Target Validation Information
Target ID T08813
Target Name CAMP-dependent protein kinase type I-alpha regulatory chain
Target Type
Research
Drug Potency against Target AdcAhxArg6 Drug Info IC50 = 700 nM [1]
AdoC(betaAsp)2AlaArg6 Drug Info IC50 = 11100 nM [2]
AdoC(GABA)Arg6 Drug Info IC50 = 1300 nM [2]
AdcAhxArg4Lys(biotin)-PEG-OMe Drug Info IC50 = 1200 nM [1]
AdoC(Aun)Arg6 Drug Info IC50 = 330 nM [2]
5-(2-methylpiperazin-1-ylsulfonyl)isoquinoline Drug Info Ki = 3000 nM [3]
RO-316233 Drug Info IC50 = 11800 nM [4]
AdoCGlyArg6 Drug Info IC50 = 4000 nM [2]
AdcAhxArg4Lys-PEGOMe Drug Info IC50 = 460 nM [1]
AdoC(beta-Ala)Arg6 Drug Info IC50 = 1800 nM [2]
AdoC(Dpr)2AlaArg6 Drug Info IC50 = 2600 nM [2]
AdoC(beta-Ala)2AlaArg6 Drug Info IC50 = 4300 nM [2]
AdoC(Aoc)Arg6 Drug Info IC50 = 240 nM [2]
AdcAhxArg4NH(CH2)6NH2 Drug Info IC50 = 680 nM [1]
AdoC(Ahx)Arg6 Drug Info IC50 = 120 nM [2]
References
REF 1Bioorg Med Chem Lett. 2003 Sep 15;13(18):3035-9.Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase.
REF 2Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.
REF 3J Biol Chem. 1996 Oct 18;271(42):26157-64.Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity.
REF 4J Med Chem. 1992 Jan;35(1):177-84.Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides.

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