| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T16514 | ||||
| Target Name | Fatty acid synthase | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Cerulenin | Drug Info | IC50 = 1 mol | [1] | |
| 2-Hexadecynoic acid | Drug Info | Ki = 4800 nM | [2] | ||
| BIOCHANIN | Drug Info | IC50 = 8000 nM | [3] | ||
| (-)-CATECHINGALLATE | Drug Info | Ki = 2800 nM | [3] | ||
| GALLOCATECHIN GALLATE | Drug Info | IC50 = 600 nM | [3] | ||
| 4-hydroxy-8-nitro-3-phenylquinolin-2(1H)-one | Drug Info | IC50 = 3000 nM | [4] | ||
| 4-hydroxy-6-nitro-3-phenylquinolin-2(1H)-one | Drug Info | IC50 = 550 nM | [4] | ||
| EPIGALOCATECHIN GALLATE | Drug Info | IC50 = 400 nM | [3] | ||
| MORIN | Drug Info | IC50 = 8000 nM | [3] | ||
| FISETIN | Drug Info | IC50 = 2000 nM | [3] | ||
| References | |||||
| REF 1 | Binding site of cerulenin in fatty acid synthetase. J Biochem. 1989 May;105(5):751-5. | ||||
| REF 2 | Bioorg Med Chem. 2010 Nov 1;18(21):7475-85. Epub 2010 Sep 18.2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections. | ||||
| REF 3 | J Med Chem. 2006 Jun 1;49(11):3345-53.Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. | ||||
| REF 4 | Bioorg Med Chem Lett. 2006 Sep 1;16(17):4620-3. Epub 2006 Jun 19.3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors. | ||||
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