Target Validation Information
TTD ID T74952
Target Name cAMP protein kinase type II-beta (PRKAR2B)
Type of Target
Literature-reported
Drug Potency against Target 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]
BALANOL Drug Info Ki = 4.7 nM [3]
Ro-4396686 Drug Info IC50 = 9010 nM [4]
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 Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address;
REF 4 Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.

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