Co-Target(s) Information

Target General Information

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Target ID

T07663

Target Info

Target Name

Phosphodiesterase 5A (PDE5A)

Synonyms

cGMP-specific 3',5'-cyclic phosphodiesterase; PDE5A; CGMP-binding cGMP-specific phosphodiesterase; CGB-PDE

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Target Type

Successful Target

Gene Name

PDE5A

Biochemical Class

Phosphoric diester hydrolase

UniProt ID

PDE5A_HUMAN

Co-Targets of This Target

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Co-Target Name

Phosphodiesterase 4 (PDE4)

Successful Target

UniProt ID

PDE4A_HUMAN; PDE4B_HUMAN; PDE4C_HUMAN; PDE4D_HUMAN

Gene Name

NO-GeName

Synonyms

PDE-4

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Representative Drug(s)

ROLIPRAM

Drug Info

Ki = 1.6 nM

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[1]

Dipyridamole

Drug Info

IC50 = 500 nM

[12]

Drug Info

IC50 ~ 500 nM

[11]

Co-Target Name

Phosphodiesterase 4A (PDE4A)

Successful Target

UniProt ID

PDE4A_HUMAN

Gene Name

PDE4A

Synonyms

cAMP-specific 3',5'-cyclic phosphodiesterase 4A; Type 4A cAMP phosphodiesterase; PDE46; DPDE2

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Representative Drug(s)

ROLIPRAM

Drug Info

IC50 = 4 nM

[2]

Co-Target Name

Solute carrier family 29 member 1 (SLC29A1)

Successful Target

UniProt ID

S29A1_HUMAN

Gene Name

SLC29A1

Synonyms

SLC29A1; Nucleoside transporter, es-type; Nucleoside transporter 1; Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter; Equilibrative NBMPR-sensitive nucleoside transporter; ENT1

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Representative Drug(s)

Dipyridamole

Drug Info

Ki = 8.18 nM

[3]

Co-Target Name

Phosphodiesterase 4D (PDE4D)

Successful Target

UniProt ID

PDE4D_HUMAN

Gene Name

PDE4D

Synonyms

cAMP-specific 3',5'-cyclic phosphodiesterase 4D; PDE43; DPDE3

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Representative Drug(s)

ROLIPRAM

Drug Info

IC50 = 31.6 nM

[4]

Co-Target Name

Adenosine A2a receptor (ADORA2A)

Successful Target

UniProt ID

AA2AR_HUMAN

Gene Name

ADORA2A

Synonyms

Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor

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Representative Drug(s)

Drug Info

Ki = 199.53 nM

[5]

Co-Target Name

Tumor necrosis factor (TNF)

Successful Target

UniProt ID

TNFA_HUMAN

Gene Name

TNF

Synonyms

Tumour necrosis factor alpha; Tumour necrosis factor; Tumor necrosis factor ligand superfamily member 2; TNFalpha; TNFSF2; TNFA; TNF-alpha; TNF-a; TNF alpha; Cachectin

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Representative Drug(s)

ROLIPRAM

Drug Info

IC50 = 200 nM

[6]

Co-Target Name

Human immunodeficiency virus Reverse transcriptase (HIV RT)

Successful Target

UniProt ID

POL_HV1B1

Gene Name

HIV RT

Synonyms

HIV p66 RT; HIV Exoribonuclease H

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Representative Drug(s)

Papaverine

Drug Info

IC50 < 200 ug.mL-1

[7]

Co-Target Name

Phosphodiesterase 1 (PDE1)

Successful Target

UniProt ID

PDE1A_HUMAN; PDE1B_HUMAN; PDE1C_HUMAN

Gene Name

NO-GeName

Synonyms

PDE-I; Cam-PDE 1

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Representative Drug(s)

Vardenafil

Drug Info

IC50 = 230 nM

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[8]

Drug Info

IC50 = 270 nM

[9]

Co-Target Name

Phosphodiesterase 3A (PDE3A)

Successful Target

UniProt ID

PDE3A_HUMAN

Gene Name

PDE3A

Synonyms

cGMP-inhibited 3',5'-cyclic phosphodiesterase A; Phosphodiesterase 3A; Cyclic GMP-inhibited phosphodiesterase A; Cyclic GMP inhibited phosphodiesterase A; CGI-PDE A

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Representative Drug(s)

Papaverine

Drug Info

Ki = 279 nM

[10]

Co-Target Name

Phosphodiesterase 3 (PDE3)

Successful Target

UniProt ID

PDE3A_HUMAN; PDE3B_HUMAN

Gene Name

NO-GeName

Synonyms

Phosphodiesterase III; PDE3; Cyclic GMP inhibited phosphodiesterase; Cyclic AMP phosphodiesterase III; CGI-PDE; CAMP phosphodiesterase III

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Representative Drug(s)

Drug Info

IC50 ~ 500 nM

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[11]

Vardenafil

Drug Info

IC50 = 580 nM

[13]

Co-Target Name

Phosphodiesterase 10A (PDE10)

Clinical trial Target

UniProt ID

PDE10_HUMAN

Gene Name

PDE10A

Synonyms

cAMP and cAMPinhibited cGMP 3',5'cyclic phosphodiesterase 10A; cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A

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Representative Drug(s)

Papaverine

Drug Info

IC50 = 17 nM

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[14]

Vardenafil

Drug Info

IC50 = 790 nM

[8]

Dipyridamole

Drug Info

Ki = 1000 nM

[16]

Co-Target Name

Phosphodiesterase 4B (PDE4B)

Clinical trial Target

UniProt ID

PDE4B_HUMAN

Gene Name

PDE4B

Synonyms

cAMP-specific 3',5'-cyclic phosphodiesterase 4B; Type 4B cAMP phosphodiesterase; Type 4 cyclic adenosine monophosphate phosphodiesterase (type 4 PDE); PDE32; DPDE4

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Representative Drug(s)

ROLIPRAM

Drug Info

IC50 = 20 nM

[15]

Co-Target Name

Phosphodiesterase 9 (PDE9)

Clinical trial Target

UniProt ID

PDE9A_HUMAN

Gene Name

PDE9A

Synonyms

High affinity cGMPspecific 3',5'cyclic phosphodiesterase 9A; High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A

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Representative Drug(s)

Vardenafil

Drug Info

IC50 = 460 nM

[8]

Co-Target Name

Phosphodiesterase 4C (PDE4C)

Patented-recorded Target

UniProt ID

PDE4C_HUMAN

Gene Name

PDE4C

Synonyms

cAMP-specific 3',5'-cyclic phosphodiesterase 4C; PDE21; DPDE1

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Representative Drug(s)

ROLIPRAM

Drug Info

IC50 = 118 nM

[17]

Co-Target Name

Phosphodiesterase 3B (PDE3B)

Patented-recorded Target

UniProt ID

PDE3B_HUMAN

Gene Name

PDE3B

Synonyms

cGMPinhibited 3',5'cyclic phosphodiesterase B; cGMP-inhibited 3',5'-cyclic phosphodiesterase B; Cyclic GMPinhibited phosphodiesterase B; Cyclic GMP-inhibited phosphodiesterase B; CGIPDE1; CGIPDE B; CGIP1; CGI-PDE B

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Representative Drug(s)

Papaverine

Drug Info

Ki = 417 nM

[10]

Co-Target Name

Phosphodiesterase 7A (PDE7A)

Discontinued Target

UniProt ID

PDE7A_HUMAN

Gene Name

PDE7A

Synonyms

TM22; High affinity cAMPspecific 3',5'cyclic phosphodiesterase 7A; High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A

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Representative Drug(s)

Dipyridamole

Drug Info

Ki = 600 nM

[16]

Co-Target Name

Phosphodiesterase 7B (PDE7B)

Discontinued Target

UniProt ID

PDE7B_HUMAN

Gene Name

PDE7B

Synonyms

cAMPspecific 3',5'cyclic phosphodiesterase 7B; cAMP-specific 3',5'-cyclic phosphodiesterase 7B

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Representative Drug(s)

Dipyridamole

Drug Info

Ki = 600 nM

[16]

Co-Target Name

Phosphodiesterase 11A (PDE11A)

Literature-reported Target

UniProt ID

PDE11_HUMAN

Gene Name

PDE11A

Synonyms

cAMP and cGMP phosphodiesterase 11A; Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A

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Representative Drug(s)

Tadalafil

Drug Info

IC50 = 10 nM

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[13]

Vardenafil

Drug Info

IC50 = 130 nM

[8]

Dipyridamole

Drug Info

Ki = 400 nM

[16]

Co-Target Name

Phosphodiesterase 1A (PDE1A)

Literature-reported Target

UniProt ID

PDE1A_HUMAN

Gene Name

PDE1A

Synonyms

hCam-1; Cam-PDE 1A; Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A; 61 kDa Cam-PDE

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Representative Drug(s)

Drug Info

IC50 = 600 nM

[18]

Co-Target Name

Phosphodiesterase 6 (PDE6)

Co-Target

UniProt ID

PDE6A_HUMAN; PDE6B_HUMAN; PDE6C_HUMAN; PDE6D_HUMAN; CNCG_HUMAN; CNRG_HUMAN

Gene Name

PDE6A; PDE6B; PDE6C; PDE6D; PDE6H; PDE6G

Synonyms

PDE6

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Representative Drug(s)

Drug Info

IC50 = 0.5 nM

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[13]

Vardenafil

Drug Info

IC50 = 1 nM

[8]

Dipyridamole

Drug Info

Ki = 125 nM

[16]

Tadalafil

Drug Info

IC50 = 980 nM

[8]

Co-Target Name

Phosphodiesterase 6C (PDE6C)

Co-Target

UniProt ID

PDE6C_HUMAN

Gene Name

PDE6C

Synonyms

Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'; cGMP phosphodiesterase 6C

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Representative Drug(s)

Drug Info

IC50 = 24 nM

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[18]

Tadalafil

Drug Info

IC50 = 402 nM

[19]

Co-Target Name

Protein prune homolog (PRUNE1)

Co-Target

UniProt ID

PRUN1_HUMAN

Gene Name

PRUNE1

Synonyms

Exopolyphosphatase PRUNE1; Drosophila-related expressed sequence 17; DRES-17; DRES17; HTcD37; Protein prune homolog 1; hPrune

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Representative Drug(s)

Dipyridamole

Drug Info

IC50 = 780 nM

[20]

References

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REF 1

The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2235-8.

REF 2

Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl... J Med Chem. 2000 Oct 19;43(21):3820-3.

REF 3

Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibit... J Med Chem. 2007 Aug 9;50(16):3906-20.

REF 4

Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4. J Med Chem. 1998 Jan 29;41(3):266-70.

REF 5

A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. J Med Chem. 2012 Jun 14;55(11):5311-25.

REF 6

Synthesis and in vitro evaluations of 6-(hetero)-aryl-imidazo[1,2-b]pyridazine-3-sulfonamide's as an inhibitor of TNF-alpha production. Bioorg Med Chem Lett. 2018 Jan 1;28(1):24-30.

REF 7

Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. J Nat Prod. 1991 Jan-Feb;54(1):143-54.

REF 8

Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED. Bioorg Med Chem Lett. 2005 May 2;15(9):2365-9.

REF 9

1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2341-5.

REF 10

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. J Med Chem. 2007 Jan 25;50(2):182-5.

REF 11

Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors. Bioorg Med Chem Lett. 2002 Mar 25;12(6):865-8.

REF 12

2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors. Bioorg Med Chem Lett. 1998 Oct 6;8(19):2737-42.

REF 13

Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease. Eur J Med Chem. 2013 Feb;60:285-94.

REF 14

Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors. Bioorg Med Chem. 2011 Jan 1;19(1):642-9.

REF 15

Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. J Med Chem. 2008 Sep 25;51(18):5471-89.

REF 16

The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. J Med Chem. 2005 May 19;48(10):3449-62.

REF 17

Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings. Eur J Med Chem. 2016 Nov 29;124:372-379.

REF 18

Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5. Bioorg Med Chem. 2015 May 1;23(9):2121-8.

REF 19

Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2019 May 23;62(10):4979-4990.

REF 20

Novel pyrimidopyrimidine derivatives for inhibition of cellular proliferation and motility induced by h-prune in breast cancer. Eur J Med Chem. 2012 Nov;57:41-50.

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