Target Validation Information
TTD ID T51565
Target Name Casein kinase II alpha (CSNK2A1)
Type of Target
Clinical trial
Drug Potency against Target 4,5,6,7-tetrabromo-1H-benzimidazole Drug Info IC50 = 1300 nM [3]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Drug Info IC50 = 900 nM [4]
5,6,8-trichloroquinoline-4-one-3-carboxylic acid Drug Info IC50 = 300 nM [2]
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole Drug Info IC50 = 13000 nM [4]
7,8-dichloroquinoline-4-one-3-carboxylic acid Drug Info IC50 = 800 nM [2]
AdoC(Dpr)2AlaArg6 Drug Info IC50 = 17000 nM [1]
APIGENIN Drug Info IC50 = 800 nM [4]
BALANOL Drug Info IC50 = 30 nM [5]
CGP-029482 Drug Info IC50 = 390 nM [4]
ELLAGIC ACID Drug Info IC50 = 40 nM [4]
EMODIN Drug Info IC50 = 2000 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 Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2. J Med Chem. 2006 Nov 2;49(22):6443-50.
REF 3 Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2. Bioorg Med Chem. 2009 Feb 15;17(4):1573-8.
REF 4 Structural insight into human CK2alpha in complex with the potent inhibitor ellagic acid. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2920-3.
REF 5 Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. J Med Chem. 1996 Dec 20;39(26):5215-27.

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