Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T75596 | ||||
Target Name | Methionine aminopeptidase 2 (METAP2) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | 2-(4-fluorophenylsulfonamido)-1-naphthoic acid | Drug Info | IC50 = 15 nM | [2] | |
2-(phenylsulfonamido)-1-naphthoic acid | Drug Info | IC50 = 19 nM | [2] | ||
2-(phenylsulfonamido)-5-propylbenzoic acid | Drug Info | IC50 = 1100 nM | [2] | ||
2-(pyridin-2-yl)-1H-benzo[d]imidazol-5-amine | Drug Info | IC50 = 9300 nM | |||
2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | IC50 = 13300 nM | |||
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine | Drug Info | IC50 = 8000 nM | |||
2-(thiazol-4-yl)-1H-benzo[d]imidazol-5-amine | Drug Info | IC50 = 10100 nM | |||
3,5-dimethyl-2-(phenylsulfonamido)benzoic acid | Drug Info | IC50 = 350 nM | [2] | ||
3-anilino-5-benzylthio-1,2,4-triazole | Drug Info | Ki = 0.5 nM | [4] | ||
5-bromo-2-(4-chlorophenylsulfonamido)benzoic acid | Drug Info | IC50 = 9100 nM | [2] | ||
5-butyl-2-(phenylsulfonamido)benzoic acid | Drug Info | IC50 = 10000 nM | [2] | ||
5-chloro-2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | IC50 = 18100 nM | |||
5-ethyl-2-(phenylsulfonamido)benzoic acid | Drug Info | IC50 = 90 nM | [2] | ||
5-methyl-2-(phenylsulfonamido)benzoic acid | Drug Info | IC50 = 1400 nM | [3] | ||
5-methyl-2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | IC50 = 7700 nM | |||
5-p-Tolyl-1H-[1,2,3]triazole | Drug Info | IC50 = 10 nM | [1] | ||
OXYQUINOLINE | Drug Info | IC50 = 5600 nM | |||
References | |||||
REF 1 | 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. J Med Chem. 2005 Sep 8;48(18):5644-7. | ||||
REF 2 | Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. | ||||
REF 3 | Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of a... J Med Chem. 2006 Jun 29;49(13):3832-49. | ||||
REF 4 | Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. J Med Chem. 2007 Aug 9;50(16):3777-85. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.