50 = 69 nM
CP0075285 Compound Info	2-methoxy-6,7-dimethyl-9-propylimidazo[1,5-a]pyrido[3,2-e]pyrazine Show/Hide	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 Show/Hide	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 Show/Hide	C18H14F2N4O	1
1	IC50 = 1150 nM
CP0059743 Compound Info	1-methyl-3-(2-methylpropyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione Show/Hide	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 Show/Hide	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 Show/Hide	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

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han