Target Validation Information
TTD ID T16514
Target Name Fatty acid synthase (FASN)
Type of Target
Successful
Drug Potency against Target Cerulenin Drug Info IC50 = 1 mol [4]
(-)-CATECHINGALLATE Drug Info Ki = 2800 nM [1]
2-Hexadecynoic acid Drug Info Ki = 4800 nM [3]
3,7,3',4'-TETRAHYDROXYFLAVONE Drug Info IC50 = 2000 nM [1]
4-hydroxy-6-nitro-3-phenylquinolin-2(1H)-one Drug Info IC50 = 550 nM [2]
4-hydroxy-8-nitro-3-phenylquinolin-2(1H)-one Drug Info IC50 = 3000 nM [2]
biochanin A Drug Info IC50 = 8000 nM [1]
Epigallocatechin gallate Drug Info IC50 = 400 nM [1]
GALLOCATECHIN GALLATE Drug Info IC50 = 600 nM [1]
MORIN Drug Info IC50 = 8000 nM [1]
References
REF 1 Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem. 2006 Jun 1;49(11):3345-53.
REF 2 3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3.
REF 3 2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. Bioorg Med Chem. 2010 Nov 1;18(21):7475-85.
REF 4 Binding site of cerulenin in fatty acid synthetase. J Biochem. 1989 May;105(5):751-5.

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