Target Validation Information
Target ID T75596
Target Name Methionine aminopeptidase 2
Target Type
Clinical Trial
Drug Potency against Target 5-chloro-2-(pyridin-2-yl)-1H-benzo[d]imidazole Drug Info IC50 = 18100 nM
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine Drug Info IC50 = 8000 nM
2-(pyridin-2-yl)-1H-benzo[d]imidazole Drug Info IC50 = 13300 nM
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 [527712]
3-anilino-5-benzylthio-1,2,4-triazole Drug Info Ki = 0.5 nM [528951]
2-(thiazol-4-yl)-1H-benzo[d]imidazol-5-amine Drug Info IC50 = 10100 nM
2-(pyridin-2-yl)-1H-benzo[d]imidazol-5-amine Drug Info IC50 = 9300 nM
OXYQUINOLINE Drug Info IC50 = 5600 nM
2-(4-fluorophenylsulfonamido)-1-naphthoic acid Drug Info IC50 = 15 nM [528149]
2-(phenylsulfonamido)-5-propylbenzoic acid Drug Info IC50 = 1100 nM [528149]
5-ethyl-2-(phenylsulfonamido)benzoic acid Drug Info IC50 = 90 nM [528149]
2-(phenylsulfonamido)-1-naphthoic acid Drug Info IC50 = 19 nM [528149]
5-methyl-2-(phenylsulfonamido)benzoic acid Drug Info IC50 = 1400 nM [528266]
5-bromo-2-(4-chlorophenylsulfonamido)benzoic acid Drug Info IC50 = 9100 nM [528149]
3,5-dimethyl-2-(phenylsulfonamido)benzoic acid Drug Info IC50 = 350 nM [528149]
5-butyl-2-(phenylsulfonamido)benzoic acid Drug Info IC50 = 10000 nM [528149]
References
Ref 527712J Med Chem. 2005 Sep 8;48(18):5644-7.4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Ref 528951J Med Chem. 2007 Aug 9;50(16):3777-85. Epub 2007 Jul 18.Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528266J Med Chem. 2006 Jun 29;49(13):3832-49.Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Ref 528149Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.

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