Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T61744 | Target Info | |||
| Target Name | Phosphodiesterase 4A (PDE4A) | ||||
| Synonyms |
cAMP-specific 3',5'-cyclic phosphodiesterase 4A; Type 4A cAMP phosphodiesterase; PDE46; DPDE2
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| Target Type | Successful Target | ||||
| Gene Name | PDE4A | ||||
| Biochemical Class | Phosphoric diester hydrolase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Piclamilast | Drug Info | IC50 = 0.021 nM | Click to Show More | [1] | |
| 2 | MK-0873 | Drug Info | IC50 = 5.1 nM | [2] | ||
| 3 | TOFIMILAST | Drug Info | IC50 = 13 nM | [3] | ||
| 4 | ROLIPRAM | Drug Info | IC50 = 31.6 nM | [4] | ||
| 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 | [5] | ||
| Co-Target Name | Phosphodiesterase 5A (PDE5A) | Successful Target | ||||
| UniProt ID | PDE5A_HUMAN | |||||
| Gene Name | PDE5A | |||||
| Synonyms |
cGMP-specific 3',5'-cyclic phosphodiesterase; PDE5A; CGMP-binding cGMP-specific phosphodiesterase; CGB-PDE
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| Representative Drug(s) | ROLIPRAM | Drug Info | IC50 = 720 nM | [6] | ||
| 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) | Piclamilast | Drug Info | IC50 = 0.041 nM | Click to Show More | [1] | |
| 2 | MK-0873 | Drug Info | IC50 = 5.1 nM | [2] | ||
| 3 | TOFIMILAST | Drug Info | IC50 = 13 nM | [3] | ||
| 4 | ROLIPRAM | Drug Info | IC50 = 20 nM | [7] | ||
| 5 | AN-2898 | Drug Info | IC50 = 240 nM | [1] | ||
| 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) | Piclamilast | Drug Info | IC50 = 3.8 nM | Click to Show More | [4] | |
| 2 | TOFIMILAST | Drug Info | IC50 ~ 100 nM | [3] | ||
| 3 | ROLIPRAM | Drug Info | IC50 = 118 nM | [8] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design. J Med Chem. 2016 Aug 11;59(15):7029-65. | ||||
| REF 2 | Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6387-93. | ||||
| REF 3 | SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase. J Med Chem. 2007 Jan 25;50(2):344-9. | ||||
| 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 | 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 6 | Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. J Med Chem. 1994 Jun 24;37(13):2106-11. | ||||
| REF 7 | 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 8 | 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. | ||||
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