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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