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((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
(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
-
-
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
-
(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
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
(3R)-amino-(2S)-hydroxypentanoic acid
-
IC50: 0.0123 mM for the Co2+-substituted enzyme, 0.0115 mM for the Mn2+-substituted enzyme, 0.0093 mM for the Zn2+-substituted enzyme, 0.0223 for the Ni2+-substituted enzyme
(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
-
-
(5,5-Dimethyl-4,5-dihydro-thiazol-2-yl)-(3-methyl-pyridin-2-yl)-amine
-
IC50 for Co-EcMetAP1: 0.00021 mM
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
(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-(1H-benzimidazol-2-yl)thiourea
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylmorpholin-4-yl)ethanone
-
-
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylphenyl)ethanone
-
-
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-fluoro-2-sulfanylphenyl)ethanone
-
-
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-methoxy-2-sulfanylphenyl)ethanone
-
-
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
1-benzyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
1-benzyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
1-benzyl-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00099 mM
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-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
1-phenyl-2,4-dithiobiuret
-
1-[2-pyridin-2-yl-6-(trifluoromethyl)-3,4-dihydropyrimidin-4-yl]propane-2-thiol
-
-
2,2'-bipyridine
-
maximum inhibition is observed in the presence of CoCl2 rather than other metal ions
2-((1,3-thiazol-2-ylamino)carbonyl)pyridin-3-yl phenylacetate
-
Co(II)-form of enzyme, 50% inhibition at 0.00046 mM
2-((1H-1,2,4-triazol-5-ylthio)methyl)benzonitrile
-
Co(II)-form of enzyme, 50% inhibition at 0.00066 mM
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
Co(II)-form of enzyme, 50% inhibition at 0.00172 mM
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-(1H-benzimidazol-2-yl)pyridin-3-ol
2-(1H-benzimidazol-2-ylamino)pyridin-3-ol
Co(II)-form of enzyme, 50% inhibition at 0.00078 mM
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-(2-aminoethoxy)-3-ethyl-6-[[(2-propylphenyl)sulfonyl]amino]benzoic acid
-
2-(2-aminoethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
2-(2-aminoethoxy)-6-[([2-[3-(diethylamino)propyl]-4-fluorophenyl]sulfonyl)amino]-3-ethylbenzoic acid
-
2-(3H-pyrrol-5-yl)-1H-imidazo(4,5-b)pyridine
Co(II)-form of enzyme, 50% inhibition at 0.000078 mM
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-(carboxymethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
2-(prop-1-en-2-yl)-5-[2-(trifluoromethyl)phenyl]furan
-
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-amino-4-(methylthio)-1-(1,3-thiazol-2-yl)butan-1-one
50% inhibition at 0.019 mM, formation of uncleavable tetrahedral intermediate upon binding
2-amino-4-(methylthio)-1-pyridin-2-ylbutan-1-one
50% inhibition at 0.016 mM, formation of uncleavable tetrahedral intermediate upon binding
2-butyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
2-chloro-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
2-ethenyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
2-ethoxy-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
2-ethyl-1-phenyl-2-isodithiobiuret
-
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methoxybenzoic acid
-
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
2-hydroxy-1-naphthaldehyde isonicotinoyl hydrazone
-
inhibitor of HIV-1 replication and transcription, and potent and selective inhibitor of isoforms MetAP1a and MetAP1c. The inhibitor is active against replicating and aged non-growing Micobacterium tuberculosis at low micromolar concentrations
2-hydroxy-4-(2-methyl-1,3-thiazol-4-yl)benzamide
-
-
2-hydroxyethyl disulfide
inhibition is through covalent modifiction of residue C105
2-methyl-6-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 6 nM
2-pyridin-2-yl-1H-benzimidazol-5-amine
Co(II)-form of enzyme, 50% inhibition at 0.0097 mM
2-pyridin-2-yl-1H-benzimidazole-5-carbonitrile
Co(II)-form of enzyme, 50% inhibition at 0.00043 mM
2-pyridin-2-yl-1H-imidazo(4,5-b)pyrazine
Co(II)-form of enzyme, 50% inhibition at 0.00024 mM
2-pyridin-2-yl-1H-imidazo(4,5-b)pyridine
Co(II)-form of enzyme, 50% inhibition at 0.00011 mM
2-pyridin-2-yl-1H-imidazo(4,5-c)pyridine
Co(II)-form of enzyme, 50% inhibition at 0.00055 mM
2-pyridin-2-yl-4-(trifluoromethyl)-6-[2-(trifluoromethyl)benzyl]-1,6-dihydropyrimidine
-
-
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
-
2-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
potent inhibitor but lacks cellular activity and is highly protein bound
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
-
2-[([4-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]phenyl]sulfinyl)oxy]hydrazinecarboximidamide
-
-
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
-
IC50 for Co-EcMetAP1: 0.0296 mM, IC50 for Mn-EcMetAPa: 0.0441 mM, IC50 for Zn-EcMetAP1: 0.0365 mM
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
-
IC50 for Co-EcMetAP1: 0.0286 mM, IC50 for Mn-EcMetAPa: 0.0443 mM, IC50 for Zn-EcMetAP1: 0.0498 mM, IC50 for Ni-EcMetAP1: 0.0357 mM
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
-
IC50 for Co-EcMetAP1: 0.0229 mM, IC50 for Mn-EcMetAPa: 0.0252 mM, IC50 for Zn-EcMetAP1: 0.0167 mM, IC50 for Ni-EcMetAP1: 0.0125 mM
2-[4-(2-Cyano-2-ethoxycarbonyl-1-methyl-vinyl)-phenyl]-1,3-dioxo-2,3-dihydro-1H-isoindole-5-carboxylic acid
-
IC50 for Co-EcMetAP1: 0.037 mM
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
-
3,8-dihydroindeno(1,2-d)(1,2,3)triazole
-
Co(II)-form, Ki,app-value 52 nM
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
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000019 mM; 50% inhibition of enzyme at 0.000027 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
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
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000049 mM; 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; 50% inhibition of enzyme at 0.000028 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000033 mM
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
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.014 mM; 50% inhibition of enzyme at 0.00018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0083 mM
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-(((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-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-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
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-((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-((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-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-methyl-1,3-thiazol-4-yl)phenol
-
-
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(anilino)-5-(3-methyl-2-butenylthio)-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-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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-(N-methyl-anilino)-5-benzylthio-1,2,4-triazole
-
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-acetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0082 mM
3-amino-1-(cyclopropylamino)heptan-2 -one
50% inhibition at 0.007 mM, formation of uncleavable tetrahedral intermediate upon binding
3-aminopyridine-2-carboxylic acid thiazol-2-ylamide
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-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Co-EcMetAP1: 0.0001 mM, IC50 for Mn-EcMetAPa: 0.0233 mM, IC50 for Zn-EcMetAP1: 0.0224 mM, IC50 for Ni-EcMetAP1: 0.00076 mM
3-ethyl-2-methoxy-6-[[(2-[[2-(1-methylpyrrolidin-2-yl)ethyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
3-ethyl-2-methoxy-6-[[(2-[[3-(2-methylpiperidin-1-yl)propyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
3-ethyl-2-methyl-6-[(pyridin-2-ylsulfonyl)amino]benzoic acid
-
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
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-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
3-imino-4-[(E)-(4-methoxyphenyl)diazenyl]-3H-pyrazol-5-amine
-
-
3-imino-4-[(E)-[2-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
-
-
3-imino-4-[(E)-[3-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
-
-
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 52 nM
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]-2-hydroxybenzoic acid
-
-
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]benzoic acid
-
-
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-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
-
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-(((3-((2-methoxyphenoxy)methyl)-1H-1,2,4-triazol-5-yl)sulfanyl)acetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one
-
Co(II)-form of enzyme, 50% inhibition at 0.00099 mM
4-(1,3-thiazol-2-yl)benzene-1,2-diol
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(1-methyl-1H-imidazol-2-yl)benzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
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-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
4-(2-amino-1,3-thiazol-4-yl)benzene-1,2-diol
-
-
4-(2-aminothiazol-4-yl)benzene-1,2-diol
specific inhibition of Fe2+-loaded MetAP
4-(2-methyl-1,3-thiazol-4-yl)-2-nitroaniline
-
-
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diamine
-
-
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,3-diol
-
-
4-(3,4-dimethoxyphenyl)-2-methyl-1,3-thiazole
-
-
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol
-
4-(3-butylthiophen-2-yl)benzene-1,2-diol
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
4-(3-methylthiophen-2-yl)benzene-1,2-diol
4-(3-propylthiophen-2-yl)benzene-1,2-diol
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
4-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
-
-
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
4-(5-fluoropyrimidin-2-yl)benzene-1,2-diol
-
does only inhibit Fe2+- or Co2+-activated MetAP enzymes, but not Mn2+-activated MetAP enzyme
4-(5-methoxy-1,3-oxazol-2-yl)benzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(5-methoxy-2-phenyl-3,4-dihydropyrimidin-4-yl)morpholine
-
-
4-(5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
-
-
4-(5-methylthiophen-2-yl)benzene-1,2-diol
4-(thiophen-2-yl)benzene-1,2-diol
4-(thiophen-3-yl)benzene-1,2-diol
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-pyridin-2-ylbenzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-pyrimidin-2-ylbenzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-[(E)-(3-chloro-2-methylphenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
-
-
4-[(E)-(3-fluorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
-
-
4-[(E)-(4-chlorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
-
-
4-[(E)-(4-fluorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
-
-
4-[3-(2-bromoethyl)thiophen-2-yl]benzene-1,2-diol
-
-
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
5,5'-dithiobis(2-nitrobenzoic acid)
inhibition is through covalent modifiction of residue C105
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
5,6-dimethyl-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00243 mM
5-((R)-1-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline
-
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-(2,3-dichlorophenyl)furan-2-carboxylic acid
-
-
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
-
-
5-(2,3-dimethoxyphenyl)thiophene-2-carboxylic acid
-
-
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
-
-
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
-
-
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
-
-
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
-
-
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
-
-
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
-
-
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
-
-
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
-
-
5-(2-(trifluoromethyl)phenyl)-2-furoic acid
-
Co(II)-form of enzyme, 50% inhibition at 0.073 mM, Mn(II)-form, 50% inhibition at 0.000063 mM, Ni-(II)form, 50% inhibition above 200 mM, Fe-(II)form, 50% inhibition at 0.195 mM
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
-
-
5-(2-chloro-3-methylphenyl)-2-furoic acid
-
Co(II)-form of enzyme, 50% inhibition at 0.069 mM, Mn(II)-form, 50% inhibition at 0.00096 mM, Ni-(II)form, 50% inhibition above 200 mM, Fe-(II)form, 50% inhibition above 200 mM
5-(2-chloro-4-nitrophenyl)furan-2-carboxylic acid
-
5-(2-chlorobenzyl)furan-2-carboxylic acid
-
5-(2-chlorophenyl)-2-furohydrazide
-
-
5-(2-chlorophenyl)-2-furoic acid
-
Co(II)-form of enzyme, 50% inhibition at 0.154 mM, Mn(II)-form, 50% inhibition at 0.0024 mM, Ni-(II)form, 50% inhibition above 200 mM, Fe-(II)form, 50% inhibition at 0.186 mM
5-(2-chlorophenyl)-N-(2-methoxybenzyl)furan-2-carboxamide
-
-
5-(2-chlorophenyl)-N-(3-fluorophenyl)furan-2-carboxamide
-
-
5-(2-chlorophenyl)-N-hexylfuran-2-carboxamide
-
-
5-(2-chlorophenyl)-N-phenethylfuran-2-carboxamide
-
-
5-(2-chlorophenyl)-N-phenylfuran-2-carboxamide
-
-
5-(2-chlorophenyl)furan-2-carbohydrazide
-
5-(2-chlorophenyl)furan-2-carboxylic acid
5-(2-ethoxyphenyl)furan-2-carboxylic acid
-
-
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
-
-
5-(2-fluorophenyl)-2-furoic acid
-
Co(II)-form of enzyme, 50% inhibition at 0.198 mM, Mn(II)-form, 50% inhibition at 0.014 mM, Ni-(II)form, 50% inhibition above 200 mM, Fe-(II)form, 50% inhibition above 200 mM
5-(2-methoxyphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 150 nM
5-(2-methoxyphenyl)furan-2-carboxylic acid
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
-
-
5-(2-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 112 nM
5-(2-methylphenyl)furan-2-carboxylic acid
-
-
5-(2-methylphenyl)thiophene-2-carboxylic acid
-
-
5-(2-nitrophenyl)furan-2-carboxylic acid
-
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-(3,4-dihydroxyphenyl)-2-methyl-N-(propan-2-yl)-1,3-thiazole-4-carboxamide
-
-
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide
specific inhibition of Fe2+-loaded MetAP
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
5-(3-bromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 4 nM
5-(3-chlorophenyl)-2-furoic acid
-
Co(II)-form of enzyme, 50% inhibition at 0.193 mM, Mn(II)-form, 50% inhibition at 0.019 mM, Ni-(II)form, 50% inhibition above 200 mM, Fe-(II)form, 50% inhibition above 200 mM
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-methylnaphthalen-1-yl)-N-phenethylfuran-2-carboxamide
-
-
5-(4-methylnaphthalen-1-yl)-N-phenylfuran-2-carboxamide
-
-
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
-
-
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-(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-(biphenyl-4-yl)-N-(2,4-dimethylphenylsulfonyl)furan-2-carboxamide
-
-
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-biphenyl-2-yl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value above 1000 nM
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
-
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
-
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-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00169 mM
5-chloro-4,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
-
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
-
5-chloro-4-methyl-6-(4-methylbenzyl)-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
5-chloro-6-(2-ethylphenyl)-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
highly selective inhibitor
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-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
5-ethyl-2-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
5-fluoro-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00151 mM
5-methoxy-2-phenyl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
-
5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-ol
-
-
5-methoxy-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
-
-
5-methoxy-6,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
5-methoxy-6-methyl-2-phenyl-1,6-dihydropyrimidine
-
-
5-methoxy-6-methyl-6-phenyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
5-methoxy-6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
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-(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-methyl-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00209 mM
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
-
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
5-nitro-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00016 mM
5-phenyl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 70 nM
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
5-tert-butyl-2-pyridin-2-yl-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00260 mM
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
5-[(2E)-hepta-2,6-dien-4-yn-1-ylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
5-[(4-methylbenzyl)sulfanyl]-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-(trifluoromethoxy)phenyl]furan-2-carboxylic acid
-
5-[2-(trifluoromethyl)phenyl]furan-2-carboxylic acid
5-[[(2-methyl-2,5-dihydro-1,3-thiazol-4-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
5-[[(4-chlorophenyl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
most potent compound in the host-cell viability assay
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-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
6-(1H-benzimidazol-2-ylamino)pyridin-2-ol
Co(II)-form of enzyme, 50% inhibition at 0.00134 mM
6-(2-chlorobenzyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
-
6-(4-methylnaphthalen-1-yl)-N-phenethylpicolinamide
-
-
6-(benzylsulfanyl)-5-chloro-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
6-(phenylsulfanyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
-
6-benzyl-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
-
6-benzyl-5-chloro-4-methyl-2-pyridin-3-yl-1,6-dihydropyrimidine
-
-
6-bromo-N-phenethylpicolinamide
-
-
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
-
6-[(2,4-dichlorophenyl)sulfanyl]-5-methoxy-2-pyridin-2-yl-1,6-dihydropyrimidine
-
-
6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
-
-
6-[([2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-ethyl-2-methoxybenzoic acid
-
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-(1H-imidazol-4-yl)-3-methoxybenzoic acid
-
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-2-yl-3-methoxybenzoic acid
-
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
-
6-[[(2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-furan-3-yl-2-methoxybenzoic acid
-
6-[[(2-[[3-(dimethylamino)propyl]amino]-4-fluorophenyl)sulfonyl]amino]-3-furan-3-yl-2-methoxybenzoic acid
-
6-[[(2-[[4-(dimethylamino)butyl]amino]phenyl)sulfonyl]amino]-3-ethyl-2-methoxybenzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-2,3-dimethylbenzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(1-hydroxyethyl)-3-methylbenzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(hydroxymethyl)-3-methylbenzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-2-methoxy-3-(1H-pyrazol-4-yl)benzoic acid
-
6-[[(4-fluorophenyl)sulfonyl]amino]-3-methyl-2-propylbenzoic acid
-
7-amino-4-methylcoumarin
-
product inhibition
8-(pyridin-2-yl)-7H-purine
8-pyridin-2-yl-7H-purine
Co(II)-form of enzyme, 50% inhibition at 0.00038 mM
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+
bengamide B
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide E
nonspecific inhibitor
bengamide G
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide L
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide M
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide N
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide O
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
butaneboronic acid
-
substrate analog
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate
-
DTNB
-
the enzyme is fully reactivated when incubated with tris(2-carboxyethyl)-phosphine hydrochloride
E-64
1 mM, 89.1% of initial activity
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
ethyl 5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxylate
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
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
imidazo[2,1-a]isoquinoline-2-carbohydrazide
-
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-methionine
weak, competitive
L-Nle
-
product inhibition
LAF 389
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
MCB2379
-
IC50: 599 nM in presence of Co2+, 1455 nM in presence of Zn2+
MCB2813
-
IC50: 43.7 nM in presence of Co2+, 300 nM in presence of Zn2+
methionine
feedback inhibition. 70% inhibition at 0.1 mM
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
-
methyl N-[(2S,3R)-3-amino-2-hydroxy-3-(4-methylphenyl)propanoyl]-L-alanylleucinate
-
-
methyl N-[(2S,3R)-3-amino-2-hydroxy-3-[4-(1-methylethyl)phenyl]propanoyl]-L-alanylleucinate
-
-
methyl N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-serylleucinate
-
-
methyl [[(2S)-2-([(2S,3R)-3-amino-2-hydroxy-3-[4-(trifluoromethyl)phenyl]propanoyl]amino)propanoyl]amino]acetate
-
-
Mg2+
-
1.0 mM MgCl2, 21% 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)-1H-benzimidazol-2-amine
N-(1,3-thiazol-2-yl)-3-[(N-[2-[2-(2-[2-[(1H-triaziren-1-ylacetyl)amino]ethoxy]ethoxy)ethoxy]-4-[3-(trifluoromethyl)-3H-diaziren-3-yl]benzoyl]glycyl)amino]pyridine-2-carboxamide
-
-
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-2-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
-
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-3-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
-
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-4-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
-
-
N-(2-methoxybenzyl)-6-(4-methylnaphthalen-1-yl)picolinamide
-
-
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-(3-fluorophenyl)-5-o-tolylfuran-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-(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-(2-(trifluoromethyl)phenyl)furan-2-carboxamide
-
-
N-(4-methoxyphenyl)-5-(4-methylnaphthalen-1-yl)furan-2-carboxamide
-
-
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-chloroquinolin-8-yl)benzenesulfonamide
Co(II)-form of enzyme, 50% inhibition at 0.00169 mM, Mn(II)-form, 50% inhibition at 0.0185 mM, Fe(II)-form, at 0.0138 mM, Ni(II)-form, at 0.00742 mM, Zn(II)-form, at 0.0113 mM
N-(5-chloroquinolin-8-yl)methanesulfonamide
Co(II)-form of enzyme, 50% inhibition at 0.000154 mM, Mn(II)-form, 50% inhibition at 0.00164 mM, Fe(II)-form, at 0.00393 mM, Ni(II)-form, at 0.000171 mM, Zn(II)-form, at 0.000806 mM; inhibits the Co(II)- and Ni(II)-forms of MetAP potently
N-(5-methyl-1,2-oxazol-3-yl)pyridine-2-carboxamide
-
-
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-(pyridin-2-ylmethyl)-N'-(1,3-thiazol-2-yl)ethanediamide
-
-
N-(pyridin-2-ylmethyl)-N'-1,3-thiazol-2-ylethanediamide
N-(quinolin-8-yl)benzenesulfonamide
N-(quinolin-8-yl)methanesulfonamide
N-1,3-thiazol-2-yl-1H-benzimidazol-2-amine
Co(II)-form of enzyme, 50% inhibition at 0.00054 mM
N-1,3-thiazol-2-yl-3-(N-[(2-2-[(1H-triaziren-1-ylacetyl)amino]ethoxy]-4-[[3-(trifluoromethyl)-[3H-diaziren-3-yl]phenyl)carbonyl]glycyl]amino)pyridine-2-carboxamide
-
-
N-1,3-thiazol-2-ylpyridine-2-carboxamide
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
N-benzyl-3-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 29 nM
N-benzyl-5-(2-ethoxyphenyl)furan-2-carboxamide
-
-
N-benzyl-5-(4-methylnaphthalen-1-yl)furan-2-carboxamide
-
-
N-benzyl-6-(4-methylnaphthalen-1-yl)picolinamide
-
-
N-benzyl-6-bromopicolinamide
-
-
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-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxamide
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
-
-
N-cyclobutyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
-
-
N-cyclopentyl-5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxamide
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
N-cyclopentyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
-
-
N-cyclopentyl-N'-(1,3-thiazol-2-yl)ethanediamide
-
-
N-cyclopentyl-N'-1,3-thiazol-2-ylethanediamide
N-cyclopentyl-N-(thiazol-2-yl)oxalamide
potent and selective inhibitor
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
N-cyclopropyl-5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxamide
-
-
N-cyclopropyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
N-ethylmaleimide
1 mM, 90% inhibition. Inhibition is through covalent modifiction of residue C105
N-hexyl-5-(4-methylnaphthalen-1-yl)furan-2-carboxamide
-
-
N-hexyl-6-(4-methylnaphthalen-1-yl)picolinamide
-
-
N-isobutyl-N'-1,3-thiazol-2-ylethanediamide
-
Co(II)-form of enzyme, 50% inhibition at 0.00028 mM, Mn(II)-form, 50% inhibition at 0.108 mM, Ni-(II)form, 50% inhibition at 0.0034 mM, Fe-(II)form, 50% inhibition at 0.118 mM
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
N-pyrazin-2-yl-1H-benzimidazol-2-amine
Co(II)-form of enzyme, 50% inhibition at 0.0046 mM
N-pyridin-2-yl-1H-benzimidazol-2-amine
Co(II)-form of enzyme, 50% inhibition at 0.00057 mM
N-quinolin-8-ylmethanesulfonamide
Co(II)-form of enzyme, 50% inhibition at 0.000137 mM, Mn(II)-form, 50% inhibition at 0.00214 mM, Fe(II)-form, at 0.00374 mM, Ni(II)-form, at 0.000184 mM, Zn(II)-form, at 0.00111 mM
N-[4-(2-methyl-1,3-thiazol-4-yl)-2-nitrophenyl]acetamide
-
-
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
-
nitrilotriacetic acid
-
-
phenyl(2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl)methanone
Co(II)-form of enzyme, 50% inhibition at 0.00240 mM
phenyl(2-pyridin-2-yl-1H-benzimidazol-5-yl)methanone
Co(II)-form of enzyme, 50% inhibition at 0.00040 mM
phenylmethylsulfonyl fluoride
-
29.4% relative activity at 5 mM
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
PMSF
1 mM, 82.8% of initial activity
Pyridine-2-carboxylic acid thiazol-2-ylamide
quinolin-8-yl 4-methylbenzenesulfonate
-
-
quinolin-8-yl benzenesulfonate
-
-
quinolin-8-yl benzoate
-
-
tert-butyl [2-(4,5-dihydro-1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate
-
XC-11
-
a pyridinyl-pyrimidine inhibitor selective for MetAP1b
[(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, potent irreversible inhibitor
[(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
[(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
[amino(cyclohexyl)methyl]phosphonic acid
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
A-311263, the inhibitor has little or no preference for the type of divalent metal ion that occupies the active site of MetAP
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
A-311263, the inhibitor has little or no preference for the type of divalent metal ion that occupies the active site of MetAP
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
-
IC50: 0.0229
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
-
IC50: 0.095 mM
1,10-phenanthroline
-
-
1-(1H-benzimidazol-2-yl)thiourea
Co(II)-form of enzyme, 50% inhibition at 0.0089 mM
1-(1H-benzimidazol-2-yl)thiourea
-
-
1-(1H-benzimidazol-2-yl)thiourea
-
-
1-benzyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00046 mM
1-benzyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00050 mM
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
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-2-yl)-1H-imidazo[4,5-b]pyridine
-
-
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
Co(II)-form of enzyme, 50% inhibition at 0.00339 mM
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
-
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
-
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
-
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(1H-benzimidazol-2-yl)pyridin-3-ol
-
-
2-(1H-benzimidazol-2-yl)pyridin-3-ol
-
-
2-(pyrazin-2-yl)-1H-benzimidazole
-
-
2-(pyrazin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
-
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
-
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
-
2-(pyridin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazole
-
-
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
-
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
-
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]pyrazine
-
-
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-b]pyridine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-mercaptoethanol
-
complete inhibition at 10 mM
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
A-310840, the inhibitor binds to the Co2+-loaded enzyme well but is approximately 23fold less potent for Mn2+-loaded MetAP
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
A-310840
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000034 mM
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00492
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00034 mM; IC50: 0.00054 mM
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
-
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00068 mM
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00078 mM
3-(2-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0016 mM
3-(2-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
0.015 mM
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00028 mM
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00083 mM
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.016 mM
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0013 mM
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00089 mM
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0017 mM
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00055 mM
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00028 mM
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0109 mM
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0044 mM
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00039 mM
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
-
IC50: 0.0021 mM; IC50 above 0.1 mM
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
-
-
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0025 mM
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0034 mM
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00071 mM
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000095 mM
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0017 mM
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00302 mM
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00022 mM
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00077 mM
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0026 mM
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00049 mM
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00015 mM
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00467
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0006 mM
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00136 mM
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0011 mM
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.062 mM
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00024 mM
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00014 mM
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000671 mM
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00031 mM
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00013 mM
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00038 mM
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00087 mM
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00239 mM
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00032 mM
3-aminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 1.7 mM, IC50: 0.0328 mM
3-aminopyridine-2-carboxylic acid thiazol-2-ylamide
-
-
3-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00089 mM
3-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC5ß0 above 0.1 mM
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00122 mM
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00103 mM
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00033 mM
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00032
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000038 mM
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00062 mM
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00102 mM
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000174 mM
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00187 mM
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00486 mM
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00192 mM
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0537
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00004 mM
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00082 mM
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000054 mM
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0002 mM
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00026 mM
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00035 mM
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0054 mM
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00038 mM
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00018 mM
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00335 mM
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
-
-
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
-
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0021 mM
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0099 mM
4-(1,3-thiazol-2-yl)benzene-1,2-diol
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(1,3-thiazol-2-yl)benzene-1,2-diol
-
-
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
-
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
-
-
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
specific inhibition of Fe2+-loaded MetAP
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
-
-
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
-
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
-
-
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
-
-
4-(3-butylthiophen-2-yl)benzene-1,2-diol
-
4-(3-butylthiophen-2-yl)benzene-1,2-diol
-
-
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
-
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
-
-
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
does only inhibit Fe2+-activated MetAP enzyme, but not Mn2+- or Co2+-activated MetAP enzymes
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
-
4-(3-methylthiophen-2-yl)benzene-1,2-diol
-
-
4-(3-propylthiophen-2-yl)benzene-1,2-diol
-
4-(3-propylthiophen-2-yl)benzene-1,2-diol
-
-
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
-
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
-
-
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
-
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
-
-
4-(5-methylthiophen-2-yl)benzene-1,2-diol
-
4-(5-methylthiophen-2-yl)benzene-1,2-diol
-
-
4-(thiophen-2-yl)benzene-1,2-diol
-
4-(thiophen-2-yl)benzene-1,2-diol
-
-
4-(thiophen-3-yl)benzene-1,2-diol
-
4-(thiophen-3-yl)benzene-1,2-diol
-
-
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
-
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
potent and selective inhibitor
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
-
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
-
-
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
-
-
5-(2-chlorophenyl)furan-2-carboxylic acid
-
5-(2-chlorophenyl)furan-2-carboxylic acid
-
5-(2-chlorophenyl)furan-2-carboxylic acid
-
-
5-(2-chlorophenyl)furan-2-carboxylic acid
-
-
5-(2-methoxyphenyl)furan-2-carboxylic acid
-
5-(2-methoxyphenyl)furan-2-carboxylic acid
-
-
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
-
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
-
-
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00515 mM
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00431 mM
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00716 mM
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00122 mM
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Co(II)-form of enzyme, 50% inhibition at 0.00391 mM
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
5-[2-(trifluoromethyl)phenyl]furan-2-carboxylic acid
potent and selective inhibitor
5-[2-(trifluoromethyl)phenyl]furan-2-carboxylic acid
-
6-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
-
-
6-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
-
-
8-(pyridin-2-yl)-7H-purine
-
-
8-(pyridin-2-yl)-7H-purine
-
-
8-hydroxy quinoline
-
-
A-357300
-
reversible
A-357300
-
potent MetAP2 inhibitor
A-357300
-
potent MetAP2 inhibitor
A-800141
-
A-800141
-
potent MetAP2 inhibitor
A-800141
-
potent MetAP2 inhibitor
actinonin
0.01 mM, 40% loss of activity; 0.01 mM, 70% loss of activity
actinonin
-
12.6% relative activity at 0.05 mM
amastatin
1 mM, 37.6% of initial activity
amastatin
-
29.7% relative activity at 0.05 mM
bengamide A
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide A
nonspecific, reversible inhibitor of MetAP-1 and MetAP-2; nonspecific, reversible inhibitor of MetAP-1 and MetAP-2
bestatin
1 mM, 35.9% of initial activity
bestatin
0.01 mM, 25% loss of activity; 0.01 mM, 50% loss of activity
bestatin
-
44.9% relative activity at 0.05 mM
Ca2+
-
50% inhibition at 2 mM, 52% inhibition at 4 mM
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
Co2+
-
inhibitory above 0.0625 mM, activating below
Cu2+
-
52% inhibition at 2 mM, 88% inhibition at 4 mM
EDTA
1 mM, 37.8% of initial activity
EDTA
-
33.7% relative activity at 100 mM, the enzyme activity inhibited by 1 mM EDTA is restored in presence of 5 mM Mg2+
EDTA
1 mM, about 10% residual activity. The aminopeptidase activity of the EDTA-inactivated enzyme is successfully restored by Mn2+
Fe2+
-
1 mM, complete inhibition
fumagillin
specific inhibitor
fumagillin
selectively inhibits MetAP2
fumagillin
-
binding structure, overview
fumagillin
binding structure, overview. Fumagillin and its analogues show inhibitory activity in vitro and in animal models of microsporidiosis and human infections due to Enterocytozoon bieneusi
fumagillin
-
fumagillin covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase
fumagillin
-
IC50 above 0.1 mM
fumagillin
Co(II)-form of enzyme, 50% inhibition at 0.000915 mM
fumagillin
-
selectively inhibits MetAP2
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
-
inhibition of type II enzyme
fumagillin
MetAP2-specific inhibitor
fumagillin
irreversible inhibition
fumagillin
selectively inhibits MetAP2
fumagillin
higher affinity to MetAP2 than to MetAP1; 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
fumagillin
irreversible inhibition
fumagillin
-
potent MetAP2 inhibitor
fumagillin
-
targets MetAP2, no binding to MetAP1 isozymes
fumagillin
irreversible inhibition
fumagillin
-
IC50 above 0.1 mM
fumarranol
selective inhibitor
fumarranol
-
binds to MetAP2 noncovalently and reversibly
Hg2+
-
1 mM, complete inhibition
IV-43
MetAP1-specific inhibitor
IV-43
reversible MetAP-1 inhibitor
L-MetStaCys
-
-
L-MetStaVal
-
-
Mn2+
-
1 mM, complete inhibition
Mn2+
-
0.1 mM MnCl2, 26% inhibition. 5.0 mM, 36% inhibition
N-(1,3-thiazol-2-yl)-1H-benzimidazol-2-amine
-
-
N-(1,3-thiazol-2-yl)-1H-benzimidazol-2-amine
-
-
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
-
-
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
-
-
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
-
-
N-(pyridin-2-ylmethyl)-N'-1,3-thiazol-2-ylethanediamide
-
Co(II)-form of enzyme, 50% inhibition at 0.000073 mM, Mn(II)-form, 50% inhibition at 0.043 mM, Ni-(II)form, 50% inhibition at 0.002 mM, Fe-(II)form, 50% inhibition at 0.065 mM
N-(pyridin-2-ylmethyl)-N'-1,3-thiazol-2-ylethanediamide
-
-
N-(quinolin-8-yl)benzenesulfonamide
-
-
N-(quinolin-8-yl)benzenesulfonamide
-
-
N-(quinolin-8-yl)benzenesulfonamide
-
-
N-(quinolin-8-yl)methanesulfonamide
inhibits the Co(II)- and Ni(II)-forms of MetAP potently
N-(quinolin-8-yl)methanesulfonamide
-
a trimetalated enzyme, forms a complex with the enzyme, cuases bacterial growth inhibition of strains AS19, D22 and SM101 by targeting MetAP by recruitment of a third auxiliary metal, binding structure, overview
N-1,3-thiazol-2-ylpyridine-2-carboxamide
Co(II)-form of enzyme, 50% inhibition at 0.000063 mM, binds to an additional Co2+ ion at the entrance of the active site
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-1,3-thiazol-2-ylpyridine-2-carboxamide
-
Co(II)-form of enzyme, 50% inhibition at 0.0071 mM
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
-
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
-
-
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
-
-
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
-
-
N-cyclopentyl-N'-1,3-thiazol-2-ylethanediamide
-
Co(II)-form of enzyme, 50% inhibition at 0.000067 mM, Mn(II)-form, 50% inhibition at 0.053 mM, Ni-(II)form, 50% inhibition at 0.001 mM, Fe-(II)form, 50% inhibition at 0.046 mM
N-cyclopentyl-N'-1,3-thiazol-2-ylethanediamide
-
-
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
specific inhibition of Fe2+-loaded MetAP
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
-
-
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
-
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
-
-
Ni2+
-
1 mM, complete inhibition
ovalicin
-
covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase
ovalicin
-
inhibition of type II enzyme
ovalicin
MetAP2-specific inhibitor
ovalicin
higher affinity to MetAP2 than to MetAP1; lower affinity to MetAP1 than to MetAP2
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
-
-
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
-
-
PPI-2458
-
PPI-2458
potent selective inhibitor of MetAP2
PPI-2458
-
1-10 nM, selective non-reversible inhibition of MetAP-2
PPI-2458
-
potent inhibitor, 80% inhibition at 100 mg/kg
Pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Co-EcMetAP1: 0.0013 mM
Pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.005 mM
Pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.007 mM
thiabendazole
Co(II)-form of enzyme, 50% inhibition at 0.00047 mM, binds to an additional Co2+ ion at the entrance of the active site
TNP-470
specific inhibitor
TNP-470
-
binding structure, overview
TNP-470
binding structure, overview
TNP-470
is likely to inhibit the enzyme by occupying the active site in the same fashion as fumagillin
TNP-470
-
inhibition of type II enzyme
TNP-470
MetAP2-specific inhibitor
TNP-470
selective covalent MetAP-2 inhibitor
TNP-470
potent selective inhibitor of MetAP2
TNP-470
irreversible inhibitor
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
TNP-470
treatment inhibits programmed cell death in miltefosine-treated promastigotes. It inhibits the biochemical features of metazoan apoptosis, including caspase3/7 protease like activity, oligonucleosomal DNA fragmentation, collapse of mitochondrial transmembrane potential, and increase in cytosolic pool of calcium ions but does not prevent the cell death and phosphatidyl serine externalization
TNP-470
-
potent MetAP2 inhibitor
TNP-470
-
a fumagillin derivative, targets MetAP2, no binding to MetAP1 isozymes
Zn2+
-
71% inhibition at 5 mM
Zn2+
-
0.1 mM, complete inhibition
Zn2+
-
inhibitory above 0.031 mM, activating below
[(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
[(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, 5 mg/kg
[(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
[(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
[(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
[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
additional information
one of the protomeric states of the enzyme is relevant for inhibitor binding, whereas the other is relevant for substrate hydrolysis
-
additional information
thiabendazole and its derivatives are potent inhibitors in vitro, but fail to inhibit in vivo because they bind as Co2+-complexes to H79, thus blocking the active site of enzyme. In the in vitro assay the metal ion concentration is considerably higher than under in vivo conditions
-
additional information
-
thiabendazole and its derivatives are potent inhibitors in vitro, but fail to inhibit in vivo because they bind as Co2+-complexes to H79, thus blocking the active site of enzyme. In the in vitro assay the metal ion concentration is considerably higher than under in vivo conditions
-
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
-
additional information
-
a set of inhibitors displayed completely different inhibitory profiles on the two mycobacterial MetAPs in both potency and metalloform selectivity
-
additional information
identification of inhibitors with high selectivity toward the Fe(II)-form, the Mn(II)-form, or the Co(II) and Ni(II) forms of the enzyme, respectively, overview. Binding structure of inhibitors in the active site of isozyme MetAP1c, overview
-
additional information
-
identification of inhibitors with high selectivity toward the Fe(II)-form, the Mn(II)-form, or the Co(II) and Ni(II) forms of the enzyme, respectively, overview. Binding structure of inhibitors in the active site of isozyme MetAP1c, overview
-
additional information
-
identification of pyridinyl-pyrimidine inhibitors with selectivity to isozyme MetAP1b before MetAP1a and MetAP1c
-
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0.02 - 0.034
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
0.0013 - 0.179
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
0.00054 - 0.075
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
0.00076 - 0.201
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
0.00062 - 0.12
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
0.0002 - 0.08
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
0.0004 - 0.15
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
0.00096 - 0.187
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
0.0229 - 0.095
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
0.0123
(3R)-amino-(2S)-hydroxypentanoic acid
Escherichia coli
-
IC50: 0.0123 mM for the Co2+-substituted enzyme, 0.0115 mM for the Mn2+-substituted enzyme, 0.0093 mM for the Zn2+-substituted enzyme, 0.0223 for the Ni2+-substituted enzyme
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
0.00021
(5,5-Dimethyl-4,5-dihydro-thiazol-2-yl)-(3-methyl-pyridin-2-yl)-amine
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.00021 mM
0.000027
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Homo sapiens
-
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
0.009 - 0.0359
1-(1H-benzimidazol-2-yl)thiourea
0.00312
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylmorpholin-4-yl)ethanone
Plasmodium falciparum
-
-
0.00154
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylphenyl)ethanone
Plasmodium falciparum
-
-
0.00124
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-fluoro-2-sulfanylphenyl)ethanone
Plasmodium falciparum
-
-
0.00102
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-methoxy-2-sulfanylphenyl)ethanone
Plasmodium falciparum
-
-
0.0011 - 0.0081
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
0.00046
1-benzyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.00099
1-benzyl-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0005 - 0.0324
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.00118
1-[2-pyridin-2-yl-6-(trifluoromethyl)-3,4-dihydropyrimidin-4-yl]propane-2-thiol
Plasmodium falciparum
-
-
0.000667
2,2'-bipyridine
Enterococcus faecalis
-
pH 7.5, 30°C
0.00008 - 0.0398
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
0.0023 - 0.0101
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
0.0017 - 0.0455
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
0.00078 - 0.0044
2-(1H-benzimidazol-2-yl)pyridin-3-ol
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
0.000016
2-(2-aminoethoxy)-3-ethyl-6-[[(2-propylphenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.000046
2-(2-aminoethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.000024
2-(2-aminoethoxy)-6-[([2-[3-(diethylamino)propyl]-4-fluorophenyl]sulfonyl)amino]-3-ethylbenzoic acid
Mus musculus
-
0.0058
2-(carboxymethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.0005
2-(prop-1-en-2-yl)-5-[2-(trifluoromethyl)phenyl]furan
Rickettsia prowazekii
pH 7.0, 30°C, Hill slope 2.1
0.0046 - 0.0329
2-(pyrazin-2-yl)-1H-benzimidazole
0.00097 - 0.0093
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
0.00057 - 0.0284
2-(pyridin-2-yl)-1H-benzimidazole
0.00043 - 0.0373
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
0.00024 - 0.0484
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
0.00011 - 0.0276
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
0.00055 - 0.0228
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
0.0013
2-butyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
Mus musculus
-
0.000015
2-chloro-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.00006
2-ethenyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
Mus musculus
-
0.000038
2-ethoxy-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.000011
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methoxybenzoic acid
Mus musculus
-
0.000016
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
Mus musculus
-
0.00107
2-pyridin-2-yl-4-(trifluoromethyl)-6-[2-(trifluoromethyl)benzyl]-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.0039
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
Homo sapiens
-
0.000009
2-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Mus musculus
-
0.0011
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
Homo sapiens
-
0.02
2-[([4-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]phenyl]sulfinyl)oxy]hydrazinecarboximidamide
Escherichia coli
-
-
0.0296 - 0.0441
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
0.0286 - 0.0498
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
0.0125 - 0.0252
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
0.037
2-[4-(2-Cyano-2-ethoxycarbonyl-1-methyl-vinyl)-phenyl]-1,3-dioxo-2,3-dihydro-1H-isoindole-5-carboxylic acid
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.037 mM
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
-
0.0001
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
0.015 - 1
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
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
0.000034 - 0.00492
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00034 - 0.00054
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00068 - 0.00078
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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
0.0016
3-(2-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0016 mM
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
0.00028 - 0.1
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00083 - 0.016
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00089 - 0.0013
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00055 - 0.0017
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00028 - 0.0109
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00039 - 0.0044
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.0021 - 0.1
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
0.0025 - 0.0034
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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
0.00071 - 0.1
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.000095 - 0.1
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.0017 - 0.00302
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00022 - 0.00077
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
0.00049 - 0.0026
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00015 - 0.00467
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.0006 - 0.1
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
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
0.00136 - 0.1
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.0011 - 0.062
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00014 - 0.00024
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00031 - 0.000671
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
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
0.00013 - 0.00038
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00087 - 0.1
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
0.00032 - 0.00239
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
0.0082
3-acetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0082 mM
0.0328
3-aminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 1.7 mM, IC50: 0.0328 mM
0.00089
3-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00089 mM
0.00103 - 0.00122
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
0.0001 - 0.0233
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
0.000015
3-ethyl-2-methoxy-6-[[(2-[[2-(1-methylpyrrolidin-2-yl)ethyl]amino]phenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.000018
3-ethyl-2-methoxy-6-[[(2-[[3-(2-methylpiperidin-1-yl)propyl]amino]phenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.000067
3-ethyl-2-methyl-6-[(pyridin-2-ylsulfonyl)amino]benzoic acid
Mus musculus
-
0.00032 - 0.00033
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.000038 - 0.00062
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.000174 - 0.00102
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
0.00187 - 0.00486
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
0.0015
3-imino-4-[(E)-(4-methoxyphenyl)diazenyl]-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00025
3-imino-4-[(E)-[2-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00025
3-imino-4-[(E)-[3-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00192 - 0.0537
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.00004 - 0.00082
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.000054 - 0.0002
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
0.00026 - 0.00035
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.00038 - 0.0054
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
0.00018 - 0.00335
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
0.00058 - 0.25
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
0.002
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]-2-hydroxybenzoic acid
Escherichia coli
-
-
0.00175
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]benzoic acid
Escherichia coli
-
-
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
-
0.0021 - 0.0099
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
0.000015
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
Homo sapiens
-
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
0.0166
4-(1,3-thiazol-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0161 - 0.0246
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
0.1
4-(1-methyl-1H-imidazol-2-yl)benzene-1,2-diol
Escherichia coli
-
IC50 above 0.1 mM, using Fe2+, Co2+, or Mn2+-activated MetAP enzymes
0.0202 - 0.0624
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
0.0074 - 0.1
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
0.0066 - 0.1
4-(2-aminothiazol-4-yl)benzene-1,2-diol
0.000031 - 0.079
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
0.0073 - 0.0224
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol
0.0092 - 0.1
4-(3-butylthiophen-2-yl)benzene-1,2-diol
0.0129 - 0.0626
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
0.00007 - 0.055
4-(3-methylthiophen-2-yl)benzene-1,2-diol
0.014 - 0.1
4-(3-propylthiophen-2-yl)benzene-1,2-diol
0.0021 - 0.0031
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
0.000152
4-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
Plasmodium falciparum
-
-
0.0128 - 0.1
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
0.0106 - 0.0526
4-(5-fluoropyrimidin-2-yl)benzene-1,2-diol
0.0112
4-(5-methoxy-1,3-oxazol-2-yl)benzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.1
4-(5-methoxy-2-phenyl-3,4-dihydropyrimidin-4-yl)morpholine
Plasmodium falciparum
-
IC50 above 0.1 mM
0.00513
4-(5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)morpholine
Plasmodium falciparum
-
-
0.028 - 0.0515
4-(5-methylthiophen-2-yl)benzene-1,2-diol
0.0051 - 0.0237
4-(thiophen-2-yl)benzene-1,2-diol
0.0038 - 0.0404
4-(thiophen-3-yl)benzene-1,2-diol
0.0193
4-pyridin-2-ylbenzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0255
4-pyrimidin-2-ylbenzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.00055
4-[(E)-(3-chloro-2-methylphenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00055
4-[(E)-(3-fluorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00125
4-[(E)-(4-chlorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
Escherichia coli
-
-
0.00058
4-[(E)-(4-fluorophenyl)diazenyl]-3-imino-3H-pyrazol-5-amine
Escherichia coli
-
-
0.01 - 0.0388
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0024 - 0.0326
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
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
0.0009 - 4
5-(2,3-dichlorophenyl)furan-2-carboxylic acid
0.00275 - 0.05
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
0.00053 - 0.05
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
0.00338 - 0.05
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
0.00044 - 0.05
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
0.00032 - 0.05
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
0.0077 - 0.05
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
0.00025 - 0.494
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
0.00042 - 0.05
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
0.0046 - 0.05
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
0.00118 - 0.05
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
0.00089 - 0.05
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
0.002
5-(2-chlorophenyl)-2-furohydrazide
Escherichia coli
-
Mn2+-activated enzyme (0.004 mM MnCl2), pH 7.5, 21°C
0.00116 - 0.0771
5-(2-chlorophenyl)furan-2-carbohydrazide
0.00051 - 0.394
5-(2-chlorophenyl)furan-2-carboxylic acid
0.00048 - 0.05
5-(2-ethoxyphenyl)furan-2-carboxylic acid
0.00508 - 0.05
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
0.00055 - 0.2
5-(2-methoxyphenyl)furan-2-carboxylic acid
0.00499 - 0.0477
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
0.00151 - 0.05
5-(2-methylphenyl)thiophene-2-carboxylic acid
0.0154 - 0.1
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide
0.0148 - 0.0363
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
0.00067 - 0.05
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
0.0091
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
Homo sapiens
-
0.01
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.0052 - 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
0.0017 - 0.0488
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
0.000843
5-chloro-4,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.000521
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.0004 - 0.0008
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
0.000158
5-chloro-4-methyl-6-(4-methylbenzyl)-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.000112
5-chloro-6-(2-ethylphenyl)-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.0006 - 0.0076
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
0.0033
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
0.0000177
5-demethylovalicin
Homo sapiens
-
IC50: 17.7 nM, inhibition of recombinant enzyme
0.00009
5-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.000055
5-ethyl-2-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
Mus musculus
-
0.0043 - 0.0458
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0015 - 0.0401
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
0.1
5-methoxy-2-phenyl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
IC50 above 0.1 mM
0.1
5-methoxy-2-pyridin-2-yl-3,4-dihydropyrimidin-4-ol
Plasmodium falciparum
-
IC50 above 0.1 mM
0.00791
5-methoxy-2-pyridin-2-yl-6-pyrrolidin-1-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.0017
5-methoxy-6,6-dimethyl-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.1
5-methoxy-6-methyl-2-phenyl-1,6-dihydropyrimidine
Plasmodium falciparum
-
IC50 above 0.1 mM
0.00217
5-methoxy-6-methyl-6-phenyl-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.00113
5-methoxy-6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
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
-
0.0072 - 0.0406
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0021 - 0.0326
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
0.001
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens
-
0.0012 - 0.0485
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.00016 - 0.0288
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
0.0039 - 0.0417
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0026 - 0.0441
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
0.00024 - 0.25
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
0.00064 - 0.303
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
0.0021 - 0.25
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
0.03
5-[[(4-chlorophenyl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
Rickettsia prowazekii
pH 7.0, 30°C, Hill slope 1.6
0.0575
6-(1,5-dimethylhex-4-en-1-yl)-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens
-
0.0013 - 0.0292
6-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
0.00106
6-(2-chlorobenzyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.000938
6-(benzylsulfanyl)-5-chloro-4-methyl-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.00111
6-(phenylsulfanyl)-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.00106
6-benzyl-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.1
6-benzyl-5-chloro-4-methyl-2-pyridin-3-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
IC50 above 0.1 mM
0.0338
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens
-
0.00104
6-[(2,4-dichlorophenyl)sulfanyl]-5-methoxy-2-pyridin-2-yl-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.00123
6-[(4-methoxyphenyl)sulfanyl]-2-pyridin-2-yl-4-(trifluoromethyl)-1,6-dihydropyrimidine
Plasmodium falciparum
-
-
0.000026
6-[([2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-ethyl-2-methoxybenzoic acid
Mus musculus
-
0.036
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-(1H-imidazol-4-yl)-3-methoxybenzoic acid
Mus musculus
-
0.001
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-2-yl-3-methoxybenzoic acid
Mus musculus
-
0.00002
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
Mus musculus
-
0.000015
6-[[(2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-furan-3-yl-2-methoxybenzoic acid
Mus musculus
-
0.000017
6-[[(2-[[3-(dimethylamino)propyl]amino]-4-fluorophenyl)sulfonyl]amino]-3-furan-3-yl-2-methoxybenzoic acid
Mus musculus
-
0.00001
6-[[(2-[[4-(dimethylamino)butyl]amino]phenyl)sulfonyl]amino]-3-ethyl-2-methoxybenzoic acid
Mus musculus
-
0.000078
6-[[(4-fluorophenyl)sulfonyl]amino]-2,3-dimethylbenzoic acid
Mus musculus
-
0.0025
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(1-hydroxyethyl)-3-methylbenzoic acid
Mus musculus
-
0.008
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(hydroxymethyl)-3-methylbenzoic acid
Mus musculus
-
0.000008
6-[[(4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
Mus musculus
-
0.00028
6-[[(4-fluorophenyl)sulfonyl]amino]-2-methoxy-3-(1H-pyrazol-4-yl)benzoic acid
Mus musculus
-
0.00015
6-[[(4-fluorophenyl)sulfonyl]amino]-3-methyl-2-propylbenzoic acid
Mus musculus
-
0.00038 - 0.0364
8-(pyridin-2-yl)-7H-purine
0.00077 - 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+
0.00012 - 0.00015
A-357300
0.000008 - 0.00002
A-800141
0.0019 - 0.0105
bengamide A
0.0179 - 0.0293
bengamide B
0.0268 - 0.05
bengamide G
0.0371 - 0.05
bengamide L
0.0054 - 0.05
bengamide M
0.0402 - 0.05
bengamide N
0.0027 - 0.05
bengamide O
0.0111 - 0.1
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate
0.014
ethyl 5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxylate
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.008
fumagalone
Homo sapiens
-
0.002 - 0.00323
fumarranol
0.00064 - 0.0278
imidazo[2,1-a]isoquinoline-2-carbohydrazide
0.0017 - 0.0025
L-MetStaCys
0.002 - 0.0043
L-MetStaVal
0.000049
L134
Escherichia coli
-
-
0.00013
L288
Escherichia coli
-
-
0.000599 - 0.001455
MCB2379
Staphylococcus aureus
-
IC50: 599 nM in presence of Co2+, 1455 nM in presence of Zn2+
0.0000437 - 0.0003
MCB2813
Staphylococcus aureus
-
IC50: 43.7 nM in presence of Co2+, 300 nM in presence of Zn2+
0.025
methyl N-[(2S,3R)-3-amino-2-hydroxy-3-(4-methylphenyl)propanoyl]-L-alanylleucinate
Escherichia coli
-
-
0.0035
methyl N-[(2S,3R)-3-amino-2-hydroxy-3-[4-(1-methylethyl)phenyl]propanoyl]-L-alanylleucinate
Escherichia coli
-
-
0.012
methyl N-[(2S,3R)-3-amino-2-hydroxyheptanoyl]-L-serylleucinate
Escherichia coli
-
-
0.0017
methyl [[(2S)-2-([(2S,3R)-3-amino-2-hydroxy-3-[4-(trifluoromethyl)phenyl]propanoyl]amino)propanoyl]amino]acetate
Escherichia coli
-
-
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
0.00054 - 0.0224
N-(1,3-thiazol-2-yl)-1H-benzimidazol-2-amine
0.00072
N-(1,3-thiazol-2-yl)-3-[(N-[2-[2-(2-[2-[(1H-triaziren-1-ylacetyl)amino]ethoxy]ethoxy)ethoxy]-4-[3-(trifluoromethyl)-3H-diaziren-3-yl]benzoyl]glycyl)amino]pyridine-2-carboxamide
Escherichia coli
-
-
0.00006 - 0.0258
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
0.000199
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-2-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
Plasmodium falciparum
-
-
0.1
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-3-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
Plasmodium falciparum
-
IC50 above 0.1 mM
0.1
N-(2-aminoethyl)-N'-[5-chloro-6-methyl-2-pyridin-4-yl-4-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydropyrimidin-4-yl]ethane-1,2-diamine
Plasmodium falciparum
-
IC50 above 0.1 mM
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
0.0028
N-(5-methyl-1,2-oxazol-3-yl)pyridine-2-carboxamide
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.011 - 0.0449
N-(quinolin-8-yl)benzenesulfonamide
0.000804
N-1,3-thiazol-2-yl-3-(N-[(2-2-[(1H-triaziren-1-ylacetyl)amino]ethoxy]-4-[[3-(trifluoromethyl)-[3H-diaziren-3-yl]phenyl)carbonyl]glycyl]amino)pyridine-2-carboxamide
Escherichia coli
-
-
0.03 - 0.2
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
0.0134
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.001 - 0.0212
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
0.0012 - 0.0225
N-cyclobutyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
0.011
N-cyclopentyl-5-(3,4-dihydroxyphenyl)-1,3-oxazole-4-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0009 - 0.0301
N-cyclopentyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
0.0078 - 0.1
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
0.0148
N-cyclopropyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0238 - 0.034
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
0.0024 - 0.041
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
0.0013 - 0.007
Pyridine-2-carboxylic acid thiazol-2-ylamide
0.016
quinolin-8-yl 4-methylbenzenesulfonate
Staphylococcus aureus
-
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
0.00047 - 0.0478
thiabendazole
0.0007
XC-11
Plasmodium falciparum
-
isozyme MetAP1b
additional information
additional information
-
0.02
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
Pyrococcus furiosus
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.027
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
Pyrococcus furiosus
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.032
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
Escherichia coli
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.034
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
Escherichia coli
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.0013
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.045
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.067
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.068
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.141
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.179
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.00054
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0042
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.0045
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.0069
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0079
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.033
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.075
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.00076
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.011
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.018
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.031
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.14
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.201
(2R,3R,4S,5R,E)-N-(2,3-dihydro-1H-inden-2-yl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.00062
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0037
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.014
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.021
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.049
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.05
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.114
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.12
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.0002
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0067
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.0081
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.012
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.052
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.068
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.08
(2R,3R,4S,5R,E)-N-[3-(4-fluorophenyl)-3-(furan-2-yl)propyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.0004
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0055
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.006
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.011
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.026
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.039
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.061
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.15
(2R,3R,4S,5R,E)-N-[3-(furan-2-yl)-3-phenylpropyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Ni2+, pH 7.5, 22°C
0.00096
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.088
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Co2+, pH 7.5, 22°C
0.11
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Fe2+, pH 7.5, 22°C
0.187
(2R,3R,4S,5R,E)-N-[[1-(cyclopropanecarbonyl)piperidin-3-yl]methyl]-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
Mycobacterium tuberculosis
-
apoenyme activated by Mn2+, pH 7.5, 22°C
0.0229
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
Escherichia coli
-
IC50: 0.0229 mM
0.095
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
Saccharomyces cerevisiae
-
IC50: 0.095 mM
0.009
1-(1H-benzimidazol-2-yl)thiourea
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0359
1-(1H-benzimidazol-2-yl)thiourea
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0011
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
Homo sapiens
MetAP1
0.0081
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
Homo sapiens
MetAP2
0.0005
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
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
0.00008
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
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
0.0023
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0034
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
Escherichia coli
-
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
0.0017
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
Escherichia coli
-
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
0.0455
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.00078
2-(1H-benzimidazol-2-yl)pyridin-3-ol
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0044
2-(1H-benzimidazol-2-yl)pyridin-3-ol
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0046
2-(pyrazin-2-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0329
2-(pyrazin-2-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00097
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0049
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
Staphylococcus aureus
-
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
0.00057
2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0199
2-(pyridin-2-yl)-1H-benzimidazole
Staphylococcus aureus
-
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
0.00043
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
Escherichia coli
-
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
0.033
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
Staphylococcus aureus
-
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
0.00024
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.022
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
Staphylococcus aureus
-
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
0.00011
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0188
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
Staphylococcus aureus
-
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
0.00055
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
Escherichia coli
-
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
0.0228
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0296
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.0296 mM
0.0365
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Zn-EcMetAP1: 0.0365 mM
0.0441
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Mn-EcMetAPa: 0.0441 mM
0.0286
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.0286 mM
0.0357
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Ni-EcMetAP1: 0.0357 mM
0.0443
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Mn-EcMetAPa: 0.0443 mM
0.0498
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
Escherichia coli
-
IC50 for Zn-EcMetAP1: 0.0498 mM
0.0125
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
Escherichia coli
-
IC50 for Ni-EcMetAP1: 0.0125 mM
0.0167
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
Escherichia coli
-
IC50 for Zn-EcMetAP1: 0.0167 mM
0.0229
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.0229 mM
0.0252
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
Escherichia coli
-
IC50 for Mn-EcMetAPa: 0.0252 mM
0.015
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
Pyrococcus furiosus
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.044
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
Escherichia coli
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
1
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
Escherichia coli
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
1
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
Pyrococcus furiosus
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30°C
0.000034
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.000034 mM
0.00492
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00492 mM
0.00034
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00034 mM
0.00054
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00054 mM
0.00068
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00068 mM
0.00078
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00078 mM
0.00028
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00028 mM
0.1
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.00083
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00083 mM
0.016
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.016 mM
0.00089
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00089 mM
0.0013
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0013 mM
0.00055
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00055 mM
0.0017
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0017 mM
0.00028
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00028 mM
0.0109
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.0109 mM
0.00039
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00039 mM
0.0044
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0044 mM
0.0021
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
Escherichia coli
-
IC50: 0.0021 mM
0.1
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
Escherichia coli
-
IC50 above 0.1 mM
0.0025
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0025 mM
0.0034
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.0034 mM
0.00071
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00071 mM
0.1
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.000095
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.000095 mM
0.1
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.0017
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0017 mM
0.00302
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00302 mM
0.00022
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00022 mM
0.00077
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00077 mM
0.00049
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00049 mM
0.0026
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0026 mM
0.00015
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00015 mM
0.00467
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00467 mM
0.0006
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0006 mM
0.1
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.00136
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00136 mM
0.1
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.0011
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0011 mM
0.062
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.062 mM
0.00014
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00014 mM
0.00024
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00024 mM
0.00031
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00031 mM
0.000671
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.000671 mM
0.00013
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00013 mM
0.00038
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00038 mM
0.00087
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00087 mM
0.1
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
0.00032
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00032 mM
0.00239
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00239 mM
0.00103
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00103 mM
0.00122
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00122 mM
0.0001
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.0001 mM
0.00076
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50 for Ni-EcMetAP1: 0.00076 mM
0.0224
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50 for Zn-EcMetAP1: 0.0224 mM
0.0233
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50 for Mn-EcMetAPa: 0.0233 mM
0.00032
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00032 mM
0.00033
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00033 mM
0.000038
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.000038 mM
0.00062
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00062 mM
0.000174
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.000174 mM
0.00102
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00102 mM
0.00187
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00187 mM
0.00486
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00486 mM
0.00192
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00192 mM
0.0537
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.0537 mM
0.00004
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00004 mM
0.00082
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00082 mM
0.000054
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.000054 mM
0.0002
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.0002 mM
0.00026
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00026 mM
0.00035
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00035 mM
0.00038
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00038 mM
0.0054
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0054 mM
0.00018
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.00018 mM
0.00335
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.00335 mM
0.00058
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
Mycobacterium tuberculosis
pH 7.5, 37°C, with Ni2+
0.002
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
Mycobacterium tuberculosis
pH 7.5, 37°C, with Co2+
0.25
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
Mycobacterium tuberculosis
-
above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.0021
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.0021 mM
0.0099
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.0099 mM
0.0161
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0195
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.0246
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
Escherichia coli
-
using Mn2+-activated MetAP enzyme
0.0202
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0486
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0624
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0074
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.1
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.1
4-(2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0066
4-(2-aminothiazol-4-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0066
4-(2-aminothiazol-4-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.1
4-(2-aminothiazol-4-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.000031 - 0.0007
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Mycobacterium tuberculosis
-
recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.00095
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.013
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0131
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.024
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.032
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.034
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.039
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.056
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.072
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.079
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.0073
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.014
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0224
4-(3-(2-bromoethyl)thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0092
4-(3-butylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0482
4-(3-butylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.1
4-(3-butylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0129
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0557
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0626
4-(3-ethylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.00007 - 0.0023
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Mycobacterium tuberculosis
-
recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.00051
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.00065
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.008
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.008
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.021
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.022
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.023
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.023
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
-
using Mn2+-activated MetAP enzyme
0.027
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.03
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.033
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.041
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.0427
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.055
4-(3-methylthiophen-2-yl)benzene-1,2-diol
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.014
4-(3-propylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0343
4-(3-propylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.1
4-(3-propylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0021
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0024
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0031
4-(4-bromo-2,5-dimethylthiophen-3-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0128
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0448
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.1
4-(5-chlorothiophen-2-yl)benzene-1,2-diol
Escherichia coli
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0106
4-(5-fluoropyrimidin-2-yl)benzene-1,2-diol
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0526
4-(5-fluoropyrimidin-2-yl)benzene-1,2-diol
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.028
4-(5-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0327
4-(5-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0515
4-(5-methylthiophen-2-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0051
4-(thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0157
4-(thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0237
4-(thiophen-2-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0038
4-(thiophen-3-yl)benzene-1,2-diol
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2
0.0275
4-(thiophen-3-yl)benzene-1,2-diol
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0404
4-(thiophen-3-yl)benzene-1,2-diol
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.01
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
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
0.0024
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0179
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
Staphylococcus aureus
-
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
0.0009 - 4
5-(2,3-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.03
5-(2,3-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,3-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,3-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00275
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0359
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,3-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00053
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0264
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,3-dimethylphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00338
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,3-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00044
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0373
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,4-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00032
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,4-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.0077
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.00889
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0099
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,4-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00025
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0061
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.0071
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.0381
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.25
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Mycobacterium tuberculosis
-
above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.251
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.286
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.355
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.494
5-(2,5-dichlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.00042
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0095
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.0286
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,5-dimethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.0046
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0097
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,5-dimethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00118
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.004
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.0357
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2,5-dimethylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00089
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2-(trifluoromethyl)phenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00116
5-(2-chlorophenyl)furan-2-carbohydrazide
Escherichia coli
in the presence of 0.005 mM Mn2+
0.00578
5-(2-chlorophenyl)furan-2-carbohydrazide
Escherichia coli
in the presence of 0.01 mM Ni2+
0.00656
5-(2-chlorophenyl)furan-2-carbohydrazide
Escherichia coli
in the presence of 0.1 mM Mn2+
0.058
5-(2-chlorophenyl)furan-2-carbohydrazide
Escherichia coli
in the presence of 0.006 mM Fe2+
0.0771
5-(2-chlorophenyl)furan-2-carbohydrazide
Escherichia coli
in the presence of 0.1 mM Co2+
0.00051
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
in the presence of 0.1 mM Mn2+
0.00078
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
in the presence of 0.005 mM Mn2+
0.00092
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.013
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.02 - 0.25
5-(2-chlorophenyl)furan-2-carboxylic acid
Mycobacterium tuberculosis
-
recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.116
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
in the presence of 0.006 mM Fe2+
0.138
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
in the presence of 0.1 mM Co2+
0.141
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
in the presence of 0.01 mM Ni2+
0.186
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.188
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.2
5-(2-chlorophenyl)furan-2-carboxylic acid
Escherichia coli
IC50 above 0.2 mM, in the presence of 0.001 mM Co2+
0.288
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.358
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.381
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.394
5-(2-chlorophenyl)furan-2-carboxylic acid
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.00048
5-(2-ethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0419
5-(2-ethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2-ethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2-ethoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00508
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2-ethoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00055
5-(2-methoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.132
5-(2-methoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.2
5-(2-methoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.2
5-(2-methoxyphenyl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.00499
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.0273
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.0457
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.0477
5-(2-methoxyphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.00151
5-(2-methylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(2-methylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(2-methylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(2-methylphenyl)thiophene-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.0154
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.0154
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.1
5-(3,4-dihydroxyphenyl)-N-isopropyl-2-methylthiazole-4-carboxamide
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0148
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0304
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0363
5-(3,4-dihydroxyphenyl)thiophene-2-carbonitrile
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.00067
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
Escherichia coli
-
Mn(II)-form of the enzyme
0.05
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
Escherichia coli
-
Co(II)-form of the enzyme
0.05
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
Escherichia coli
-
Fe(II)-form of the enzyme
0.05
5-(4-methylnaphthalen-1-yl)furan-2-carboxylic acid
Escherichia coli
-
Ni(II)-form of the enzyme
0.0052
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0017
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0004
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
Homo sapiens
MetAP1
0.0008
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
Homo sapiens
MetAP2
0.0006
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP1
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
MetAP1
0.0033
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens
MetAP2
0.0043
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0015
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0401
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0072
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0021
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0194
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
Staphylococcus aureus
-
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
0.0012
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
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
0.00016
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
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
0.0039
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0417
5-tert-butyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.0026
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0389
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
Staphylococcus aureus
-
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
0.00024
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
pH 7.5, 37°C, with Ni2+
0.00026
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
pH 7.5, 37°C, with Co2+
0.00038
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.0004
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.00078
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.002
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
pH 7.5, 37°C, with Mn2+
0.0049
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.014
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.064
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.094
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.128
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.205 - 0.25
5-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
-
and above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.00064
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.00088
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.0013
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
pH 7.5, 37°C, with Ni2+
0.0022
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.0025
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
pH 7.5, 37°C, with Ni2+
0.023
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.034
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.25
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
-
above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.303
5-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.0021
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.0038
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.0044
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.044
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.103
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.145
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Acinetobacter baumannii
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.25
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
Mycobacterium tuberculosis
-
above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.0013
6-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0292
6-(1H-benzimidazol-2-yl)pyridin-2(1H)-one
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.00038
8-(pyridin-2-yl)-7H-purine
Escherichia coli
-
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
0.00077
8-hydroxy quinoline
Escherichia coli
-
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
0.0183
8-hydroxy quinoline
Staphylococcus aureus
-
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
0.00012
A-357300
Mus musculus
MetAP2
0.00015
A-357300
Homo sapiens
-
0.000008
A-800141
Mus musculus
MetAP2
0.00002
A-800141
Homo sapiens
-
0.0019
bengamide A
Homo sapiens
MetAP1
0.0105
bengamide A
Homo sapiens
MetAP2
0.0179
bengamide B
Homo sapiens
MetAP2
0.0293
bengamide B
Homo sapiens
MetAP1
0.0268
bengamide G
Homo sapiens
MetAP1
0.05
bengamide G
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.0371
bengamide L
Homo sapiens
MetAP1
0.05
bengamide L
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.0054
bengamide M
Homo sapiens
MetAP1
0.05
bengamide M
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.0402
bengamide N
Homo sapiens
MetAP1
0.05
bengamide N
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.0027
bengamide O
Homo sapiens
MetAP1
0.05
bengamide O
Homo sapiens
IC50 above 0.05 mM, MetAP2
0.0111
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0923
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.1
cyclopropyl 5-(3,4-dihydroxyphenyl)-2-methyl-1,3-thiazole-4-carboxylate
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.1
fumagillin
Escherichia coli
-
IC50 above 0.1 mM
0.1
fumagillin
Saccharomyces cerevisiae
-
IC50 above 0.1 mM
11.1
fumagillin
Encephalitozoon cuniculi
-
pH 8.5, 37°C, recombinant MetAP2
0.002
fumarranol
Plasmodium falciparum
-
in 20 mM Tris-HCl (pH 7.1) and 100 mM KCl, at 37°C
0.00323
fumarranol
Homo sapiens
-
0.00064
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.005 mM Mn2+
0.00244
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.001 mM Co2+
0.00431
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.1 mM Mn2+
0.00615
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.01 mM Ni2+
0.0174
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.006 mM Fe2+
0.0278
imidazo[2,1-a]isoquinoline-2-carbohydrazide
Escherichia coli
in the presence of 0.1 mM Co2+
0.0017
L-MetStaCys
Pyrococcus furiosus
-
in 25 mM HEPES buffer at 30°C (pH 7.5)
0.0025
L-MetStaCys
Escherichia coli
-
in 25 mM HEPES buffer at 30°C (pH 7.5)
0.002
L-MetStaVal
Pyrococcus furiosus
-
in 25 mM HEPES buffer at 30°C (pH 7.5)
0.0043
L-MetStaVal
Escherichia coli
-
in 25 mM HEPES buffer at 30°C (pH 7.5)
0.00054
N-(1,3-thiazol-2-yl)-1H-benzimidazol-2-amine
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0224
N-(1,3-thiazol-2-yl)-1H-benzimidazol-2-amine
Staphylococcus aureus
-
pH not specified in the publication, temperature not specified in the publication
0.00006
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
Escherichia coli
-
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
0.0212
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
Staphylococcus aureus
-
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
0.011
N-(quinolin-8-yl)benzenesulfonamide
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0229
N-(quinolin-8-yl)benzenesulfonamide
Staphylococcus aureus
-
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
0.03
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
Escherichia coli
pH not specified in the publication, temperature not specified in the publication
0.046
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
Streptococcus pneumoniae
-
pH not specified in the publication, temperature not specified in the publication
0.06
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
Haemophilus influenzae
-
pH not specified in the publication, temperature not specified in the publication
0.2
N-2-[(3,5-difluorophenyl)acetyl]-N-[(3S,7R)-1-methyl-2-oxo-7-phenyl-2,3,4,7-tetrahydro-1H-azepin-3-yl]-L-alaninamide
Staphylococcus aureus
-
value above 0.2 mM, pH not specified in the publication, temperature not specified in the publication
0.001
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0067
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Mn2+-activated MetAP enzyme
0.0212
N-but-3-en-1-yl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.0012
N-cyclobutyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0079
N-cyclobutyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Mn2+-activated MetAP enzyme
0.0225
N-cyclobutyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.0009
N-cyclopentyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Fe2+-activated MetAP enzyme
0.0118
N-cyclopentyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Mn2+-activated MetAP enzyme
0.0301
N-cyclopentyl-5-(3,4-dihydroxyphenyl)furan-2-carboxamide
Escherichia coli
-
using Co2+-activated MetAP enzyme
0.0078
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.1
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
Escherichia coli
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.1
N-cyclopropyl-2-(3,4-dihydroxyphenyl)thiophene-3-carboxamide
Escherichia coli
IC50 above 0.1 mM, Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0238
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
Escherichia coli
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0285
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
Escherichia coli
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2
0.034
N-cyclopropyl-5-(3,4-dihydroxyphenyl)thiophene-2-carboxamide
Escherichia coli
Mn2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.02 mM MnCl2
0.0024
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
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
0.0013
Pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50 for Co-EcMetAP1: 0.0013 mM
0.005
Pyridine-2-carboxylic acid thiazol-2-ylamide
Escherichia coli
-
IC50: 0.005 mM
0.007
Pyridine-2-carboxylic acid thiazol-2-ylamide
Saccharomyces cerevisiae
-
IC50: 0.007 mM
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
0.00047
thiabendazole
Escherichia coli
-
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
0.000001
TNP-470
Homo sapiens
-
0.000003
TNP-470
Homo sapiens
-
0.000012
TNP-470
Mus musculus
MetAP2
0.00105
TNP-470
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.015
TNP-470
Leishmania donovani
pH 7.5, 37°C
0.116
TNP-470
Plasmodium falciparum
-
in 20 mM Tris-HCl (pH 7.1) and 100 mM KCl, at 37°C
10.6
TNP-470
Encephalitozoon cuniculi
-
pH 8.5, 37°C, recombinant MetAP2
additional information
additional information
Escherichia coli
-
IC50 values for N-(quinolin-8-yl)methanesulfonamide with different metal ions, overview
-
additional information
additional information
Escherichia coli
-
inhibitor screening, assay method development, and assay validation, overview
-
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Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.