Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T24211 | Target Info | |||
| Target Name | C1 esterase inhibitor (SERPING1) | ||||
| Synonyms |
Serpin G1; SERPING1; Plasma protease C1 inhibitor; C1inhibiting factor; C1Inh; C1 Inh
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| Target Type | Successful Target | ||||
| Gene Name | SERPING1 | ||||
| Biochemical Class | Serpin protein | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Rhucin | Drug Info | IC50 = 1 nM | [1] | ||
| 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 | [2] | ||
| 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) | Rhucin | Drug Info | IC50 = 270 nM | [3] | ||
| 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 | [4] | ||
| 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) | Rhucin | Drug Info | IC50 ~ 500 nM | [4] | ||
| 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 | [5] | ||
| 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 | [6] | ||
| 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 | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model. Eur J Med Chem. 2019 Sep 1;177:269-290. | ||||
| REF 2 | 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 3 | 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 4 | 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 5 | Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5. Bioorg Med Chem. 2015 May 1;23(9):2121-8. | ||||
| REF 6 | 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. | ||||
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