General Information of the Protein
Protein ID
PT01479
Protein Name
3',5'-cyclic-AMP phosphodiesterase 4A
Secondarily
Protein Name
DPDE2
PDE46
cAMP-specific phosphodiesterase 4A
Gene Name
PDE4A
Secondarily
Gene Name
DPDE2
Sequence
MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQPHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGRSPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPFAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWCLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPSTAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Phosphodiesterase
>
Phosphodiesterase 4
>
Phosphodiesterase 4A
Function
Hydrolyzes the second messenger 3',5'-cyclic AMP (cAMP), which is a key regulator of many important physiological processes.
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Uniprot ID
Primary ID:
P27815

Secondarily ID:
O75522
O76092
Q16255
Q16691
Q5DM53
Q6PMT2
Q8IVA7
Q8WUQ3
Q9H3H2
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Ensembl ID
ENSG00000065989
HGNC ID
HGNC:8780
Subcellular Location
Cytoplasm
Perinuclear region
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: CL000006 , HEK293
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0500068
 Compound Info 
2-[(2-fluorophenyl)methoxy]-9,10-dimethoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C21H19FN2O4
  1
1
IC50 = 372 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0573421
 Compound Info 
2-(benzylamino)-9,10-dimethoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C21H21N3O3
  1
1
IC50 = 553 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0535032
 Compound Info 
9,10-dimethoxy-2-(2-pyridin-2-yloxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C21H21N3O5
  1
1
IC50 = 586 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0486535
 Compound Info 
2-[(3-fluoropyridin-2-yl)methoxy]-9,10-dimethoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C20H18FN3O4
  1
1
IC50 = 1088 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0532953
 Compound Info 
9,10-dimethoxy-2-(2-phenoxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C22H22N2O5
  1
1
IC50 = 2115 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0512709
 Compound Info 
9,10-dimethoxy-2-(oxolan-2-ylmethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C19H22N2O5
  1
1
IC50 = 2165 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0486534
 Compound Info 
2-[(2-fluorophenyl)methoxy]-9-methoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C20H17FN2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0511849
 Compound Info 
2-[(2-fluorophenyl)methoxy]-10-methoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C20H17FN2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0539843
 Compound Info 
2-[(3-fluoropyridin-2-yl)methoxy]-9-methoxy-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C19H16FN3O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0552896
 Compound Info 
2-[(2-fluorophenyl)methoxy]-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C19H15FN2O2
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0486533
 Compound Info 
9-methoxy-2-(2-phenoxyethoxy)-6,7-dihydropyrimido[6,1-a]isoquinolin-4-one
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C21H20N2O4
  1
1
IC50 > 10 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0035728
 Compound Info 
3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
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C17H14Cl2F2N2O3
  2
1 IC50 = 0.21 nM
2 IC50 = 0.59 nM
CP0046056
 Compound Info 
(S)-(+)-3-{2-[(3-Cyclopropyloxy-4-difluromethoxy)-phenyl]-2-[5-(2-(1-hydroxy-1-trifluoromethyl-2,2,2-trifluoro)ethyl)-thiazolyl]ethyl}pyridine N-Oxide
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C23H18F8N2O4S
  2
1 IC50 = 0.4 nM
2 Ki = 0.43 nM
CP0037308
 Compound Info 
(R,S)-Rolipram
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C16H21NO3
  8
1 IC50 = 0.770852 nM
2 IC50 = 10.7 nM
3 IC50 = 11 nM
4 IC50 = 67 nM
5 IC50 = 84 nM
6 IC50 = 162 nM
7 IC50 = 386 nM
8 IC50 = 830 nM
CP0036578
 Compound Info 
(E)-8-(3-(2-(3-methyl-1,2,4-oxadiazol-5-yl)-2-(4-(methylsulfonyl)phenyl)vinyl)phenyl)-6-(2-(methylsulfonyl)propan-2-yl)quinoline
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C31H29N3O5S2
  2
1 IC50 = 1 nM
2 IC50 = 1.4 nM
CP0171005
 Compound Info 
2-{4-[1-(3,4-Bis-difluoromethoxy-phenyl)-2-(3-methyl-1-oxy-pyridin-4-yl)-ethyl]-phenyl}-1,1,1,3,3,3-hexafluoro-propan-2-ol
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C25H19F10NO4
  1
1 IC50 = 1.3 nM
CP0166045
 Compound Info 
(R)-4-(2-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridine
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C25H27NO2
  3
1 IC50 = 2.1 nM
2 IC50 = 4 nM
3 IC50 = 4.2 nM
CP0044057
 Compound Info 
4-Oxo-1-[3-(1-oxy-pyridin-3-ylethynyl)-phenyl]-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid cyclopropylamide
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C25H18N4O3
  1
1 IC50 = 5.1 nM
CP0069130
 Compound Info 
(Ibudilast)1-(2-Isopropyl-pyrazolo[1,5-a]pyridin-3-yl)-2-methyl-propan-1-one
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C14H18N2O
  2
1 IC50 = 54 nM
2 IC50 = 1300 nM
CP0140806
 Compound Info 
2-[5-[(1R)-1-[3-cyclopropyloxy-4-(difluoromethoxy)phenyl]-2-(1-oxidopyridin-1-ium-3-yl)ethyl]-1,3-thiazol-2-yl]-1,1,1,3,3,3-hexafluoropropan-2-ol
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C23H18F8N2O4S
  1
1 IC50 = 56 nM
CP0057101
 Compound Info 
(1r,4r)-4-cyano-4-(3-(cyclopentyloxy)-4-methoxyphenyl)cyclohexanecarboxylic acid
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C20H25NO4
  2
1 IC50 = 150 nM
2 IC50 = 160 nM
Clinical Information about the Protein
Target 1 ( Phosphodiesterase 4A (PDE4A) )
Target Type Successful Target
Disease 11 Target-related Diseases  11
1 Acute bronchial asthma [ICD-11: CA23]
2 Asthma [ICD-11: CA23]
3 Cognitive impairment [ICD-11: 6D71]
4 Atopic dermatitis [ICD-11: EA80]
5 Crohn disease [ICD-11: DD70]
6 Psoriasis vulgaris [ICD-11: EA90]
7 Rheumatoid arthritis [ICD-11: FA20]
8 Chronic obstructive pulmonary disease [ICD-11: CA22]
9 Irritable bowel syndrome [ICD-11: DD91.0]
10 Multiple sclerosis [ICD-11: 8A40]
11 Peripheral vascular disease [ICD-11: BD4Z]
Approved Drug(s) 2 Approved Drugs  2
1 Dyphylline
 Drug Info 
Approved
Acute bronchial asthma
2 Enprofylline
 Drug Info 
Approved
Asthma
Clinical Trial Drug(s) 10 Clinical Trial Drugs  10
1 DENBUFYLLINE
 Drug Info 
Phase 3
Cognitive impairment
2 AN-2898
 Drug Info 
Phase 2
Atopic dermatitis
3 CC-1088
 Drug Info 
Phase 2
Crohn disease
4 HT-0712
 Drug Info 
Phase 2
Cognitive impairment
5 MK-0873
 Drug Info 
Phase 2
Psoriasis vulgaris
6 Oglemilast
 Drug Info 
Phase 2
Asthma
7 Piclamilast
 Drug Info 
Phase 2
Rheumatoid arthritis
8 TOFIMILAST
 Drug Info 
Phase 2
Chronic obstructive pulmonary disease
9 Tofisopam
 Drug Info 
Phase 2
Irritable bowel syndrome
10 Ronomilast
 Drug Info 
Phase 1
Chronic obstructive pulmonary disease
Discontinued Drug(s) 8 Discontinued Drugs  8
1 Cilomilast
 Drug Info 
Discontinued in Phase 3
Chronic obstructive pulmonary disease
2 CDP840
 Drug Info 
Discontinued in Phase 2
Chronic obstructive pulmonary disease
3 CI-1018
 Drug Info 
Discontinued in Phase 2
Asthma
4 Daxalipram
 Drug Info 
Discontinued in Phase 2
Multiple sclerosis
5 GSK256066
 Drug Info 
Discontinued in Phase 2
Asthma
6 YM-976
 Drug Info 
Discontinued in Phase 1
Asthma
7 GW-3600
 Drug Info 
Terminated
Asthma
8 Torbafylline
 Drug Info 
Terminated
Peripheral vascular disease