Target Validation Information
TTD ID	T01851
Target Name	Integrin beta-1 (ITGB1)
Type of Target	Clinical trial
Drug Potency against Target	JSM 6427	Drug Info	IC50 = 0.55 nM	[5]
	R411	Drug Info	IC50 = 12 nM
	C(-GRGDfL-)	Drug Info	IC50 = 740 nM	[3]
	MK-0668	Drug Info	IC50 = 0.15 nM	[4]
	SB-265123	Drug Info	Ki = 18000 nM	[1]
	TR-14035	Drug Info	IC50 = 414 nM	[2]
Action against Disease Model	JSM 6427	Drug Info	JSM6427 provided a dose-dependent blockade of ARPE-19 cell adhesion to fibronectin (IC(50), 7.1 +/- 2.5 microM) and inhibition of migration (IC(50), 6.0 +/- 4.5 microM). In the rabbit model, intravitreal injection of JSM6427 provided significant inhibition of proliferation of retinal cells (M?1ller cells, microglia, and macrophages)	[6]
References
REF 1	Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.
REF 2	2,6-Quinolinyl derivatives as potent VLA-4 antagonists. Bioorg Med Chem Lett. 2007 Jan 1;17(1):142-6.
REF 3	Multiple N-methylation by a designed approach enhances receptor selectivity. J Med Chem. 2007 Nov 29;50(24):5878-81.
REF 4	Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalan... Bioorg Med Chem Lett. 2009 Oct 1;19(19):5803-6.
REF 5	Inhibition of inflammatory lymphangiogenesis by integrin alpha5 blockade. Am J Pathol. 2007 Jul;171(1):361-72.
REF 6	Assessment of the integrin alpha5beta1 antagonist JSM6427 in proliferative vitreoretinopathy using in vitro assays and a rabbit model of retinal detachment. Invest Ophthalmol Vis Sci. 2010 Feb;51(2):1028-35.

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