Target Validation Information
TTD ID	T08813
Target Name	cAMP-dependent protein kinase A type I (PRKAR1A)
Type of Target	Literature-reported
Drug Potency against Target	5-(2-methylpiperazin-1-ylsulfonyl)isoquinoline	Drug Info	Ki = 3000 nM	[4]
	AdcAhxArg4Lys(biotin)-PEG-OMe	Drug Info	IC50 = 1200 nM	[2]
	AdcAhxArg4Lys-PEGOMe	Drug Info	IC50 = 460 nM	[2]
	AdcAhxArg4NH(CH2)6NH2	Drug Info	IC50 = 680 nM	[2]
	AdcAhxArg6	Drug Info	IC50 = 700 nM	[2]
	AdoC(Ahx)Arg6	Drug Info	IC50 = 120 nM	[1]
	AdoC(Aoc)Arg6	Drug Info	IC50 = 240 nM	[1]
	AdoC(Aun)Arg6	Drug Info	IC50 = 330 nM	[1]
	AdoC(beta-Ala)2AlaArg6	Drug Info	IC50 = 4300 nM	[1]
	AdoC(beta-Ala)Arg6	Drug Info	IC50 = 1800 nM	[1]
	AdoC(betaAsp)2AlaArg6	Drug Info	IC50 = 11100 nM	[1]
	AdoC(Dpr)2AlaArg6	Drug Info	IC50 = 2600 nM	[1]
	AdoC(GABA)Arg6	Drug Info	IC50 = 1300 nM	[1]
	AdoCGlyArg6	Drug Info	IC50 = 4000 nM	[1]
	RO-316233	Drug Info	IC50 = 11800 nM	[3]
References
REF 1	Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases. Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.
REF 2	Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3035-9.
REF 3	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 4	Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and... J Biol Chem. 1996 Oct 18;271(42):26157-64.

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