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(3E)-3-(furan-2-ylmethylidene)-5-(hydroxymethyl)-1-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-one
no activity at 0.1 mM
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
1-methoxy-5-(methoxymethyl)-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-one
no activity at 0.1 mM
1-phenyl-2,4-dithiobiuret
-
2-(5-methoxy-6-[2-methyl-3-((3-methylbut-2-en-1-yl)oxiran-2-yl]-4-oxobicyclo[3.1.0]hex-1-yl)methyl)-1H-isoindole-1,3(2H)-dione
no activity at 0.1 mM
2-ethyl-1-phenyl-2-isodithiobiuret
-
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
-
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
-
2-[[(4-chlorophenyl)sulfonyl]amino]-5-methylbenzoic acid
-
2-[[(4-fluorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6-dihydronaphthalene-1-carboxylic acid
-
3,5-dimethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
3-(((2-(((1'-methyl-1,4'-bipiperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000055 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((2-(((1-(1-methylethyl)piperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000046 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00095 mM
3-(((2-(((1-methylpiperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00013 mM
3-(((2-(((2-(diethylamino)ethyl)carbamoyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((2-((1E)-3-((2-hydroxyethyl)(methyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000024 mM
3-(((2-((1E)-3-(4-methylpiperazin-1-yl)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000042 mM
3-(((2-((1E)-3-(diethylamino)but-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00007 mM
3-(((2-((1E)-3-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00026 mM
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000006 mM
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
3-(((2-((1E)-3-(dimethylamino)prop-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000036 mM
3-(((2-((1E)-3-(dimethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000081 mM
3-(((2-((1E)-3-(ethyl(2-hydroxyethyl)amino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000038 mM
3-(((2-((1E)-3-(ethyl(methyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000009 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000023 mM
3-(((2-((1E)-3-(methyl(1-methylethyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000027 mM
3-(((2-((1E)-4-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
3-(((2-((1E)-5-(diethylamino)pent-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
3-(((2-((2-(1-(1-methylethyl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000062 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00035 mM
3-(((2-((2-(1-(1-methylpiperidin-4-yl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000070 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0005 mM
3-(((2-((2-(1-(cyclohexylmethyl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0015 mM
3-(((2-((2-(1-piperidin-4-ylpyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0013 mM
3-(((2-((2-(1H-imidazol-1-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0029 mM
3-(((2-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000040 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0014 mM
3-(((2-((2-(bis(1-methylethyl)amino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00064 mM
3-(((2-((2-(diethylamino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00054 mM
3-(((2-((2-(diethylamino)ethyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00052 mM
3-(((2-((2-(dimethylamino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000048 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0013 mM
3-(((2-((2-(dimethylamino)ethyl)sulfanyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000030 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0007 mM
3-(((2-((2-pyridin-2-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000053 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0020 mM
3-(((2-((2-pyridin-4-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0085 mM
3-(((2-((2-pyrrolidin-1-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0022 mM
3-(((2-((2-pyrrolidin-2-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000022 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00014 mM
3-(((2-((3-((2-hydroxyethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00028 mM
3-(((2-((3-((2-tert-butoxy-2-oxoethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0043 mM
3-(((2-((3-((tert-butoxycarbonyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000077 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0049 mM
3-(((2-((3-(1,4'-bipiperidin-1'-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000058 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0011 mM
3-(((2-((3-(1-methylpyrrolidin-2-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000096 mM
3-(((2-((3-(4-methylpiperazin-1-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000026 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00041 mM
3-(((2-((3-(bis(1-methylethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000052 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((3-(bis(2-hydroxyethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000026 mM, 50% inhibition of proliferation of HT-1080 cells at 0.001 mM
3-(((2-((3-(diethylamino)-1-methylpropyl)carbamoyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000067 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00012 mM
3-(((2-((3-(diethylamino)-1-methylpropyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0026 mM
3-(((2-((3-(diethylamino)propyl)amino)-4-methylphenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0021 mM
3-(((2-((3-(diethylamino)propyl)amino)-5-(trifluoromethyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.100 mM
3-(((2-((3-(diethylamino)propyl)amino)-5-methylphenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000066 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00066 mM
3-(((2-((3-(diethylamino)propyl)amino)-6-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
3-(((2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0014 mM
3-(((2-((3-(diethylamino)propyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00055 mM
3-(((2-((3-(dimethylamino)-2,2-dimethylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00061 mM
3-(((2-((3-(dimethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000014 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00019 mM
3-(((2-((3-(ethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00011 mM
3-(((2-((3-aminopropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00016 mM
3-(((2-((3-morpholin-4-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000022 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00032 mM
3-(((2-((3-piperazin-1-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00051 mM
3-(((2-((3-pyrrolidin-1-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000085 mM
3-(((2-((4-(diethylamino)-1-methylbutyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00021 mM
3-(((2-((4-(dimethylamino)butyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00046 mM
3-(((2-((piperidin-3-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000035 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((piperidin-4-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00046 mM
3-(((2-((pyridin-4-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000035 mM, 50% inhibition of proliferation of HT-1080 cells at 0.017 mM
3-(((2-((pyrrolidin-3-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000034 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00038 mM
3-(((2-(3,3,4,5,5-pentamethylpiperazin-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000091 mM, 50% inhibition of proliferation of HT-1080 cells at 0.015 mM
3-(((2-(3-(diethylamino)propoxy)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0062 mM
3-(((2-(3-(diethylamino)propyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000024 mM
3-(((2-(3-(diethylamino)propyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000009 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000073 mM
3-(((2-(3-(dimethylamino)propyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000035 mM
3-(((2-(4-(diethylamino)butyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000068 mM
3-(((2-(4-benzylpiperazin-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0016 mM
3-(((2-(5-(diethylamino)pentyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000045 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00035mM
3-(((2-aminophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0062 mM
3-(((3-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((4-chloro-2-((3-(diethylamino)propyl)amino)-5-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00079 mM, 50% inhibition of proliferation of HT-1080 cells at 0.013 mM
3-(((4-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0031 mM
3-(((5-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000056 mM, 50% inhibition of proliferation of HT-1080 cells at 0.010 mM
3-((phenylsulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0024 mM
3-(anilino)-5-(3-methyl-2-butenylthio)-1,2,4-triazole
-
3-(N-methyl-anilino)-5-benzylthio-1,2,4-triazole
-
3-anilino-5-(3-methyl-butylthio)-methylthio-1,2,4-triazole
-
3-anilino-5-benzylthio-1,2,4-triazole
-
3-anilino-5-benzylthio-1-(methyl-ethyl-ether)-1,2,4-triazole
-
3-anilino-5-benzylthio-1-methyl-1,2,4-triazole
-
3-anilino-5-benzylthio-2-(methyl-ethyl-ether)-1,2,4-triazole
-
3-anilino-5-benzylthio-2-methyl-1,2,4-triazole
-
3-anilino-5-mercapto-1,2,4-triazole
-
3-anilino-5-methylthio-1,2,4-triazole
-
3-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
-
3-[(phenylsulfonyl)amino]naphthalene-2-carboxylic acid
-
3-[2-(isopropyl)-anilino]-5-(furan-2-ylmethylthio)-1,2,4-triazole
-
3-[2-(isopropyl)-anilino]-5-(furan-3-ylmethylthio)-1,2,4-triazole
-
3-[2-(isopropyl)-anilino]-5-(thiophen-2-ylmethylthio)-1,2,4-triazole
-
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
-
5-((R)-1-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline
-
5-(benzylsulfanyl)-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-(benzylsulfanyl)-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-(benzylsulfanyl)-N-(4-chlorophenyl)-4H-1,2,4-triazol-3-amine
-
5-(benzylsulfanyl)-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-(benzylsulfanyl)-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-(benzylsulfanyl)-N-biphenyl-2-yl-4H-1,2,4-triazol-3-amine
-
5-(hydroxymethyl)-1-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-ol
no activity at 0.1 mM
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
-
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
-
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
-
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
5-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
5-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-4-oxobicyclo[3.1.0]hexane-1-carbaldehyde
-
5-methyl-2-((phenylsulfonyl)amino)benzoic acid
50% inhibition of enzyme at 0.0014 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0072 mM
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
-
5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[(cyclohexylmethyl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[(cyclohexylmethyl)sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[(2-methyl-2,5-dihydro-1,3-thiazol-4-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
6-(1,5-dimethylhex-4-en-1-yl)-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
-
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
-
bengamide B
nonselective inhibitor for both MetAP1 and MetAP2
bengamide G
nonselective inhibitor for both MetAP1 and MetAP2
bengamide L
nonselective inhibitor for both MetAP1 and MetAP2
bengamide M
nonselective inhibitor for both MetAP1 and MetAP2
bengamide N
nonselective inhibitor for both MetAP1 and MetAP2
bengamide O
nonselective inhibitor for both MetAP1 and MetAP2
ethyl (6E)-8-[(2R,3R)-3-[(1S,5S)-5-(hydroxymethyl)-1-methoxy-2-oxobicyclo[3.1.0]hex-6-yl]-3-methyloxiran-2-yl]oct-6-enoate
no activity at 0.1 mM
fumarranol
selective inhibitor
LAF 389
nonselective inhibitor for both MetAP1 and MetAP2
methyl 4-([5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
methyl 4-([5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
methyl 4-([5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
methyl 4-([5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
methyl 4-[(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[(5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[(5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[(5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[(5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
methyl 4-[[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]amino]benzoate
-
N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfany]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-chlorophenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methylphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methylphenyl)-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(4-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
N-(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
N-biphenyl-2-yl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(2-methoxybenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-biphenyl-2-yl-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-[4-(chloromethyl)phenyl]-5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
N-[5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
PPI-2458
potent selective inhibitor of MetAP2
[(1R)-1-carbamoyl-2-methyl-propyl]-carbamic acid-(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-but-2-enyl)-oxiranyl]-1-oxa-spiro[2.5]oct-6-yl ester
PPI-2458
(2E,4E,6E,8E)-10-((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-10-oxodeca-2,4,6,8-tetraenoic acid
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-ol
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2R)-3-methyl-1-(2-(1-methylpyrrolidin-2-yl)ethylamino)-1-oxobutan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-yl carbamate
-
i.e. PPI-2458, advanced into phase I clinical studies in non-Hodgkin's lymphoma and solid cancers, overview
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-hydroxy-3-methylbutan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-(morpholinoamino)-1-oxobutan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-oxo-1-(2-(pyrrolidin-1-yl)ethylamino)butan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-amino-2-methyl-1-oxopropan-2-ylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-carbamoylcyclopentylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(1-methylpyrrolidin-2-yl)ethylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(pyrrolidin-1-yl)ethylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl isopropylcarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl morpholinocarbamate
-
-
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl tert-butylcarbamate
-
-
(3R,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
-
-
(S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
-
-
1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
-
-
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
-
-
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
-
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 41 nM
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
-
-
2-(pyrazin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
-
2-(pyridin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-({3-[3,5-bis[4-nitrobenzylidene]-4-oxopiperidin-1-yl]-3-oxopropylsulfanyl) ethanesulfonic acid
-
inhibitor of MetAP2
2-methyl-6-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 6 nM
3,8-dihydroindeno(1,2-d)(1,2,3)triazole
-
Co(II)-form, Ki,app-value 52 nM
3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
-
-
3-((4-methylpent-3-enoyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0149 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.00068 mM
3-((5-methylhex-4-enoyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0074 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0010 mM
3-((cyclopent-1-en-1-ylcarbonyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition above 100 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition above 100 mM
3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
-
-
3-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 280 nM
3-(1H-1,2,3-triazol-5-yl)phenol
-
Co(II)-form, Ki,app-value 300 nM
3-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 260 nM
3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-{[(2-nitrophenyl)methyl]sulfanyl}-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-methylbenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(3-methoxybenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,4-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,6-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(3-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(3-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(4-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(4-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(benzoylamino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition above 100 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0074 mM
3-(benzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(hexanoylamino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0867 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0020 mM
3-(pent-4-enoylamino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition above 0.1 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.00079 mM
3-hydroxy-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0081 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0035 mM
3-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 52 nM
4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
-
-
4-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 337 nM
4-(1H-1,2,3-triazol-5-yl)phenol
-
Co(II)-form, Ki,app-value above 1000 nM
4-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value above 1000 nM
4-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 8 nM, Mn(II)-form, 0.014 mM, 50% reduction of viability of human umbilical vein endothelial cell above 0.03 mM
4-[4-(4-methoxyphenyl)piperazin-1-yl]-2-(pyridin-2-yl)quinazoline
EC50 value in presence of Co(II) is 0.0001 mM, superior inhibitory potency and selectivity for isoform MetAP1
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-(1-benzofuran-2-yl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 26% inhibition at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM
5-(2-methoxyphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 150 nM
5-(2-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 112 nM
5-(3,4-dibromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, 0.016 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM
5-(3-bromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 4 nM
5-(3-iodophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 16 nM
5-(3-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 18 nM
5-(4-bromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM
5-(4-chlorophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 6 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.005 mM
5-(4-ethylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 30 nM
5-(4-iodophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, not inhibitory at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.02 mM
5-(4-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 4400 nM, 50% reduction of viability of human umbilical vein endothelial cell at 0.03 mM
5-(4-propylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value above 1000 nM
5-biphenyl-2-yl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value above 1000 nM
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-chloro-2-(5-chloropyridin-2-yl)-6-methyl-N-((R)-2-phenyl-2-(4-phenylbutylamino)ethyl)pyrimidin-4-amine
compound shows 500fold specificity for isoform AP1 over isoform AP2
5-chloro-2-(5-chloropyridin-2-yl)-N-(2,4-diphenylbutyl)-6-methylpyrimidin-4-amine
compound shows 3175fold specificity for isoform AP1 over isoform AP2
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
-
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
5-demethylovalicin
-
IC50: 17.7 nM, inhibition of recombinant enzyme
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.015 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-phenyl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 70 nM
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-[(2E)-hepta-2,6-dien-4-yn-1-ylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
8-(pyridin-2-yl)-7H-purine
-
-
A-310840
-
IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+
A-311263
-
IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+
A-800141
-
potent MetAP2 inhibitor
bengamide B
nonselective inhibitor for both MetAP1 and MetAP2
bengamide G
nonselective inhibitor for both MetAP1 and MetAP2
bengamide L
nonselective inhibitor for both MetAP1 and MetAP2
bengamide M
nonselective inhibitor for both MetAP1 and MetAP2
bengamide N
nonselective inhibitor for both MetAP1 and MetAP2
bengamide O
nonselective inhibitor for both MetAP1 and MetAP2
fumagillol
-
i.e. (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-ol
isobutyl (2-((1,3-thiazol-2-ylamino)carbonyl)pyridin-3-yl)carbamate
-
wild-type, 50% inhibition above 100 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition above 100 mM
L-Met
-
product inhibition
L-Nle
-
product inhibition
LAF 389
nonselective inhibitor for both MetAP1 and MetAP2
Mg2+
-
1.0 mM MgCl2, 21% inhibition
Mn2+
-
0.1 mM MnCl2, 26% inhibition. 5.0 mM, 36% inhibition
N-((R)-2-(5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-ylamino)-1-phenylethyl)-3-phenylpropanamide
compound shows 323fold specificity for isoform AP1 over isoform AP2
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
-
-
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(2,2-dimethylpropanoyl)amino]pyridine-2-carboxamide
-
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(3-phenylpropanoyl)amino]pyridine-2-carboxamide
-
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[[(1E)-2-methylpropylidene]amino]pyridine-2-carboxamide
-
N-(quinolin-8-yl)benzenesulfonamide
-
-
N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0104 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0049 mM
N-benzyl-3-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 29 nM
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
-
-
quinolin-8-yl benzenesulfonate
-
-
quinolin-8-yl benzoate
-
-
tert-butyl [2-(4,5-dihydro-1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate
-
Zn2+
-
0.1 mM, complete inhibition
[(1R)-1-carbamoyl-2-methyl-propyl]-carbamic acid-(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiranyl]-1-oxaspiro(2,5)oct-6-yl ester
-
PPI-2458, potent inhibitor
[amino(cyclohexyl)methyl]phosphonic acid
compound selectively inhibits the Streptococcus pneumoniae MetAP in low micromolar range but not the human enzyme. Residue F309 in the human enzyme and M205 in the Streptococcus pneumoniae MetAP at the analogous position render them with different susceptibilities against the inhibitor
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000019 mM
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000027 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((1E)-4-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000049 mM
3-(((2-((1E)-4-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00017 mM
3-(((2-((1E)-5-(diethylamino)pent-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00012 mM
3-(((2-((1E)-5-(diethylamino)pent-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000028 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000033 mM
3-(((2-((3-(diethylamino)propyl)amino)-6-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.014 mM
3-(((2-((3-(diethylamino)propyl)amino)-6-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0083 mM
bengamide A
nonselective inhibitor for both MetAP1 and MetAP2
bengamide A
nonspecific, reversible inhibitor of MetAP-1 and MetAP-2
fumagillin
-
fumagillin
irreversible inhibition
fumagillin
a covalent bond is formed between a reactive epoxide of fumagillin and histidine-231 in the active site of Met-AP2. Fumagillin-based drugs inhibit MetAP-2 but not MetAP-1
fumagillin
higher affinity to MetAP2 than to MetAP1
fumagillin
MetAP2-specific inhibitor
fumagillin
selectively inhibits MetAP2
ovalicin
higher affinity to MetAP2 than to MetAP1
ovalicin
MetAP2-specific inhibitor
TNP-470
-
TNP-470
irreversible inhibitor
TNP-470
is likely to inhibit the enzyme by occupying the active site in the same fashion as fumagillin
TNP-470
MetAP2-specific inhibitor
TNP-470
potent selective inhibitor of MetAP2
TNP-470
selective covalent MetAP-2 inhibitor
7-amino-4-methylcoumarin
-
-
7-amino-4-methylcoumarin
-
product inhibition
A-357300
-
reversible
A-357300
-
potent MetAP2 inhibitor
bengamide A
nonselective inhibitor for both MetAP1 and MetAP2
bengamide A
nonspecific, reversible inhibitor of MetAP-1 and MetAP-2
Co2+
-
1.0 mM CoCl2, 58% inhibition
Co2+
-
in excess, a third Co2+ ion binds to the active site regions and results in inhibition
Co2+
inhibitory at 0.1 mM
fumagillin
-
-
fumagillin
-
inhibition of type II enzyme
fumagillin
lower affinity to MetAP1 than to MetAP2
fumagillin
-
potent MetAP2 inhibitor
fumagillin
-
binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview
fumagillin
-
inhibitor of MetAP2
IV-43
-
-
IV-43
MetAP1-specific inhibitor
IV-43
reversible MetAP-1 inhibitor
ovalicin
-
-
ovalicin
-
inhibition of type II enzyme
ovalicin
lower affinity to MetAP1 than to MetAP2
PPI-2458
-
TNP-470
-
-
TNP-470
-
inhibition of type II enzyme
TNP-470
-
potent MetAP2 inhibitor
TNP-470
-
binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview
TNP-470
-
inhibitor of MetAP2 and anticancer drug
additional information
-
inhibitor synthesis, pharmacokinetics, and molecular modelling
-
additional information
identification of inhibitors for human methionine aminopeptidases MetAP1 and MetAP2. 5-chloro-6-methyl-2-pyridin-2-ylpyrimidine is the minimum element for the inhibition of MetAP1, 5'-chloro is the favored substituent on the pyridine ring for the enhanced potency against MetAP1, and long C4 side chains are the essentials for higher Met AP1-selectivity
-
additional information
-
identification of inhibitors for human methionine aminopeptidases MetAP1 and MetAP2. 5-chloro-6-methyl-2-pyridin-2-ylpyrimidine is the minimum element for the inhibition of MetAP1, 5'-chloro is the favored substituent on the pyridine ring for the enhanced potency against MetAP1, and long C4 side chains are the essentials for higher Met AP1-selectivity
-
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Acidosis
Intermittent hypothermia is neuroprotective in an in vitro model of ischemic stroke.
Acute Lung Injury
Methionine aminopeptidase-2 as a selective target of myofibroblasts in pulmonary fibrosis.
Adenocarcinoma
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas.
Adenocarcinoma
Methionine Aminopeptidase 2 as a Potential Therapeutic Target for Human Non-Small-Cell Lung Cancers.
Adenocarcinoma
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Adenoma
MAP-2 Expression in the Human Adenohypophysis and in Pituitary Adenomas. An Immunohistochemical Study.
Alzheimer Disease
5-HT1A agonist and dexamethasone reversal of para-chloroamphetamine induced loss of MAP-2 and synaptophysin immunoreactivity in adult rat brain.
Alzheimer Disease
In vitro polymerization of embryonic MAP-2c and fragments of the MAP-2 microtubule binding region into structures resembling paired helical filaments.
Alzheimer Disease
MAP-2 immunolabeling can distinguish diffuse from dense-core amyloid plaques in brains with Alzheimer's disease.
Alzheimer Disease
Microtubule-associated protein 2: monoclonal antibodies demonstrate the selective incorporation of certain epitopes into Alzheimer neurofibrillary tangles.
Alzheimer Disease
Self-assembly of the brain MAP-2 microtubule-binding region into polymeric structures resembling Alzheimer filaments.
Anemia, Sickle Cell
MetAP2 inhibition modifies hemoglobin S to delay polymerization and improves blood flow in sickle cell disease.
Arthritis
An inhibitor of methionine aminopeptidase type-2, PPI-2458, ameliorates the pathophysiological disease processes of rheumatoid arthritis.
Arthritis
Suppression of inflammation and structural damage in experimental arthritis through molecular targeted therapy with PPI-2458.
Arthritis, Experimental
Methionine aminopeptidase-2 blockade reduces chronic collagen-induced arthritis: potential role for angiogenesis inhibition.
Arthritis, Rheumatoid
A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis.
Arthritis, Rheumatoid
An inhibitor of methionine aminopeptidase type-2, PPI-2458, ameliorates the pathophysiological disease processes of rheumatoid arthritis.
Astrocytoma
Cerebrospinal fluid proteomic analysis reveals dysregulation of methionine aminopeptidase-2 expression in human and mouse neurofibromatosis 1-associated glioma.
Astrocytoma
Diagnostic utility of IDH1- and p53-mutation analysis in secondary gliosarcoma.
Astrocytoma
MicroRNA profiling in pediatric pilocytic astrocytoma reveals biologically relevant targets, including PBX3, NFIB, and METAP2.
Astrocytoma
Microtubule-associated protein 2 (MAP-2) is expressed in low and high grade diffuse astrocytomas.
Autoimmune Diseases
Targeting methionine aminopeptidase 2 in cancer, obesity, and autoimmunity.
Babesiosis
Recombinant methionine aminopeptidase protein of Babesia microti: immunobiochemical characterization as a vaccine candidate against human babesiosis.
Brain Contusion
Widespread early dendritic injury associated with loss of cortical MAP-2 immunostaining in a focal ovine head impact model.
Brain Contusion
[Expression of microtubule associated protein-2 mRNA after cerebral contusion].
Brain Injuries
Combination of deferoxamine and erythropoietin: therapy for hypoxia-ischemia-induced brain injury in the neonatal rat?
Brain Injuries
The calpain proteolytic system in neonatal hypoxic-ischemia.
Brain Injuries
Topical application of the hematostatic agent Surgiflo® could attenuate brain injury in experimental TBI mice.
Brain Injuries
[Neuroprotective effect and mechanisms of hypothermia in neonatal rat cerebral hypoxic-ischemic damages]
Brain Injuries, Diffuse
Temporal Profile of Microtubule Associated Protein (MAP-2) - A Novel Indicator of Diffuse Brain Injury Severity and Early Mortality after Brain Trauma.
Brain Injuries, Traumatic
Antibodies to microtubule-associated protein 2 in patients with neuropsychiatric systemic lupus erythematosus.
Brain Injuries, Traumatic
Disruption of MAP-2 immunostaining in rat hippocampus after traumatic brain injury.
Brain Injuries, Traumatic
Increased levels of serum MAP-2 at 6-months correlate with improved outcome in survivors of severe traumatic brain injury.
Brain Ischemia
Cross-talk Between Calpain and Caspase-3 in Penumbra and Core During Focal Cerebral Ischemia-reperfusion.
Brain Ischemia
[Study on trans-differentiation of adult human myoblasts into neural precursor cells and its implantation in rats]
Brain Neoplasms
Antibodies to microtubule-associated protein 2 in patients with neuropsychiatric systemic lupus erythematosus.
Carcinogenesis
A chemical and genetic approach to the mode of action of fumagillin.
Carcinogenesis
Ectopic expression of methionine aminopeptidase-2 causes cell transformation and stimulates proliferation.
Carcinogenesis
MAP1D, a novel methionine aminopeptidase family member is overexpressed in colon cancer.
Carcinogenesis
Methionine aminopeptidase 2 over-expressed in cholangiocarcinoma: potential for drug target.
Carcinoid Tumor
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Carcinoid Tumor
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Carcinoma
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Carcinoma
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Carcinoma
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas.
Carcinoma
MAP1D, a novel methionine aminopeptidase family member is overexpressed in colon cancer.
Carcinoma
Methionine Aminopeptidase 2 as a Potential Therapeutic Target for Human Non-Small-Cell Lung Cancers.
Carcinoma
Methionine aminopeptidases type I and type II are essential to control cell proliferation.
Carcinoma
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Carcinoma, Basal Cell
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Carcinoma, Hepatocellular
Microtubule-associated protein-2 stimulates DNA synthesis catalyzed by the nuclear matrix.
Carcinoma, Merkel Cell
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Carcinoma, Neuroendocrine
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Carcinoma, Neuroendocrine
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Carcinoma, Small Cell
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Carcinoma, Small Cell
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Carcinoma, Squamous Cell
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Carcinoma, Squamous Cell
Methionine Aminopeptidase 2 as a Potential Therapeutic Target for Human Non-Small-Cell Lung Cancers.
Carcinoma, Squamous Cell
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Cerebral Hemorrhage
Motor Skill Training Promotes Sensorimotor Recovery and Increases Microtubule-Associated Protein-2 (MAP-2) Immunoreactivity in the Motor Cortex after Intracerebral Hemorrhage in the Rat.
Cerebral Infarction
[Influence of hyperbaric oxygen treatment on neural plasticity in experimental rats]
Cerebral Infarction
[Study on the effect of cluster needling of scalp acupuncture on the plasticity protein MAP-2 in rats with focal cerebral infarction]
Cholangiocarcinoma
Blocking of methionine aminopeptidase-2 by TNP-470 induces apoptosis and increases chemosensitivity of cholangiocarcinoma.
Cholangiocarcinoma
Methionine aminopeptidase 2 over-expressed in cholangiocarcinoma: potential for drug target.
Cholangiocarcinoma
Possible involvement of cyclophilin a processing in fumagillin- induced suppression of cholangiocarcinoma cell proliferation.
Cholangiocarcinoma
TNP-470, A Methionine Aminopeptidase-2 Inhibitor, Inhibits Cell Proliferation, Migration and Invasion of Human Cholangiocarcinoma Cells In Vitro.
Cholera
Membrane raft disruption results in neuritic retraction prior to neuronal death in cortical neurons.
Cholera
Phosphorylation of microtubule-associated protein-2 in GH3 cells. Regulation by cAMP and by calcium.
Choroid Plexus Neoplasms
Immunohistochemical profile and chromosomal imbalances in papillary tumours of the pineal region.
Choroidal Neovascularization
Evolving multidimensional pharmacological approaches to CNV therapy in AMD.
Ciliopathies
MetAP2 inhibition reduces food intake and body weight in a ciliopathy mouse model of obesity.
Coinfection
Genetic variability of Alder yellows phytoplasma in Alnus glutinosa in its natural Spreewald habitat
Colonic Neoplasms
Expression of methionine aminopeptidase 2, N-myristoyltransferase, and N-myristoyltransferase inhibitor protein 71 in HT29.
Colonic Neoplasms
Fumagillin inhibits colorectal cancer growth and metastasis in mice: in vivo and in vitro study of anti-angiogenesis.
Colonic Neoplasms
MAP1D, a novel methionine aminopeptidase family member is overexpressed in colon cancer.
Colonic Neoplasms
Methionine aminopeptidase 2 and cancer.
Colonic Neoplasms
Methionine Aminopeptidases as Potential Targets for Treatment of Gastrointestinal Cancers and other Tumours.
Colonic Neoplasms
NC2213: a novel methionine aminopeptidase 2 inhibitor in human colon cancer HT29 cells.
Colorectal Neoplasms
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas.
Colorectal Neoplasms
Methionine aminopeptidase 2 and cancer.
Coma
Increased levels of serum MAP-2 at 6-months correlate with improved outcome in survivors of severe traumatic brain injury.
Communicable Diseases
A simple, sensitive and reliable LC-MS/MS method for the determination of 7-bromo-5-chloroquinolin-8-ol (CLBQ14), a potent and selective inhibitor of methionine aminopeptidases: Application to pharmacokinetic studies.
Communicable Diseases
In silico identification of microRNAs predicted to regulate N-myristoyltransferase and Methionine Aminopeptidase 2 functions in cancer and infectious diseases.
Communicable Diseases
Pre-Clinical Pharmacokinetics, Tissue Distribution and Physicochemical Studies of CLBQ14, a Novel Methionine Aminopeptidase Inhibitor for the Treatment of Infectious Diseases.
Confusion
Microtubule-associated Protein-2 is a Sensitive Marker of Primary and Metastatic Neuroblastoma.
Diabetes Mellitus, Type 2
Efficacy and safety of methionine aminopeptidase 2 inhibition in type 2 diabetes: a randomised, placebo-controlled clinical trial.
Diabetes Mellitus, Type 2
The methionine aminopeptidase 2 inhibitor ZGN-1061 improves glucose control and weight in overweight and obese individuals with type 2 diabetes: A randomized, placebo-controlled trial.
Diaschisis
Ultrastructure of diaschisis lesions following traumatic brain injury.
Encephalitis
Highly active antiretroviral therapy of cognitive dysfunction and neuronal abnormalities in SCID mice with HIV encephalitis.
Encephalitis, Tick-Borne
Identification and biochemical characterisation of a novel methionine aminopeptidase from the taiga tick Ixodes persulcatus.
Endometriosis
Expression of microtubule associated protein 2 and synaptophysin in endometrium: high levels in deep infiltrating endometriosis lesions.
Ependymoma
Immunohistochemical profile and chromosomal imbalances in papillary tumours of the pineal region.
Epilepsy
Overexpression of MAP-2 via Formation of Microtubules Plays an Important Role in the Sprouting of Mossy Fibers in Epileptic Rats.
Epilepsy
White matter neuronal heterotopia in temporal lobe epilepsy: a morphometric and immunohistochemical study.
Gastrointestinal Neoplasms
Methionine Aminopeptidases as Potential Targets for Treatment of Gastrointestinal Cancers and other Tumours.
Glioblastoma
Anti-brain cancer activity of chloroform and hexane extracts of Tinospora cordifolia Miers: an in vitro perspective.
Glioblastoma
Microtubule-associated protein 2 (MAP-2) is expressed in low and high grade diffuse astrocytomas.
Glioblastoma
Redox regulation of methionine aminopeptidase 2 activity.
Glioblastoma
Suppression of glioblastoma growth and angiogenesis through molecular targeting of methionine aminopeptidase-2.
Glioma
Absence of neuron-associated microtubule proteins in the rat C-6 glioma cell line. A comparative immunoblot and immunohistochemical study.
Glioma
Cerebrospinal fluid proteomic analysis reveals dysregulation of methionine aminopeptidase-2 expression in human and mouse neurofibromatosis 1-associated glioma.
Glioma
Identification and spatial arrangement of high molecular weight proteins (Mr 300 000-330 000) co-assembling with microtubules from a cultured cell line (rat glioma C6).
Glioma
MAP-2e, a novel MAP-2 isoform, is expressed in gliomas and delineates tumor architecture and patterns of infiltration.
Graves Disease
Identification Of New Rare Variants Associated With Familial Autoimmune Thyroid Diseases By Deep Sequencing Of Linked Loci.
Hirschsprung Disease
Utility of Microtubule Associated Protein-2 (MAP-2) Immunohistochemistry for Identification of Ganglion Cells in Paraffin-Embedded Rectal Suction Biopsies.
Hirschsprung Disease
Utility of Peripherin Versus MAP-2 and Calretinin in the Evaluation of Hirschsprung Disease.
Hypertension
Early treatment with fumagillin, an inhibitor of methionine aminopeptidase-2, prevents Pulmonary Hypertension in monocrotaline-injured rats.
Hypertension, Pulmonary
Early treatment with fumagillin, an inhibitor of methionine aminopeptidase-2, prevents Pulmonary Hypertension in monocrotaline-injured rats.
Hypothyroidism
Royal jelly increased map-2 expression in hippocampal neurons of hypothyroid rats: an immunohistochemical study.
Infarction, Middle Cerebral Artery
Calpain cleaves methionine aminopeptidase-2 in a rat model of ischemia/reperfusion.
Infarction, Middle Cerebral Artery
Diacylglycerol kinase zeta is involved in the process of cerebral infarction.
Infarction, Middle Cerebral Artery
Neuronal damage and plasticity identified by microtubule-associated protein 2, growth-associated protein 43, and cyclin D1 immunoreactivity after focal cerebral ischemia in rats.
Infarction, Middle Cerebral Artery
NXY-059 maintains Akt activation and inhibits release of cytochrome C after focal cerebral ischemia.
Infections
In Vitro and In Vivo Characterization of Potent Antileishmanial Methionine Aminopeptidase-1 Inhibitors.
Infections
In Vitro Gene Silencing of the Fish Microsporidian Heterosporis saurida by RNA Interference.
Infections
Increased neurogenesis after experimental Streptococcus pneumoniae meningitis.
Infections
Salicylanilide derivatives block Mycobacterium tuberculosis through inhibition of isocitrate lyase and methionine aminopeptidase.
Infections
Targeting essential genes of Nosema for the diagnosis of pebrine disease in silkworms.
Infections
Therapeutic targets for the treatment of microsporidiosis in humans.
Infertility
The C. elegans methionine aminopeptidase 2 analog map-2 is required for germ cell proliferation.
Insulinoma
Calcium-stimulated phosphorylation of MAP-2 in pancreatic betaTC3-cells is mediated by Ca2+/calmodulin-dependent kinase II.
Intellectual Disability
METAP1 mutation is a novel candidate for autosomal recessive intellectual disability.
Latent Tuberculosis
Salicylanilide derivatives block Mycobacterium tuberculosis through inhibition of isocitrate lyase and methionine aminopeptidase.
Leiomyoma
Increased expression of neurogenic factors in uterine fibroids.
Leishmaniasis
Angiogenesis inhibitors specific for methionine aminopeptidase 2 as drugs for malaria and leishmaniasis.
Leishmaniasis, Visceral
A novel recombinant Leishmania donovani p45, a partial coding region of methionine aminopeptidase, generates protective immunity by inducing a Th1 stimulatory response against experimental visceral leishmaniasis.
Leukemia
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.
Lung Diseases
Methionine aminopeptidase-2 as a selective target of myofibroblasts in pulmonary fibrosis.
Lung Neoplasms
Methionine Aminopeptidase 2 as a Potential Therapeutic Target for Human Non-Small-Cell Lung Cancers.
Lupus Vasculitis, Central Nervous System
Antibodies to microtubule-associated protein 2 in patients with neuropsychiatric systemic lupus erythematosus.
Lyme Disease
Identification and biochemical characterisation of a novel methionine aminopeptidase from the taiga tick Ixodes persulcatus.
Lymphoma
A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo.
Lymphoma
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Lymphoma
Expression of microtubule-associated proteins, MAP-1 and MAP-2, in human neuroblastomas and differential diagnosis of immature neuroblasts.
Lymphoma
High expression of methionine aminopeptidase type 2 in germinal center B cells and their neoplastic counterparts.
Lymphoma, B-Cell
High expression of methionine aminopeptidase type 2 in germinal center B cells and their neoplastic counterparts.
Lymphoma, Non-Hodgkin
A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo.
Macular Degeneration
Evolving multidimensional pharmacological approaches to CNV therapy in AMD.
Malaria
Angiogenesis inhibitors specific for methionine aminopeptidase 2 as drugs for malaria and leishmaniasis.
Malaria
Antiparasitic activities of novel, orally available fumagillin analogs.
Malaria
Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo.
Malaria
Functional characterization of both MAP kinases of the human malaria parasite Plasmodium falciparum by reverse genetics.
Malaria
PfMAP-2 is essential for male gametogenesis in the malaria parasite Plasmodium falciparum.
Medulloblastoma
Apoptosis, neuronal maturation, and neurotrophin expression within medulloblastoma nodules.
Medulloblastoma
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Medulloblastoma
SPARC Stimulates Neuronal Differentiation of Medulloblastoma Cells via the Notch1/STAT3 Pathway.
Melanoma
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Melanoma
Differential expression of microtubule-associated protein 2 in melanocytic skin lesions.
Melanoma
Expression of microtubule-associated protein 2 in benign and malignant melanocytes: implications for differentiation and progression of cutaneous melanoma.
Melanoma
Inhibition of melanoma tumor growth by a pharmacological inhibitor of MetAP-2, PPI-2458.
Mesothelioma
High expression of methionine aminopeptidase type 2 in germinal center B cells and their neoplastic counterparts.
Mesothelioma
Methionine aminopeptidase-2 regulates human mesothelioma cell survival: role of Bcl-2 expression and telomerase activity.
Microsporidiosis
Investigations into microsporidian methionine aminopeptidase type 2: a therapeutic target for microsporidiosis.
Microsporidiosis
Molecular characterization of Nosema bombycis methionine aminopeptidase 2 (MetAP2) gene and evaluation of anti-microsporidian activity of Fumagilin-B in silkworm Bombyx mori.
Microsporidiosis
System for Expression of Microsporidian Methionine Amino Peptidase Type 2 (MetAP2) in the Yeast Saccharomyces cerevisiae.
Microsporidiosis
Therapeutic targets for the treatment of microsporidiosis in humans.
Neoplasm Metastasis
CHD1L promotes EOC cell invasiveness and metastasis via the regulation of METAP2.
Neoplasm Metastasis
Differential expression of microtubule-associated protein 2 in melanocytic skin lesions.
Neoplasm Metastasis
Hypoxia-Induced LIN28A mRNA Promotes the Metastasis of Colon Cancer in a Protein-Coding-Independent Manner.
Neoplasms
1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents.
Neoplasms
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Neoplasms
5-demethylovalicin, as a methionine aminopeptidase-2 inhibitor produced by Chrysosporium.
Neoplasms
A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo.
Neoplasms
Cerebellar Liponeurocytoma, an Unusual Tumor of the Central Nervous System--Ultrastructural Examination.
Neoplasms
Cerebrospinal fluid proteomic analysis reveals dysregulation of methionine aminopeptidase-2 expression in human and mouse neurofibromatosis 1-associated glioma.
Neoplasms
CHD1L promotes EOC cell invasiveness and metastasis via the regulation of METAP2.
Neoplasms
Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor.
Neoplasms
Diagnostic utility of IDH1- and p53-mutation analysis in secondary gliosarcoma.
Neoplasms
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Neoplasms
Diagnostic value of microtubule-associated protein-2 in Merkel cell carcinoma.
Neoplasms
Differential expression of microtubule-associated protein 2 in melanocytic skin lesions.
Neoplasms
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Neoplasms
Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
Neoplasms
Discovery, identification, and characterization of candidate pharmacodynamic markers of methionine aminopeptidase-2 inhibition.
Neoplasms
Ectopic expression of methionine aminopeptidase-2 causes cell transformation and stimulates proliferation.
Neoplasms
Expression of microtubule-associated proteins, MAP-1 and MAP-2, in human neuroblastomas and differential diagnosis of immature neuroblasts.
Neoplasms
Fumagillin treatment of hepatocellular carcinoma in rats: an in vivo study of antiangiogenesis.
Neoplasms
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas.
Neoplasms
Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer.
Neoplasms
Identification of potential inhibitors of human methionine aminopeptidase (type II) for cancer therapy: Structure-based virtual screening, ADMET prediction and molecular dynamics studies.
Neoplasms
Immunohistochemical profile and chromosomal imbalances in papillary tumours of the pineal region.
Neoplasms
Immunomodulatory activity of a methionine aminopeptidase-2 inhibitor on B cell differentiation.
Neoplasms
In silico identification of microRNAs predicted to regulate N-myristoyltransferase and Methionine Aminopeptidase 2 functions in cancer and infectious diseases.
Neoplasms
In Vivo Imaging of Methionine Aminopeptidase II for Prostate Cancer Risk Stratification.
Neoplasms
Increased expression of neurogenic factors in uterine fibroids.
Neoplasms
Inhibition of melanoma tumor growth by a pharmacological inhibitor of MetAP-2, PPI-2458.
Neoplasms
MAP-2e, a novel MAP-2 isoform, is expressed in gliomas and delineates tumor architecture and patterns of infiltration.
Neoplasms
MAP1D, a novel methionine aminopeptidase family member is overexpressed in colon cancer.
Neoplasms
Metabolites of PPI-2458, a Selective, Irreversible Inhibitor of Methionine Aminopeptidase-2: Structure Determination and In Vivo Activity.
Neoplasms
MetAP1 and MetAP2 drive cell selectivity for a potent anti-cancer agent in synergy, by controlling glutathione redox state.
Neoplasms
Methionine aminopeptidase 2 and cancer.
Neoplasms
Methionine Aminopeptidase 2 as a Potential Therapeutic Target for Human Non-Small-Cell Lung Cancers.
Neoplasms
Methionine aminopeptidase 2 over-expressed in cholangiocarcinoma: potential for drug target.
Neoplasms
Methionine aminopeptidase-2 blockade reduces chronic collagen-induced arthritis: potential role for angiogenesis inhibition.
Neoplasms
Methionine aminopeptidase-2 regulates human mesothelioma cell survival: role of Bcl-2 expression and telomerase activity.
Neoplasms
Methionine aminopeptidases and angiogenesis.
Neoplasms
Methionine Aminopeptidases as Potential Targets for Treatment of Gastrointestinal Cancers and other Tumours.
Neoplasms
Microtubule-associated Protein-2 is a Sensitive Marker of Primary and Metastatic Neuroblastoma.
Neoplasms
Microtubule-associated protein-2: a new sensitive and specific marker for pulmonary carcinoid tumor and small cell carcinoma.
Neoplasms
Novel inhibitors targeted to methionine aminopeptidase 2 (MetAP2) strongly inhibit the growth of cancers in xenografted nude model.
Neoplasms
Optimizing the dosing schedule of TNP-470 [O-(chloroacetyl-carbamoyl) fumagillol] enhances its antitumor and antiangiogenic efficacies.
Neoplasms
Orally active fumagillin analogues: transformations of a reactive warhead in the gastric environment.
Neoplasms
Possible involvement of cyclophilin a processing in fumagillin- induced suppression of cholangiocarcinoma cell proliferation.
Neoplasms
Redox regulation of methionine aminopeptidase 2 activity.
Neoplasms
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
Neoplasms
Suppression of glioblastoma growth and angiogenesis through molecular targeting of methionine aminopeptidase-2.
Neoplasms
Targeting methionine aminopeptidase 2 in cancer, obesity, and autoimmunity.
Neoplasms
The clinicopathological features of liponeurocytoma.
Neoplasms
The Development of MetAP-2 Inhibitors in Cancer Treatment.
Neoplasms
The Role of Methionine Aminopeptidase 2 in Lymphangiogenesis.
Neoplasms
TNP-470, A Methionine Aminopeptidase-2 Inhibitor, Inhibits Cell Proliferation, Migration and Invasion of Human Cholangiocarcinoma Cells In Vitro.
Neoplasms
Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.
Neoplasms, Neuroepithelial
MAP-2 immunoexpression in gliomatosis cerebri.
Nervous System Diseases
Antibodies to microtubule-associated protein 2 in patients with neuropsychiatric systemic lupus erythematosus.
Neuritis
[Cysteinyl leukotriene receptor 1 antagonist pranlukast modulates differentiation of SK-N-SH cells]
Neuroblastoma
Aminohexanoic hydroxamate is a potent inducer of the differentiation of mouse neuroblastoma cells.
Neuroblastoma
Anti-brain cancer activity of chloroform and hexane extracts of Tinospora cordifolia Miers: an in vitro perspective.
Neuroblastoma
Differential distribution of microtubule-associated proteins MAP-1 and MAP-2 in neurons of rat brain and association of MAP-1 with microtubules of neuroblastoma cells (clone N2A).
Neuroblastoma
Expression of microtubule-associated proteins, MAP-1 and MAP-2, in human neuroblastomas and differential diagnosis of immature neuroblasts.
Neuroblastoma
Ganglioside-enhanced neurite growth: evidence for a selective induction of high-molecular-weight MAP-2.
Neuroblastoma
Localization of specific epitopes on human microtubule-associated protein 2.
Neuroblastoma
Methionine aminopeptidase 2 inhibition is an effective treatment strategy for neuroblastoma in preclinical models.
Neuroblastoma
Microtubule-associated Protein-2 is a Sensitive Marker of Primary and Metastatic Neuroblastoma.
Neuroblastoma
Prospects for therapeutic inhibition of neuroblastoma angiogenesis.
Neuroblastoma
Sellar neuroblastoma mimicking a pituitary tumour: case report and review of the literature.
Neuroblastoma
Tinospora cordifolia Induces Differentiation and Senescence Pathways in Neuroblastoma Cells.
Neurocytoma
Diagnostic value of microtubule-associated protein-2 (MAP-2) for neuroendocrine neoplasms.
Neurodegenerative Diseases
Survey for CAG repeat polymorphisms in the human MAP-2 gene.
Neurofibromatoses
Cerebrospinal fluid proteomic analysis reveals dysregulation of methionine aminopeptidase-2 expression in human and mouse neurofibromatosis 1-associated glioma.
Nevus, Pigmented
Expression of microtubule-associated protein 2 in benign and malignant melanocytes: implications for differentiation and progression of cutaneous melanoma.
Obesity
Approaches for the Development of Drugs for Treatment of Obesity and Metabolic Syndrome.
Obesity
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 1.
Obesity
Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 2.
Obesity
Effects of MetAP2 inhibition on hyperphagia and body weight in Prader-Willi syndrome: A randomized, double-blind, placebo-controlled trial.
Obesity
Efficacy and safety of methionine aminopeptidase 2 inhibition in type 2 diabetes: a randomised, placebo-controlled clinical trial.
Obesity
Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity.
Obesity
MetAP2 inhibition reduces food intake and body weight in a ciliopathy mouse model of obesity.
Obesity
Preclinical Efficacy and Safety of the Novel Antidiabetic, Antiobesity MetAP2 Inhibitor ZGN-1061.
Obesity
Robust Reductions of Excess Weight and Hyperphagia by Beloranib in Rat Models of Genetic and Hypothalamic Obesity.
Obesity
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
Obesity
Targeting methionine aminopeptidase 2 in cancer, obesity, and autoimmunity.
Obesity
Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 inhibitors.
Ovarian Cysts
Increased expression of neurogenic factors in uterine fibroids.
Overweight
The methionine aminopeptidase 2 inhibitor ZGN-1061 improves glucose control and weight in overweight and obese individuals with type 2 diabetes: A randomized, placebo-controlled trial.
Overweight
[Significance of mean arterial blood pressure in the 2d trimester and the roll-over test for gestosis screening in normal, overweight and underweight primigravid patients]
Persistent Vegetative State
Increased levels of serum MAP-2 at 6-months correlate with improved outcome in survivors of severe traumatic brain injury.
Pituitary Neoplasms
MAP-2 Expression in the Human Adenohypophysis and in Pituitary Adenomas. An Immunohistochemical Study.
Pneumonia
Identification of the Molecular Basis of Inhibitor Selectivity between the Human and Streptococcal Type I Methionine Aminopeptidases.
Prader-Willi Syndrome
Effects of MetAP2 inhibition on hyperphagia and body weight in Prader-Willi syndrome: A randomized, double-blind, placebo-controlled trial.
Prader-Willi Syndrome
Preclinical Efficacy and Safety of the Novel Antidiabetic, Antiobesity MetAP2 Inhibitor ZGN-1061.
Pre-Eclampsia
Elevated midtrimester mean arterial blood pressure in women with severe preeclampsia.
Prediabetic State
MetAP2 Inhibitor Treatment of High-Fat and -Fructose Fed Dogs: Impact on the Response to Oral Glucose Ingestion and a Hyperinsulinemic Hyperglycemic Clamp.
Prostatic Neoplasms
In Vivo Imaging of Methionine Aminopeptidase II for Prostate Cancer Risk Stratification.
Prostatic Neoplasms
Synthesis, Anticancer Activity on Prostate Cancer Cell Lines and Molecular Modeling Studies of Flurbiprofen-Thioether Derivatives as Potential Target of MetAP (type II).
Pulmonary Arterial Hypertension
Early treatment with fumagillin, an inhibitor of methionine aminopeptidase-2, prevents Pulmonary Hypertension in monocrotaline-injured rats.
Pulmonary Fibrosis
Early treatment with fumagillin, an inhibitor of methionine aminopeptidase-2, prevents Pulmonary Hypertension in monocrotaline-injured rats.
Pulmonary Fibrosis
Methionine aminopeptidase-2 as a selective target of myofibroblasts in pulmonary fibrosis.
Retinoblastoma
Immunohistochemical analysis of retinoblastoma cell phenotype using neuronal and glial cell markers.
Rett Syndrome
Dendritic cytoskeletal protein expression in mental retardation: an immunohistochemical study of the neocortex in Rett syndrome.
Rhabdomyosarcoma
Expression of microtubule-associated proteins, MAP-1 and MAP-2, in human neuroblastomas and differential diagnosis of immature neuroblasts.
Sarcoma
Microtubule-associated Protein-2 is a Sensitive Marker of Primary and Metastatic Neuroblastoma.
Sarcoma, Ewing
Expression of microtubule-associated proteins, MAP-1 and MAP-2, in human neuroblastomas and differential diagnosis of immature neuroblasts.
Seizures
Effect of connexin 36 blockers on the neuronal cytoskeleton and synaptic plasticity in kainic acid-kindled rats.
Starvation
An alternative methionine aminopeptidase, MAP-A, is required for nitrogen starvation and high-light acclimation in the cyanobacterium Synechocystis sp. PCC 6803.
Starvation
[The influence of protein starvation on hydrolytic and transport characteristics of the rat small intestine in chronic experiments]
Stroke
Antibodies to microtubule-associated protein 2 in patients with neuropsychiatric systemic lupus erythematosus.
Stroke
Cortical neurogenesis in adult rats after reversible photothrombotic stroke.
Stroke
Cortical neurogenesis in adult rats after transient middle cerebral artery occlusion.
Synovitis
Involution of collagen-induced arthritis with an angiogenesis inhibitor, PPI-2458.
Tetanus
Neuronal development and migration in explant cultures of the adult canary forebrain.
Thyroiditis
Identification Of New Rare Variants Associated With Familial Autoimmune Thyroid Diseases By Deep Sequencing Of Linked Loci.
Tuberculosis
Amino-terminal extension present in the methionine aminopeptidase type 1c of Mycobacterium tuberculosis is indispensible for its activity.
Tuberculosis
Bengamides display potent activity against drug-resistant Mycobacterium tuberculosis.
Tuberculosis
Catalysis and inhibition of Mycobacterium tuberculosis methionine aminopeptidase.
Tuberculosis
Computational validation of 3-ammonio-3-(4-oxido- 1H-imidazol-1-ium-5-yl) propane-1, 1-bis (olate) as a potent anti-tubercular drug against mt-MetAP.
Tuberculosis
Determination of binding affinity of metal cofactor to the active site of methionine aminopeptidase based on quantitation of functional enzyme.
Tuberculosis
Expression and characterization of Mycobacterium tuberculosis methionine aminopeptidase type 1a.
Tuberculosis
Identification of an SH3-binding motif in a new class of methionine aminopeptidases from Mycobacterium tuberculosis suggests a mode of interaction with the ribosome.
Tuberculosis
MapB Protein is the Essential Methionine Aminopeptidase in Mycobacterium tuberculosis.
Tuberculosis
Methionine aminopeptidases from Mycobacterium tuberculosis as novel antimycobacterial targets.
Tuberculosis
Salicylanilide derivatives block Mycobacterium tuberculosis through inhibition of isocitrate lyase and methionine aminopeptidase.
Tuberculosis
Structural analysis of inhibition of Mycobacterium tuberculosis methionine aminopeptidase by bengamide derivatives.
Tuberculosis
The unique functional role of the C-HS hydrogen bond in the substrate specificity and enzyme catalysis of type 1 methionine aminopeptidase.
Uterine Cervical Neoplasms
Molecular analysis of cellular loci disrupted by papillomavirus 16 integration in cervical cancer: frequent viral integration in topologically destabilized and transcriptionally active chromosomal regions.
Vitamin E Deficiency
Vitamin E deficiency and aging effect on expression levels of GAP-43 and MAP-2 in selected areas of the brain.
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0.000001
3-(anilino)-5-(3-methyl-2-butenylthio)-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000015
3-(N-methyl-anilino)-5-benzylthio-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000066
3-anilino-5-(3-methyl-butylthio)-methylthio-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.0000005
3-anilino-5-benzylthio-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.01
3-anilino-5-benzylthio-1-methyl-1,2,4-triazole
IC50 above 0.01 mM, in 50 mM HEPES-Na+ (pH 7.5), with 100 mM NaCl
0.0013
3-anilino-5-benzylthio-2-methyl-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.001
3-anilino-5-methylthio-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000003
3-[2-(isopropyl)-anilino]-5-(furan-2-ylmethylthio)-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000024
3-[2-(isopropyl)-anilino]-5-(furan-3-ylmethylthio)-1,2,4-triazole
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.00000004
5-(benzylsulfanyl)-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000017
5-(benzylsulfanyl)-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00000043
5-(benzylsulfanyl)-N-(4-chlorophenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00000005
5-(benzylsulfanyl)-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00000007
5-(benzylsulfanyl)-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00074
5-(benzylsulfanyl)-N-biphenyl-2-yl-4H-1,2,4-triazol-3-amine
apparent value
0.00000015
5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000033
5-[(cyclohexylmethyl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000083
5-[(cyclohexylmethyl)sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000031
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0001
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000012
5-[[(2-methyl-2,5-dihydro-1,3-thiazol-4-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000036
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000035 - 0.0000078
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
0.00000023
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00000013
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.00000065
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.000061
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.01
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
Ki above 0.01 mM, apparent value
0.0000024
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.000004
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000021
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000033
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000005
methyl 4-([5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
apparent value
0.0000027
methyl 4-([5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
apparent value
0.0000009
methyl 4-([5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
apparent value
0.0000009
methyl 4-([5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
apparent value
0.0000038
methyl 4-[(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.0000008
methyl 4-[(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.00000041
methyl 4-[(5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.00001
methyl 4-[(5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.000135
methyl 4-[(5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.0000013
methyl 4-[(5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
apparent value
0.0000007
methyl 4-[[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]amino]benzoate
apparent value
0.0000037
N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000038
N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000025
N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000009
N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000024
N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000096
N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000021
N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000007
N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000013
N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.001
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
Ki above 0.001 mM, apparent value
0.000018
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.00000052
N-(4-chlorophenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000052
N-(4-chlorophenyl)-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000004
N-(4-chlorophenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000025
N-(4-chlorophenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000048
N-(4-chlorophenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000018
N-(4-chlorophenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfany]-4H-1,2,4-triazol-3-amine
apparent value
0.00000061
N-(4-chlorophenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.01
N-(4-chlorophenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000023
N-(4-chlorophenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.00000016
N-(4-methoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000018
N-(4-methoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000061
N-(4-methoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000016
N-(4-methoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.000034
N-(4-methoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000078
N-(4-methylphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000057
N-(4-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000052
N-(4-methylphenyl)-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000078
N-(4-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000065
N-(4-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000091
N-(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
apparent value
0.0000015
N-(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
apparent value
0.00035
N-biphenyl-2-yl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.002
N-biphenyl-2-yl-5-[(2-methoxybenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Ki above 0.002 mM, apparent value
0.00048
N-biphenyl-2-yl-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.00065
N-biphenyl-2-yl-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.002
N-biphenyl-2-yl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Ki above 0.002 mM, apparent value
0.0017
N-biphenyl-2-yl-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.00000075
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.0000015
N-[4-(chloromethyl)phenyl]-5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
apparent value
0.00000004
N-[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.0000003
N-[5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.0000017
N-[5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.0000005
N-[5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.000003
N-[5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.0000057
N-[5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
apparent value
0.162
5-[(2E)-hepta-2,6-dien-4-yn-1-ylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
0.29
7-amino-4-methylcoumarin
-
pH 7.5, 30°C
0.0000016
fumagillin
-
pH 7.5, 30°C
0.02
L-Met
-
pH 7.5, 30°C
0.18
L-Met-(RS)-sulfoxide
-
pH 7.5, 30°C
0.000000245
[(1R)-1-carbamoyl-2-methyl-propyl]-carbamic acid-(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiranyl]-1-oxaspiro(2,5)oct-6-yl ester
-
recombinant MetAP-2, in 50 mM Hepes, 100 mM MnCl2, 100 mM NaCl, 0.005% (w/v) bovine serum albumin, 0.006% (w/v) 3-[(3-cholamidopropyl)dimethylammonio]propanesulphonic acid, at pH 7.5
0.5
[amino(cyclohexyl)methyl]phosphonic acid
IC50 value above 0.5 mM, pH not specified in the publication, temperature not specified in the publication
0.0000035
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
0.0000078
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
apparent value
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000027
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Homo sapiens
-
0.0081
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
Homo sapiens
MetAP2
0.0039
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
Homo sapiens
-
0.0011
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
Homo sapiens
-
0.011
2-[[(4-chlorophenyl)sulfonyl]amino]-5-methylbenzoic acid
Homo sapiens
-
0.00001
2-[[(4-fluorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Homo sapiens
-
0.00002
2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6-dihydronaphthalene-1-carboxylic acid
Homo sapiens
-
0.00035
3,5-dimethyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.000009
3-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
Homo sapiens
-
0.000019
3-[(phenylsulfonyl)amino]naphthalene-2-carboxylic acid
Homo sapiens
-
0.000015
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
Homo sapiens
-
0.000038
5-((R)-1-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0091
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
Homo sapiens
-
0.01
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.0008
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
Homo sapiens
MetAP2
0.0076
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP2
0.0033
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP2
0.00009
5-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.0132
5-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-4-oxobicyclo[3.1.0]hexane-1-carbaldehyde
Homo sapiens
-
0.001
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.0575
6-(1,5-dimethylhex-4-en-1-yl)-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens
-
0.0338
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens
-
0.00015
A-357300
Homo sapiens
-
0.00002
A-800141
Homo sapiens
-
0.0105
bengamide A
Homo sapiens
MetAP2
0.0179
bengamide B
Homo sapiens
MetAP2
0.05
bengamide G
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.05
bengamide L
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.05
bengamide M
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.05
bengamide N
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.05
bengamide O
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.008
fumagalone
Homo sapiens
-
0.00323
fumarranol
Homo sapiens
-
0.000001 - 0.000003
TNP-470
0.0000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2R)-3-methyl-1-(2-(1-methylpyrrolidin-2-yl)ethylamino)-1-oxobutan-2-ylcarbamate
Homo sapiens
-
above, in HUVEC
0.000000095
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-ylcarbamate
Homo sapiens
-
in HUVEC
0.0000017
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-(morpholinoamino)-1-oxobutan-2-ylcarbamate
Homo sapiens
-
in HUVEC
0.0000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-oxo-1-(2-(pyrrolidin-1-yl)ethylamino)butan-2-ylcarbamate
Homo sapiens
-
in HUVEC
0.0000017
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-amino-2-methyl-1-oxopropan-2-ylcarbamate
Homo sapiens
-
in HUVEC
0.0000007
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-carbamoylcyclopentylcarbamate
Homo sapiens
-
in HUVEC
0.0000002
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(1-methylpyrrolidin-2-yl)ethylcarbamate
Homo sapiens
-
above, in HUVEC
0.0000001
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(pyrrolidin-1-yl)ethylcarbamate
Homo sapiens
-
in HUVEC
0.00000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl isopropylcarbamate
Homo sapiens
-
in HUVEC
0.0000007
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl morpholinocarbamate
Homo sapiens
-
in HUVEC
0.0000011
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl tert-butylcarbamate
Homo sapiens
-
in HUVEC
0.00000025
(3R,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
Homo sapiens
-
in HUVEC
0.000000036
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
Homo sapiens
-
in HUVEC
0.00000004
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
Homo sapiens
-
in HUVEC
0.000000038
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
Homo sapiens
-
in HUVEC
0.000000018
(S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
Homo sapiens
-
in HUVEC
0.0000013
1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
Homo sapiens
-
in HUVEC
0.0011
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
Homo sapiens
MetAP1
0.0243 - 0.0324
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0398
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0101
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.019
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0001
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
Homo sapiens
-
in HUVEC
0.0329
2-(pyrazin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0093
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0133 - 0.0284
2-(pyridin-2-yl)-1H-benzimidazole
0.0329 - 0.0373
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
0.0401 - 0.0484
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
0.0267 - 0.0276
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
0.008 - 0.0103
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
0.0001
3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
Homo sapiens
-
in HUVEC
0.000015
3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
Homo sapiens
-
in HUVEC
0.01178
3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-{[(2-nitrophenyl)methyl]sulfanyl}-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00093
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.01766
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-methylbenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.03071
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(3-methoxybenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00224
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.01239
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00395
3-(2,4-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0048
3-(2,6-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00537
3-(2-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00184
3-(2-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00591
3-(3-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00192
3-(3-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00729
3-(4-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00345
3-(4-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00601
3-(benzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000007
4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
Homo sapiens
-
in HUVEC
0.0388
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0284 - 0.0326
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
0.028 - 0.047
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0002
5-chloro-2-(5-chloropyridin-2-yl)-6-methyl-N-((R)-2-phenyl-2-(4-phenylbutylamino)ethyl)pyrimidin-4-amine
Homo sapiens
22°C, pH not specified in the publication
0.000063
5-chloro-2-(5-chloropyridin-2-yl)-N-(2,4-diphenylbutyl)-6-methylpyrimidin-4-amine
Homo sapiens
22°C, pH not specified in the publication
0.0181 - 0.0488
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
0.0004
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
Homo sapiens
MetAP1
0.0006
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP1
0.0033
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP1
0.0000177
5-demethylovalicin
Homo sapiens
-
IC50: 17.7 nM, inhibition of recombinant enzyme
0.0384 - 0.0458
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0149 - 0.0347
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
0.0355 - 0.0406
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0077 - 0.0326
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
0.0485
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0288
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0441
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0339 - 0.0364
8-(pyridin-2-yl)-7H-purine
0.0056 - 0.0215
8-hydroxy quinoline
0.000031
A-310840
Homo sapiens
-
IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+
0.000121
A-311263
Homo sapiens
-
IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+
0.0019
bengamide A
Homo sapiens
MetAP1
0.0293
bengamide B
Homo sapiens
MetAP1
0.0268
bengamide G
Homo sapiens
MetAP1
0.0371
bengamide L
Homo sapiens
MetAP1
0.0054
bengamide M
Homo sapiens
MetAP1
0.0402
bengamide N
Homo sapiens
MetAP1
0.0027
bengamide O
Homo sapiens
MetAP1
0.000093
N-((R)-2-(5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-ylamino)-1-phenylethyl)-3-phenylpropanamide
Homo sapiens
22°C, pH not specified in the publication
0.0081 - 0.0258
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
0.0029
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(2,2-dimethylpropanoyl)amino]pyridine-2-carboxamide
Homo sapiens
MetAP1
0.0035
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(3-phenylpropanoyl)amino]pyridine-2-carboxamide
Homo sapiens
MetAP1
0.0064
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[[(1E)-2-methylpropylidene]amino]pyridine-2-carboxamide
Homo sapiens
MetAP1
0.0398 - 0.0449
N-(quinolin-8-yl)benzenesulfonamide
0.041
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0412 - 0.0417
quinolin-8-yl benzenesulfonate
0.0348 - 0.0428
quinolin-8-yl benzoate
0.0015
tert-butyl [2-(4,5-dihydro-1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate
Homo sapiens
MetAP1
0.0447 - 0.0478
thiabendazole
0.00105
TNP-470
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001
TNP-470
Homo sapiens
-
0.000003
TNP-470
Homo sapiens
-
0.0243
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0324
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0133
2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0284
2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0329
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0373
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0401
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0484
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0267
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0276
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.008
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0103
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0284
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0326
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.028
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.047
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0181
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0488
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0384
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0458
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0149
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0347
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0355
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0406
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0077
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0326
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0339
8-(pyridin-2-yl)-7H-purine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0364
8-(pyridin-2-yl)-7H-purine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0056
8-hydroxy quinoline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0215
8-hydroxy quinoline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0081
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0258
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0398
N-(quinolin-8-yl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0449
N-(quinolin-8-yl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0412
quinolin-8-yl benzenesulfonate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0417
quinolin-8-yl benzenesulfonate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0348
quinolin-8-yl benzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0428
quinolin-8-yl benzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0447
thiabendazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0478
thiabendazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
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Arfin, S.M.; Kendall, R.L.; Hall, L.; Weaver, L.H.; Stewart, A.E.; Matthews, B.W.; Bradshaw, R.A.
Eukaryotic methionyl aminopeptidases: two classes of cobalt-dependent enzymes
Proc. Natl. Acad. Sci. USA
92
7714-7718
1995
Escherichia coli, Homo sapiens, Sus scrofa
brenda
Yang, G.; Kirkpatrick, R.B.; Ho, T.; Zhang, G.F.; Liang, P.H.; Johanson, K.O.; Casper, D.J.; Doyle, M.L.; Marino, J.P., Jr.; Thompson, S.K.; Chen, W.; Tew, D.G.; Meek, T.D.
Steady-State Kinetic Characterization of Substrates and Metal-Ion Specificities of the Full-Length and N-Terminally Truncated Recombinant Human Methionine Aminopeptidases (Type 2)
Biochemistry
40
10645-10654
2001
Homo sapiens
brenda
Son, K.H.; Kwon, J.Y.; Jeong, H.W.; Kim, H.K.; Kim, C.J.; Chang, Y.H.; Choi, J.D.; Kwon, B.M.
5-demethylovalicin, as a methionine aminopeptidase-2 inhibitor produced by Chrysosporium
Bioorg. Med. Chem.
10
185-188
2002
Homo sapiens
brenda
Liu, S.; Widom, J.; Kemp, C.W.; Crews, C.M.; Clardy, J.
Structure of human methionine aminopeptidase-2 complexed with fumagillin
Science
282
1324-1327
1998
Homo sapiens (P50579), Homo sapiens
brenda
Wang, J.; Sheppard, G.S.; Lou, P.; Kawai, M.; Park, C.; Egan, D.A.; Schneider, A.; Bouska, J.; Lesniewski, R.; Henkin, J.
Physiologically relevant metal cofactor for methionine aminopeptidase-2 is manganese
Biochemistry
42
5035-5042
2003
Homo sapiens
brenda
Selvakumar, P.; Lakshmikuttyamma, A.; Lawman, Z.; Bonham, K.; Dimmock, J.R.; Sharma, R.K.
Expression of methionine aminopeptidase 2,N-myristoyltransferase, and N-myristoyltransferase inhibitor protein 71 in HT29
Biochem. Biophys. Res. Commun.
322
1012-1017
2004
Homo sapiens
brenda
Li, J.Y.; Chen, L.L.; Cui, Y.M.; Luo, Q.L.; Gu, M.; Nan, F.J.; Ye, Q.Z.
Characterization of full length and truncated type I human methionine aminopeptidases expressed from Escherichia coli
Biochemistry
43
7892-7898
2004
Homo sapiens
brenda
Addlagatta, A.; Hu, X.; Liu, J.O.; Matthews, B.W.
Structural basis for the functional differences between type I and type II human methionine aminopeptidases
Biochemistry
44
14741-14749
2005
Homo sapiens
brenda
Selvakumar, P.; Lakshmikuttyamma, A.; Kanthan, R.; Kanthan, S.C.; Dimmock, J.R.; Sharma, R.K.
High expression of methionine aminopeptidase 2 in human colorectal adenocarcinomas
Clin. Cancer Res.
10
2771-2775
2004
Homo sapiens
brenda
Morowitz, M.J.; Barr, R.; Wang, Q.; King, R.; Rhodin, N.; Pawel, B.; Zhao, H.; Erickson, S.A.; Sheppard, G.S.; Wang, J.; Maris, J.M.; Shusterman, S.
Methionine aminopeptidase 2 inhibition is an effective treatment strategy for neuroblastoma in preclinical models
Clin. Cancer Res.
11
2680-2685
2005
Homo sapiens
brenda
Cooper, A.C.; Karp, R.M.; Clark, E.J.; Taghizadeh, N.R.; Hoyt, J.G.; Labenski, M.T.; Murray, M.J.; Hannig, G.; Westlin, W.F.; Thompson, C.D.
A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo
Clin. Cancer Res.
12
2583-2590
2006
Homo sapiens, Homo sapiens (P50579)
brenda
Li, J.Y.; Cui, Y.M.; Chen, L.L.; Gu, M.; Li, J.; Nan, F.J.; Ye, Q.Z.
Mutations at the S1 sites of methionine aminopeptidases from Escherichia coli and Homo sapiens reveal the residues critical for substrate specificity
J. Biol. Chem.
279
21128-21134
2004
Homo sapiens, Escherichia coli (P0AE18), Escherichia coli
brenda
Brdlik, C.M.; Crews, C.M.
A single amino acid residue defines the difference in ovalicin sensitivity between type I and II methionine aminopeptidases
J. Biol. Chem.
279
9475-9480
2004
Homo sapiens
brenda
Kallander, L.S.; Lu, Q.; Chen, W.; Tomaszek, T.; Yang, G.; Tew, D.; Meek, T.D.; Hofmann, G.A.; Schulz-Pritchard, C.K.; Smith, W.W.; Janson, C.A.; Ryan, M.D.; Zhang, G.F.; Johanson, K.O.; Kirkpatrick, R.B.; Ho, T.F.; Fisher, P.W.; Mattern, M.R.; Johnson, R.K.; Hansbury, M.J.; Winkler, J.D.; Ward, K.W.; Veber, D.F.; Thompson, S.K.
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.
48
5644-5647
2005
Homo sapiens
brenda
Sheppard, G.S.; Wang, J.; Kawai, M.; Fidanze, S.D.; Bamaung, N.Y.; Erickson, S.A.; Barnes, D.M.; Tedrow, J.S.; Kolaczkowski, L.; Vasudevan, A.; Park, D.C.; Wang, G.T.; Sanders, W.J.; Mantei, R.A.; Palazzo, F.; Tucker-Garcia, L.; Lou, P.; Zhang, Q.; Park, C.H.; Kim, K.H.; Petros, A.; Olejniczak, E.; Nettesheim, D.; Hajduk, P.; Henkin, J.; Lesniewski, R.; Davidsen, S.K.; Bell, R.L.
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding
J. Med. Chem.
49
3832-3849
2006
Homo sapiens (P50579), Homo sapiens
brenda
Leszczyniecka, M.; Bhatia, U.; Cueto, M.; Nirmala, N.R.; Towbin, H.; Vattay, A.; Wang, B.; Zabludoff, S.; Phillips, P.E.
MAP1D, a novel methionine aminopeptidase family member is overexpressed in colon cancer
Oncogene
25
3471-3478
2006
Homo sapiens
brenda
Bernier, S.G.; Lazarus, D.D.; Clark, E.; Doyle, B.; Labenski, M.T.; Thompson, C.D.; Westlin, W.F.; Hannig, G.
A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis
Proc. Natl. Acad. Sci. USA
101
10768-10773
2004
Homo sapiens
brenda
Hu, X.; Dang, Y.; Tenney, K.; Crews, P.; Tsai, C.W.; Sixt, K.M.; Cole, P.A.; Liu, J.O.
Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases
Chem. Biol.
14
764-774
2007
Homo sapiens (P50579), Homo sapiens (P53582)
brenda
Sawanyawisuth, K.; Wongkham, C.; Pairojkul, C.; Saeseow, O.T.; Riggins, G.J.; Araki, N.; Wongkham, S.
Methionine aminopeptidase 2 over-expressed in cholangiocarcinoma: potential for drug target
Acta Oncol.
46
378-385
2007
Homo sapiens (P50579), Homo sapiens
brenda
Kass, D.; Bridges, R.S.; Borczuk, A.; Greenberg, S.
Methionine aminopeptidase-2 as a selective target of myofibroblasts in pulmonary fibrosis
Am. J. Respir. Cell Mol. Biol.
37
193-201
2007
Mus musculus (O08663), Rattus norvegicus (P38062), Homo sapiens (P50579)
brenda
Hu, X.; Addlagatta, A.; Matthews, B.W.; Liu, J.O.
Identification of pyridinylpyrimidines as inhibitors of human methionine aminopeptidases
Angew. Chem.
45
3772-3775
2006
Homo sapiens (P50579), Homo sapiens (P53582)
brenda
Upadhya, R.; Zhang, H.S.; Weiss, L.M.
System for expression of microsporidian methionine amino peptidase type 2 (MetAP2) in the yeast Saccharomyces cerevisiae
Antimicrob. Agents Chemother.
50
3389-3395
2006
Escherichia coli, Homo sapiens (P50579), Homo sapiens, Encephalitozoon cuniculi (Q8SR45), Encephalitozoon cuniculi
brenda
Hu, X.V.; Chen, X.; Han, K.C.; Mildvan, A.S.; Liu, J.O.
Kinetic and mutational studies of the number of interacting divalent cations required by bacterial and human methionine aminopeptidases
Biochemistry
46
12833-12843
2007
Escherichia coli, Homo sapiens (Q6UB28), Homo sapiens
brenda
Nonato, M.C.; Widom, J.; Clardy, J.
Human methionine aminopeptidase type 2 in complex with L- and D-methionine
Bioorg. Med. Chem. Lett.
16
2580-2583
2006
Homo sapiens (P50579), Homo sapiens
brenda
Kawai, M.; BaMaung, N.Y.; Fidanze, S.D.; Erickson, S.A.; Tedrow, J.S.; Sanders, W.J.; Vasudevan, A.; Park, C.; Hutchins, C.; Comess, K.M.; Kalvin, D.; Wang, J.; Zhang, Q.; Lou, P.; Tucker-Garcia, L.; Bouska, J.; Bell, R.L.; Lesniewski, R.; Henkin, J.; Sheppard, G.S.
Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties
Bioorg. Med. Chem. Lett.
16
3574-3577
2006
Homo sapiens (P50579)
brenda
Haldar, M.K.; Scott, M.D.; Sule, N.; Srivastava, D.K.; Mallik, S.
Synthesis of barbiturate-based methionine aminopeptidase-1 inhibitors
Bioorg. Med. Chem. Lett.
18
2373-2376
2008
Homo sapiens (P53582), Homo sapiens
brenda
Hannig, G.
Team work in protein processing
Chem. Biol.
14
732-734
2007
Homo sapiens (P50579), Homo sapiens (P53582)
brenda
Kowalinski, E.; Bange, G.; Bradatsch, B.; Hurt, E.; Wild, K.; Sinning, I.
The crystal structure of Ebp1 reveals a methionine aminopeptidase fold as binding platform for multiple interactions
FEBS Lett.
581
4450-4454
2007
Homo sapiens (P50579), Homo sapiens
brenda
Lu, J.; Chong, C.R.; Hu, X.; Liu, J.O.
Fumarranol, a rearranged fumagillin analogue that inhibits angiogenesis in vivo
J. Med. Chem.
49
5645-5648
2006
Homo sapiens (P50579)
brenda
Marino, J.P.; Fisher, P.W.; Hofmann, G.A.; Kirkpatrick, R.B.; Janson, C.A.; Johnson, R.K.; Ma, C.; Mattern, M.; Meek, T.D.; Ryan, M.D.; Schulz, C.; Smith, W.W.; Tew, D.G.; Tomazek, T.A.; Veber, D.F.; Xiong, W.C.; Yamamoto, Y.; Yamashita, K.; Yang, G.; Thompson, S.K.
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore
J. Med. Chem.
50
3777-3785
2007
Homo sapiens (P50579), Homo sapiens
brenda
Tucker, L.A.; Zhang, Q.; Sheppard, G.S.; Lou, P.; Jiang, F.; McKeegan, E.; Lesniewski, R.; Davidsen, S.K.; Bell, R.L.; Wang, J.
Ectopic expression of methionine aminopeptidase-2 causes cell transformation and stimulates proliferation
Oncogene
2008
1-10
2008
Homo sapiens (P50579), Homo sapiens
brenda
Hu, X.; Addlagatta, A.; Lu, J.; Matthews, B.W.; Liu, J.O.
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression
Proc. Natl. Acad. Sci. USA
103
18148-18153
2006
Homo sapiens (P53582), Homo sapiens
brenda
Addlagatta, A.; Matthews, B.W.
Structure of the angiogenesis inhibitor ovalicin bound to its noncognate target, human type 1 methionine aminopeptidase
Protein Sci.
15
1842-1848
2006
Homo sapiens (P50579), Homo sapiens (P53582), Homo sapiens
brenda
Priest, R.C.; Spaull, J.; Buckton, J.; Grimley, R.L.; Sims, M.; Binks, M.; Malhotra, R.
Immunomodulatory activity of a methionine aminopeptidase-2 inhibitor on B cell differentiation
Clin. Exp. Immunol.
155
514-522
2009
Callithrix jacchus, Homo sapiens, Mus musculus
brenda
Warder, S.E.; Tucker, L.A.; McLoughlin, S.M.; Strelitzer, T.J.; Meuth, J.L.; Zhang, Q.; Sheppard, G.S.; Richardson, P.L.; Lesniewski, R.; Davidsen, S.K.; Bell, R.L.; Rogers, J.C.; Wang, J.
Discovery, identification, and characterization of candidate pharmacodynamic markers of methionine aminopeptidase-2 inhibition
J. Proteome Res.
7
4807-4820
2008
Homo sapiens, Mus musculus
brenda
Arico-Muendel, C.C.; Benjamin, D.R.; Caiazzo, T.M.; Centrella, P.A.; Contonio, B.D.; Cook, C.M.; Doyle, E.G.; Hannig, G.; Labenski, M.T.; Searle, L.L.; Lind, K.; Morgan, B.A.; Olson, G.; Paradise, C.L.; Self, C.; Skinner, S.R.; Sluboski, B.; Svendsen, J.L.; Thompson, C.D.; Westlin, W.; White, K.F.
Carbamate analogues of fumagillin as potent, targeted inhibitors of methionine aminopeptidase-2
J. Med. Chem.
52
8047-8056
2009
Homo sapiens
brenda
Alvarado, J.J.; Nemkal, A.; Sauder, J.M.; Russell, M.; Akiyoshi, D.E.; Shi, W.; Almo, S.C.; Weiss, L.M.
Structure of a microsporidian methionine aminopeptidase type 2 complexed with fumagillin and TNP-470
Mol. Biochem. Parasitol.
168
158-167
2009
Homo sapiens, Encephalitozoon cuniculi, Enterocytozoon bieneusi (B7XJ30), Enterocytozoon bieneusi, Enterocytozoon bieneusi H348 (B7XJ30)
brenda
Selvakumar, P.; Lakshmikuttyamma, A.; Das, U.; Pati, H.N.; Dimmock, J.R.; Sharma, R.K.
NC2213: a novel methionine aminopeptidase 2 inhibitor in human colon cancer HT29 cells
Mol. Cancer
8
65
2009
Homo sapiens
brenda
Xiao, Q.; Zhang, F.; Nacev, B.A.; Liu, J.O.; Pei, D.
Protein N-terminal processing: substrate specificity of Escherichia coli and human methionine aminopeptidases
Biochemistry
49
5588-5599
2010
Escherichia coli, Homo sapiens
brenda
Altmeyer, M.A.; Marschner, A.; Schiffmann, R.; Klein, C.D.
Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors
Bioorg. Med. Chem. Lett.
20
4038-4044
2010
Escherichia coli, Homo sapiens, Staphylococcus aureus
brenda
Hou, Y.P.; Sun, J.; Pang, Z.H.; Lv, P.C.; Li, D.D.; Yan, L.; Zhang, H.J.; Zheng, E.X.; Zhao, J.; Zhu, H.L.
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors
Bioorg. Med. Chem.
19
5948-5954
2011
Homo sapiens
brenda
Ma, A.C.; Fung, T.K.; Lin, R.H.; Chung, M.I.; Yang, D.; Ekker, S.C.; Leung, A.Y.
Methionine aminopeptidase 2 is required for hematopoietic stem cell initiation and proliferation
Blood
118
5448-5457
2011
Danio rerio, Homo sapiens
brenda
Chiu, J.; Wong, J.W.; Hogg, P.J.
Redox regulation of methionine aminopeptidase 2 activity
J. Biol. Chem.
289
15035-15043
2014
Homo sapiens (P50579)
brenda
Zhang, F.; Bhat, S.; Gabelli, S.B.; Chen, X.; Miller, M.S.; Nacev, B.A.; Cheng, Y.L.; Meyers, D.J.; Tenney, K.; Shim, J.S.; Crews, P.; Amzel, L.M.; Ma, D.; Liu, J.O.
Pyridinylquinazolines selectively inhibit human methionine aminopeptidase-1 in cells
J. Med. Chem.
56
3996-4016
2013
Homo sapiens (P53582), Homo sapiens
brenda
Heinrich, T.; Buchstaller, H.P.; Cezanne, B.; Rohdich, F.; Bomke, J.; Friese-Hamim, M.; Krier, M.; Knoechel, T.; Musil, D.; Leuthner, B.; Zenke, F.
Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates
Bioorg. Med. Chem. Lett.
27
551-556
2017
Homo sapiens (P50579)
brenda
Arya, T.; Reddi, R.; Kishor, C.; Ganji, R.J.; Bhukya, S.; Gumpena, R.; McGowan, S.; Drag, M.; Addlagatta, A.
Identification of the molecular basis of inhibitor selectivity between the human and streptococcal type I methionine aminopeptidases
J. Med. Chem.
58
2350-2357
2015
Streptococcus pneumoniae (B2IQ22), Homo sapiens (P53582), Homo sapiens, Streptococcus pneumoniae CGSP14 (B2IQ22)
brenda
Van Damme, P.; Hole, K.; Gevaert, K.; Arnesen, T.
N-terminal acetylome analysis reveals the specificity of Naa50 (Nat5) and suggests a kinetic competition between N-terminal acetyltransferases and methionine aminopeptidases
Proteomics
15
2436-2446
2015
Homo sapiens (P50579), Homo sapiens
brenda