Target Validation Information
TTD ID	T47107
Target Name	Protein kinase C gamma (PRKCG)
Type of Target	Successful
Drug Potency against Target	Midostaurin	Drug Info	IC50 = 10 nM	[9]
		Drug Info	IC50 = 3 nM	[2]
	(-)-Cercosporamide	Drug Info	IC50 = 5800 nM	[7]
	8-Octyl-benzolactam-V9	Drug Info	Ki = 5200 nM	[4]
	BALANOL	Drug Info	IC50 = 30 nM
	Bisindolylmaleimide-I	Drug Info	IC50 = 30 nM	[6]
	LY-317644	Drug Info	IC50 = 6400 nM
	LY-326449	Drug Info	IC50 = 630 nM	[8]
	Monoctanoin component C	Drug Info	Ki = 2930 nM
	PROSTRATIN	Drug Info	Ki = 12.5 nM	[3]
	RO-316233	Drug Info	IC50 = 550 nM	[5]
	Ro-32-0557	Drug Info	IC50 = 5.4 nM
	RO-320432	Drug Info	IC50 = 36.5 nM
	[2,2':5',2'']Terthiophen-4-yl-methanol	Drug Info	IC50 = 3000 nM	[1]
	[2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde	Drug Info	IC50 = 700 nM	[1]
	[2,2':5',2'']Terthiophene-4-carbaldehyde	Drug Info	IC50 = 5000 nM	[1]
Action against Disease Model	Midostaurin	Drug Info	The effect of midostaurin on IgE-dependent mediator release in normal h uMan blood basophils and cultured cord blood cell-derived MC, and on spontaneous histamine secretion in the MC leukaemia cell line HMC-1 and the basophil cell line KU812 were studied. The effects of midostaurin on histamine release were dose-dependent and occurred at pharmacologic concentrations (IC(50) 10-100 nm). Midostaurin was also found to inhibit the IgE-dependent up-regulation of CD63 on cultured cord blood cell-derived h uMan MC, but did not inhibit IgE-dependent up-regulation of CD63 or CD203c in h uMan blood basophils.	[10]
References
REF 1	Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.
REF 2	Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 3	A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1. J Med Chem. 1992 May 29;35(11):1978-86.
REF 4	Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta. J Med Chem. 2006 May 4;49(9):2681-8.
REF 5	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 6	Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.
REF 7	(-)-Cercosporamide derivatives as novel antihyperglycemic agents. Bioorg Med Chem Lett. 2009 Feb 1;19(3):724-6.
REF 8	(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71.
REF 9	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 10	Midostaurin (PKC412) inhibits immunoglobulin E-dependent activation and mediator release in human blood basophils and mast cells. Clin Exp Allergy. 2009 Nov;39(11):1711-20.

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