Co-Target(s) Information
| Target General Information | Top | ||||
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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 | |||||
| Co-Targets of This Target | Top | |||||
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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 | Click to Show More | [1] | |
| 2 | Dipyridamole | Drug Info | IC50 = 500 nM | [12] | ||
| 3 | Rhucin | 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) | Rhucin | 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 | Click to Show More | [8] | |
| 2 | Rhucin | 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) | Rhucin | Drug Info | IC50 ~ 500 nM | Click to Show More | [11] | |
| 2 | 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 | Click to Show More | [14] | |
| 2 | Vardenafil | Drug Info | IC50 = 790 nM | [8] | ||
| 3 | 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 | Click to Show More | [13] | |
| 2 | Vardenafil | Drug Info | IC50 = 130 nM | [8] | ||
| 3 | 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) | Rhucin | 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) | Rhucin | Drug Info | IC50 = 0.5 nM | Click to Show More | [13] | |
| 2 | Vardenafil | Drug Info | IC50 = 1 nM | [8] | ||
| 3 | Dipyridamole | Drug Info | Ki = 125 nM | [16] | ||
| 4 | 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) | Rhucin | Drug Info | IC50 = 24 nM | Click to Show More | [18] | |
| 2 | 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 | Top | ||||
|---|---|---|---|---|---|
| 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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