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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