Target Information
Target General Infomation | |||||
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Target ID |
T87463
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Former ID |
TTDR00260
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Target Name |
Protein kinase A
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Gene Name |
ypkA
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Synonyms |
CAMP-dependent protein kinase; PKA; ypkA
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Target Type |
Discontinued
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BioChemical Class |
Kinase
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Target Validation |
T87463
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UniProt ID | |||||
EC Number |
EC 2.7.1.37
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Sequence |
MKIMGTMSPSISLAKAHERISKHWQNPVGELNIEGKRYRIIDNQVVRLNPHSGFSLFREG
VGKIFSGKMFSFSIARNLTDTLHAAQKTTSQELRSDIPNALSNLFGAKPQTELPLGWKGK PLSGAPDLEGMRVAETDKFAEGESHISIIETKDKQRLVAKIERSIAEGHLFAELEAYKHI YKTAGKHPNLANVHGMAVVPYGNRKEEALLMDEVDGWRCSDTLRSLADSWKQGKINSEAY WGTIKFIAHRLLDVTNHLAKAGIVHNDIKPGNVVFDRASGEPVVIDLGLHSRSGEQPKGF TESFKAPELGVGNLGASEKSDVFLVVSSLLHGIEGFEKDPEIKPNQGLRFITSEPAHVMD ENGYPIHRPGIAGVETAYTRFITDILGVSADSRPDSNEARLHEFLSDGTIDEESAKQILK DTLTGEMSPLPTDVRRITPKKLRELSDLLRTHLSSAATKQLDMGVVLSDLDTMLVALDKA EREGGVDKDQLKSFNSLILKTYSVIGAYIKGREGDTKSSSTEVSPYHRSNFMLSIVEPSL QRIQKHLDQTHSSDIGSLMRAHKHLETLLEVLVTLSQQGQPVTSETYSFLNRLAEAKVTL SQQLNTLQQQQESAKAQLSILINRSGSWADVARQSLLRFDSTRPVVKFGTEQYTAIHRQM MAAHAAITLQEVSEFTDDMRNFTADSIPLLIQLGRSSLMDEHLVEQREKLRELTTIAERL NRLEREWM |
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Drugs and Mode of Action | |||||
Inhibitor | 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol | Drug Info | [528490] | ||
BALANOL | Drug Info | [527710] | |||
BX-795 | Drug Info | [527484] | |||
BX-912 | Drug Info | [527484] | |||
chelerythrine | Drug Info | [529213] | |||
compound 1 | Drug Info | [530572] | |||
compound 1 | Drug Info | [532161] | |||
compound 33 | Drug Info | [530078] | |||
Ro-4396686 | Drug Info | [528018] | |||
Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPS) | Drug Info | [535638] | |||
Rp-cAMPS | Drug Info | [543459] | |||
Activator | N6 benzyl-cAMP | Drug Info | [526651] | ||
[3H]cAMP | Drug Info | [543459] | |||
References | |||||
Ref 526651 | cAMP analog mapping of Epac1 and cAMP kinase. Discriminating analogs demonstrate that Epac and cAMP kinase act synergistically to promote PC-12 cell neurite extension. J Biol Chem. 2003 Sep 12;278(37):35394-402. Epub 2003 Jun 20. | ||||
Ref 527484 | Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. Epub 2005 Mar 16. | ||||
Ref 527710 | J Med Chem. 2005 Sep 8;48(18):5613-38.Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. | ||||
Ref 528018 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. | ||||
Ref 528490 | J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. | ||||
Ref 529213 | Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. Epub 2007 Dec 11.A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. | ||||
Ref 530078 | Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51. | ||||
Ref 530572 | 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. | ||||
Ref 532161 | A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038. Epub 2012 Oct 22. |
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