Target Validation Information
TTD ID	T79798
Target Name	MAP kinase p38 (MAPK12)
Type of Target	Successful
Drug Potency against Target		Drug Info	IC50 = 0.1 nM	[6]
	Talmapimod	Drug Info	IC50 = 9 nM	[8]
	VX-745	Drug Info	IC50 = 0.8 nM	[7]
	ML-3163	Drug Info	IC50 = 880 nM	[1]
	ML-3375	Drug Info	IC50 = 1200 nM	[3]
	ML-3403	Drug Info	IC50 = 990 nM	[3]
	RWJ-68354	Drug Info	IC50 = 7 nM	[2]
	SB 235699	Drug Info	IC50 = 71 nM	[4]
Action against Disease Model	VX-745	Drug Info	VX-745 induces modest growth inhibition of MM.1S, RPMI8226, and U266 cell lines in a dose-dependent fashion, with inhibitory concentration of 50% (IC50) of 10 M as assessed by MTT assay.	[5]
References
REF 1	From imidazoles to pyrimidines: new inhibitors of cytokine release. J Med Chem. 2002 Jun 20;45(13):2733-40.
REF 2	Imidazopyrimidines, potent inhibitors of p38 MAP kinase. Bioorg Med Chem Lett. 2003 Feb 10;13(3):347-50.
REF 3	Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J Med Chem. 2003 Jul 17;46(15):3230-44.
REF 4	Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity. J Med Chem. 2003 Dec 18;46(26):5651-62.
REF 5	Targeting p38 MAPK inhibits multiple myeloma cell growth in the bone marrow milieu. Blood. 2003 Jan 15;101(2):703-5.
REF 6	A small molecule-kinase interaction map for clinical kinase inhibitors. Nat Biotechnol. 2005 Mar;23(3):329-36.
REF 7	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 8	Successful structure-based design of recent p38 MAP kinase inhibitors. Curr Top Med Chem. 2009;9(7):655-76.

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