Target Validation Information
TTD ID	T87024
Target Name	Amyloid beta A4 protein (APP)
Type of Target	Successful
Drug Potency against Target	1,6-bis(4'-aminophenyl)-hexa-1,3,5-triene	Drug Info	Ki = 9 nM	[5]
	1,6-bis(4'-dimethylaminophenyl)-hexa-1,3,5-triene	Drug Info	Ki = 837 nM	[5]
	1,6-Bis(4'-hydroxyphenyl)-hexa-1,3,5-triene	Drug Info	Ki = 9 nM	[5]
	1,6-bis(4'-methylaminophenyl)-hexa-1,3,5-triene	Drug Info	Ki = 7.5 nM	[5]
	1,6-bis(4'-nitrophenyl)-hexa-1,3,5-triene	Drug Info	Ki = 500 nM	[5]
	2,5-bis(2-methoxyphenyl)thiophene	Drug Info	Ki = 625 nM	[2]
	2,5-bis(4-Hydroxyphenyl)thiophene	Drug Info	Ki = 4 nM	[2]
	2,5-bis(4-methoxyphenyl)thiophene	Drug Info	Ki = 108 nM	[2]
	2,5-bis(4-nitrophenyl)thiophene	Drug Info	Ki = 185 nM	[2]
	2-(4-(methylamino)phenyl)benzo[d]thiazol-6-ol	Drug Info	Ki = 2.8 nM	[5]
	2-(4-nitrophenyl)-5-(4-methoxyphenyl)thiophene	Drug Info	Ki = 18.5 nM	[2]
	4-(5-(4-(methylamino)phenyl)thiophen-2-yl)phenol	Drug Info	Ki = 31.2 nM	[2]
	4-(5-(4-aminophenyl)thiophen-2-yl)benzenamine	Drug Info	Ki = 6.1 nM	[2]
	4-(5-(4-aminophenyl)thiophen-2-yl)phenol	Drug Info	Ki = 9.6 nM	[2]
	4-(5-(4-methoxyphenyl)thiophen-2-yl)benzenamine	Drug Info	Ki = 5.6 nM	[2]
	4-(5-(4-methoxyphenyl)thiophen-2-yl)phenol	Drug Info	Ki = 6.1 nM	[2]
	5-hydroxy-2-(4-aminophenyl)benzofuran	Drug Info	Ki = 11.5 nM	[4]
	5-hydroxy-2-(4-dimethylaminophenyl)benzofuran	Drug Info	Ki = 2.8 nM	[4]
	5-hydroxy-2-(4-methylaminophenyl)benzofuran	Drug Info	Ki = 0.7 nM	[4]
	5-methoxy-2-(4-aminophenyl)benzofuran	Drug Info	Ki = 2.3 nM	[4]
	5-methoxy-2-(4-dimethylaminophenyl)benzofuran	Drug Info	Ki = 12 nM	[4]
	5-methoxy-2-(4-methylaminophenyl)benzofuran	Drug Info	Ki = 1.3 nM	[4]
	6-iodo-4'-dimethyaminoflavone	Drug Info	Ki = 15.6 nM	[1]
	6-iodo-4'-hydroxyflavone	Drug Info	Ki = 77.2 nM	[1]
	6-iodo-4'-methoxyflavone	Drug Info	Ki = 38.3 nM	[1]
	6-iodo-4'-methylaminoflavone	Drug Info	Ki = 30 nM	[1]
	Chrysamine -G	Drug Info	Ki = 0.16 nM	[6]
	Curcumin	Drug Info	Ki = 0.208 nM	[6]
	DEHYDROZINGERONE	Drug Info	Ki = 54.24 nM	[6]
	SB-13	Drug Info	Ki = 1.2 nM	[5]
	SR-973	Drug Info	IC50 = 200 nM	[3]
Action against Disease Model	Gantenerumab	Drug Info	In the new study, led by Gen He, a research associate in Greengard's lab, the researchers showed that GSAP stimulates production of beta-amyloid in cell lines, and that reducingGSAP reduces beta-amyloid.
References
REF 1	Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain. J Med Chem. 2005 Nov 17;48(23):7253-60.
REF 2	Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2.
REF 3	Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63.
REF 4	Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains. J Med Chem. 2006 May 4;49(9):2725-30.
REF 5	Synthesis of biphenyltrienes as probes for beta-amyloid plaques. J Med Chem. 2006 May 4;49(9):2841-4.
REF 6	Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging. J Med Chem. 2006 Oct 5;49(20):6111-9.

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