Target Validation Information
Target ID T87024
Target Name Amyloid beta A4 protein
Target Type
Successful
Drug Potency against Target 4-(5-(4-methoxyphenyl)thiophen-2-yl)phenol Drug Info Ki = 6.1 nM [527907]
5-methoxy-2-(4-dimethylaminophenyl)benzofuran Drug Info Ki = 12 nM [528159]
6-iodo-4'-dimethyaminoflavone Drug Info Ki = 15.6 nM [527855]
1,6-bis(4'-methylaminophenyl)-hexa-1,3,5-triene Drug Info Ki = 7.5 nM [528161]
2-(4-(methylamino)phenyl)benzo[d]thiazol-6-ol Drug Info Ki = 2.8 nM [528161]
DEHYDROZINGERONE Drug Info Ki = 54.24 nM [528454]
6-iodo-4'-methoxyflavone Drug Info Ki = 38.3 nM [527855]
6-iodo-4'-methylaminoflavone Drug Info Ki = 30 nM [527855]
Chrysamine -G Drug Info Ki = 0.16 nM [528454]
Curcumin Drug Info Ki = 0.208 nM [528454]
4-(5-(4-(methylamino)phenyl)thiophen-2-yl)phenol Drug Info Ki = 31.2 nM [527907]
2,5-bis(4-Hydroxyphenyl)thiophene Drug Info Ki = 4 nM [527907]
5-methoxy-2-(4-aminophenyl)benzofuran Drug Info Ki = 2.3 nM [528159]
5-hydroxy-2-(4-dimethylaminophenyl)benzofuran Drug Info Ki = 2.8 nM [528159]
6-iodo-4'-hydroxyflavone Drug Info Ki = 77.2 nM [527855]
2-(4-nitrophenyl)-5-(4-methoxyphenyl)thiophene Drug Info Ki = 18.5 nM [527907]
2,5-bis(4-methoxyphenyl)thiophene Drug Info Ki = 108 nM [527907]
4-(5-(4-methoxyphenyl)thiophen-2-yl)benzenamine Drug Info Ki = 5.6 nM [527907]
5-hydroxy-2-(4-methylaminophenyl)benzofuran Drug Info Ki = 0.7 nM [528159]
1,6-Bis(4'-hydroxyphenyl)-hexa-1,3,5-triene Drug Info Ki = 9 nM [528161]
2,5-bis(4-nitrophenyl)thiophene Drug Info Ki = 185 nM [527907]
SB-13 Drug Info Ki = 1.2 nM [528161]
1,6-bis(4'-dimethylaminophenyl)-hexa-1,3,5-triene Drug Info Ki = 837 nM [528161]
2,5-bis(2-methoxyphenyl)thiophene Drug Info Ki = 625 nM [527907]
5-methoxy-2-(4-methylaminophenyl)benzofuran Drug Info Ki = 1.3 nM [528159]
5-hydroxy-2-(4-aminophenyl)benzofuran Drug Info Ki = 11.5 nM [528159]
4-(5-(4-aminophenyl)thiophen-2-yl)phenol Drug Info Ki = 9.6 nM [527907]
1,6-bis(4'-aminophenyl)-hexa-1,3,5-triene Drug Info Ki = 9 nM [528161]
4-(5-(4-aminophenyl)thiophen-2-yl)benzenamine Drug Info Ki = 6.1 nM [527907]
1,6-bis(4'-nitrophenyl)-hexa-1,3,5-triene Drug Info Ki = 500 nM [528161]
SR-973 Drug Info IC50 = 200 nM [528025]
Action against Disease Model Gantenerumab 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. Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Amyloid precursor protein (APP) is involved in the pathogenesis of Alzheimer's disease (AD), but its role in cognition has been relatively little studied. APP knockout (KO) animals have been described previously and show deficits in grip strength, reduced locomotor activity and impaired learning and memory in a conditioned avoidance test and the Morris water-maze. In order to further investigate the in vivo function of APP and its proteolytic derivatives, we tested APP KO mice and age-matched wild type controls at two different ages, 3 and 8 months, in a range of behavioural tests measuring neuromuscular, locomotor and cognitive functions. These tests included the acquisition of a passive avoidance response as a measure of long-term memory of an aversive experience, and spontaneous alternation in a Y-maze, regarded as a measure of spatial short-term memory. The absence of APP expression in APP KO mice was confirmed at the protein level using hippocampal tissue inWestern blotting. APP KO mice displayed deficits in forelimb grip strength and locomotor activity in agreement with previous studies. In the Y-maze test used for spontaneous alternation behaviour, APP KO animals did not exhibit reduced alternation rates. On the other hand, in the passive avoidance test, APP KO mice showed an age-related deficit in retention of memory for an aversive experience. The results suggest that APP and/or its proteolytic derivatives may play a role in long-term memory in adult brain and/or may be required during the development and maintenance of neuronal networks involved in this type of memory.
References
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 527855J Med Chem. 2005 Nov 17;48(23):7253-60.Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 528454J Med Chem. 2006 Oct 5;49(20):6111-9.Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging.
Ref 527855J Med Chem. 2005 Nov 17;48(23):7253-60.Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
Ref 527855J Med Chem. 2005 Nov 17;48(23):7253-60.Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
Ref 528454J Med Chem. 2006 Oct 5;49(20):6111-9.Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging.
Ref 528454J Med Chem. 2006 Oct 5;49(20):6111-9.Curcumin and dehydrozingerone derivatives: synthesis, radiolabeling, and evaluation for beta-amyloid plaque imaging.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 527855J Med Chem. 2005 Nov 17;48(23):7253-60.Radioiodinated flavones for in vivo imaging of beta-amyloid plaques in the brain.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 528159J Med Chem. 2006 May 4;49(9):2725-30.Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 527907Bioorg Med Chem Lett. 2006 Mar 1;16(5):1350-2. Epub 2005 Dec 1.Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.
Ref 528161J Med Chem. 2006 May 4;49(9):2841-4.Synthesis of biphenyltrienes as probes for beta-amyloid plaques.
Ref 528025Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. Epub 2006 Feb 10.Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.

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