Target Validation Information
TTD ID	T40097
Target Name	Stress-activated protein kinase JNK1 (JNK1)
Type of Target	Clinical trial
Drug Potency against Target	AM-111	Drug Info	IC50 < 500 nM	[7]
	CC-401	Drug Info	IC50 = 10000 nM	[5]
	2-(2-(butylamino)pyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 2600 nM	[3]
	2-(2-(pentyloxy)pyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 1100 nM	[3]
	2-(2-(phenylamino)pyrimidin-4-ylamino)benzamide	Drug Info	IC50 = 590 nM	[3]
	2-(2-butoxypyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 1900 nM	[3]
	2-(2-phenoxypyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 300 nM	[3]
	2-(2-propoxypyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 2300 nM	[3]
	2-(2-sec-butoxypyrimidin-4-ylamino)benzoic acid	Drug Info	IC50 = 700 nM	[3]
	AS-601245	Drug Info	IC50 = 2600 nM	[4]
	N-(4-amino-5-cyano-6-ethoxypyridin-2-yl)acetamide	Drug Info	IC50 = 840 nM	[2]
	N-(4-amino-5-cyano-6-phenylpyridin-2-yl)acetamide	Drug Info	Ki = 1900 nM	[1]
	N-(4-amino-6-butoxy-5-cyanopyridin-2-yl)acetamide	Drug Info	IC50 = 2100 nM	[1]
	N-(6-ethoxypyridin-2-yl)acetamide	Drug Info	IC50 = 750 nM	[1]
	NM-PP1	Drug Info	IC50 = 140 nM	[4]
Action against Disease Model	AM-111	Drug Info	AM-111 blocked JNK mediated phosphorylation and activation of transcription factors c-Jun and c-Fos. AM-111 has been shown to prevent loss of hearing using a guinea pig model inthe setting of systemic aminoglycoside administration as well as in the setting of acute acoustic tra uMa. Hearing preservation has also been noted with AM-111 when given after exposure to impulse noise tra uMa in chinchillas.	[6]
References
REF 1	Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. J Med Chem. 2006 Jun 15;49(12):3563-80.
REF 2	Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors. J Med Chem. 2006 Jul 27;49(15):4455-8.
REF 3	Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72.
REF 4	The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
REF 5	Inhibitors of c-Jun N-terminal kinases: JuNK no more Biochim Biophys Acta. 2008 Jan;1784(1):76-93.
REF 6	AM-111 prevents hearing loss from semicircular canal injury in otitis media. Laryngoscope. 2010 Jan;120(1):178-82.
REF 7	c-Jun N-terminal kinase (JNK) signaling: recent advances and challenges. Biochim Biophys Acta. 2010 Mar;1804(3):463-75.

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