Target Validation Information
TTD ID	T44861
Target Name	Protein kinase C delta (PRKCD)
Type of Target	Clinical trial
Drug Potency against Target		Drug Info	IC50 = 3 nM	[3]
	INDOLACTUM	Drug Info	Ki = 2.01 nM	[4]
	Ingenol-3-bezoate	Drug Info	Ki = 1.41 nM	[2]
	LY-317644	Drug Info	IC50 = 6400 nM
	LY-326449	Drug Info	IC50 = 630 nM	[8]
	Phorbol 12,13-butyrate	Drug Info	Ki = 19 nM	[7]
	PROSTRATIN	Drug Info	Ki = 12.5 nM	[5]
	RO-316233	Drug Info	IC50 = 550 nM	[6]
	Ro-32-0557	Drug Info	IC50 = 6.8 nM
	RO-320432	Drug Info	IC50 = 21 nM
	THYMELEATOXIN	Drug Info	Ki = 47.1 nM	[2]
	[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	KAI-9803	Drug Info	KAI-9803 reduced infarct size, enhanced early recovery of regional left ventricular contractility, and improved microvascular patency and function in animal models of acute myocardial infarction	[9]
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	Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method a... J Med Chem. 2001 May 24;44(11):1690-701.
REF 3	Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 4	Structural basis of RasGRP binding to high-affinity PKC ligands. J Med Chem. 2002 Feb 14;45(4):853-60.
REF 5	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 6	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 7	Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of ... J Med Chem. 2007 Jul 26;50(15):3465-81.
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	Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. Circulation. 2008 Feb 19;117(7):886-96.

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