Information on EC 3.4.11.18 - methionyl aminopeptidase

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The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea

EC NUMBER
COMMENTARY hide
3.4.11.18
-
RECOMMENDED NAME
GeneOntology No.
methionyl aminopeptidase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
release of N-terminal amino acids, preferentially methionine, from peptides and arylamides
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
61229-81-0
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
isoforms MAP and YflG
-
-
Manually annotated by BRENDA team
marmoset
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
strain H348
UniProt
Manually annotated by BRENDA team
strain H348
UniProt
Manually annotated by BRENDA team
Escherichia coli K-12 MG1655
-
-
-
Manually annotated by BRENDA team
strain RF1
-
-
Manually annotated by BRENDA team
strain RF1
-
-
Manually annotated by BRENDA team
cv. Dongbori
UniProt
Manually annotated by BRENDA team
strain mc2155
-
-
Manually annotated by BRENDA team
strain mc2155
-
-
Manually annotated by BRENDA team
-
Uniprot
Manually annotated by BRENDA team
strain NRC-1
-
-
Manually annotated by BRENDA team
strain NRC-1
-
-
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
Plasmodium vivax Salvador I
-
UniProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
strain PCC6803, three isozymes encoded by lr0786 or map-1, slr0918 or map-2, and sll0555 or map-3
-
-
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
blockade of the isozymes can is lethal to cell proliferation
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
14-3-3gamma protein + H2O
?
show the reaction diagram
-
14-3-3gamma is a shared substrate between isoform MetAP1 and MetAP2 in HUVEC cells
-
-
?
cyclophillin A + H2O
?
show the reaction diagram
eukaryotic elongation factor-2 + H2O
?
show the reaction diagram
GAPDH + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
glutathione-S-transferase + H2O
?
show the reaction diagram
glyceraldehye 3-phosphate dehydrogenase + H2O
?
show the reaction diagram
L-Ala-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
L-Leu-L-Ala-L-Ser-L-Trp + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met 4-nitroanilide + H2O
L-Met + 4-nitroaniline
show the reaction diagram
L-Met-4-nitroanilide + H2O
L-Met + 4-nitroaniline
show the reaction diagram
-
-
-
?
L-Met-7-amido-4-methylcoumarin + H2O
L-Met + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Met-Gly-L-Met-L-Met + H2O
L-Met + Gly-L-Met-L-Met
show the reaction diagram
L-Met-Gly-L-Trp-L-Met-L-Asp + H2O
L-Met + Gly-L-Trp-L-Met-L-Asp
show the reaction diagram
L-Met-L-Ala-L-Ser
L-Met + L-Ala-L-Ser
show the reaction diagram
-
isoform MAP, 77% of the activity with L-Met-Gly-L-Met-L-Met, isoform YflG, 18% of the activity with L-Met-Gly-L-Met-L-Met
-
-
-
L-Met-L-Ala-L-Ser + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met-L-Ala-L-Ser + H2O
L-Met + L-Ala-L-Ser
show the reaction diagram
L-Met-L-Ala-L-Ser-L-Trp + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met-L-Gln-L-Asp-onconase + H2O
L-Met + L-Gln-L-Asp-onconase
show the reaction diagram
-
wild-type, no substrate, mutant M206G/Q233G, 96% of Met removal, mutant M206T/Q233G, 91% of removal, mutant M206T/Q233T, 93% of removal
-
-
?
L-Met-L-Pro-4-nitroanilide + H2O
L-Met + L-Pro-4-nitroanilide
show the reaction diagram
-
-
-
-
?
L-Met-L-Pro-4-nitroanilide + H2O
L-Met + L-Pro-4-nitroaniline
show the reaction diagram
-
-
-
?
L-Met-L-Pro-p-nitroanilide + H2O
L-Met + L-Pro-p-nitroanilide
show the reaction diagram
L-Met-L-Ser-L-Ser-L-His-L-Arg-L-Trp-L-Asp-L-Trp + H2O
L-Met + L-Ser-L-Ser-L-His-L-Arg-L-Trp-L-Asp-L-Trp
show the reaction diagram
-
-
-
-
?
L-Met-N-myristoyltransferase + H2O
L-Met + N-myristoyltransferase
show the reaction diagram
-
-
-
-
?
L-Met-p-nitroanilide + H2O
L-Met + p-nitroanilide
show the reaction diagram
L-Met-p-nitroanilide + H2O
p-nitroaniline + L-Met
show the reaction diagram
L-Met-peptide + H2O
L-Met + peptide
show the reaction diagram
L-Met-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
L-methionine 4-methylcoumaryl-7-amide + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
L-methionine 4-nitroanilide + H2O
L-Met + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
L-methionine-4-methylcoumarin-7-amide + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
-
fluorogenic substrate
-
-
?
L-methionine-7-amido-4-methylcoumarin + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
L-methionyl 4-methylcoumarin-7-amide + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
L-methionyl-7-amido-4-methylcoumarin + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Nle-L-Ala-L-Ser + H2O
?
show the reaction diagram
-
-
-
-
?
L-Phe-L-Ala-L-Ser-L-Trp + H2O
?
show the reaction diagram
-
-
-
-
?
L-Phe-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
L-Thr-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
Leu-Gly-Gly + H2O
?
show the reaction diagram
-
34% of the activity with Met-Ala-Ser
-
-
?
Leu-Leu-Tyr + H2O
?
show the reaction diagram
-
32% of the activity with Leu-Gly-Gly
-
-
?
Leu-Ser-Phe + H2O
?
show the reaction diagram
-
30% of the activity with Met-Ala-Ser
-
-
?
MAEIEIY + H2O
L-Met + AEIEIY
show the reaction diagram
MAEWEIY + H2O
L-Met + AEWEIY
show the reaction diagram
-
-
-
-
?
MAGAIHY + H2O
L-Met + AGAIHY
show the reaction diagram
-
-
-
-
?
MAGIEIY + H2O
L-Met + AGIEIY
show the reaction diagram
-
-
-
-
?
MAHAIHY + H2O
L-Met + AHAIHY
show the reaction diagram
-
-
-
-
?
MAHIEIY + H2O
L-Met + AHIEIY
show the reaction diagram
MAPIEIY + H2O
L-Met + APIEIY
show the reaction diagram
-
-
-
-
?
MARIEIY + H2O
L-Met + ARIEIY
show the reaction diagram
MAWIEIY + H2O
L-Met + AWIEIY
show the reaction diagram
-
-
-
-
?
Met-4-methylcoumaryl-7-amide + H2O
Met + 7-amino-4-methylcoumarin
show the reaction diagram
Met-4-nitroanilide + H2O
Met + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Met-7-amido-4-methylcoumarin + H2O
Met + 7-amino-4-methylcoumarin
show the reaction diagram
Met-Ala + H2O
Met + Ala
show the reaction diagram
-
-
-
-
?
Met-Ala-Ala + H2O
Met + Ala-Ala
show the reaction diagram
-
-
-
-
?
Met-Ala-His-Thr-Leu-Pro-Glu-Glu-Leu + H2O
Met + Ala-His-Thr-Leu-Pro-Glu-Glu-Leu
show the reaction diagram
-
-
-
-
?
Met-Ala-Met + H2O
Met + Ala-Met
show the reaction diagram
Met-Ala-Met-Lys-Ser + H2O
Met + Ala-Met-Lys-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Pro-interleukin 2 + H2O
Met + Ala-Pro-interleukin 2
show the reaction diagram
-
-
-
-
?
Met-Ala-Pro-Thr + H2O
Met + Ala-Pro-Thr
show the reaction diagram
-
-
-
-
?
Met-Ala-Pro-Thr-Ser-Ser-Ser-Thr-Lys-Lys-Thr-Gln-Leu + H2O
Met + Ala-Pro-Thr-Ser-Ser-Ser-Thr-Lys-Lys-Thr-Gln-Leu
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
L-methionine + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
Met-Ala-Ser-(Gly)5-(Leu)3 + H2O
Met + Ala-Ser-(Gly)5-(Leu)3
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Ala-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser-Lys-(biotin)-Gly + H2O
Met + Ala-Ser-Lys-(biotin)-Gly
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser-Trp + H2O
Met + Ala-Ser-Trp
show the reaction diagram
-
-
-
-
?
Met-Arg-Phe + H2O
Met + Arg-Phe
show the reaction diagram
-
substrate of isozymes c1MetAP-Ia and c3MetAP-Ib, no activity with isozyme c2MetAP-Ia
-
-
?
Met-Asp-Gly + H2O
Met + Asp-Gly
show the reaction diagram
-
substrate of isozyme c3MetAP-Ib, no activity with the other two isozymes
-
-
?
Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr + H2O
Met + Gly-Ala-Gln-Phe-Ser-Lys-Thr
show the reaction diagram
-
-
-
-
?
Met-Gly-Gly + H2O
Met + Gly-Gly
show the reaction diagram
Met-Gly-Met + H2O
Met + Gly-Met
show the reaction diagram
-
low activity
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
Met-Gly-Met-Met + H2O
L-methionine + Gly-Met-Met
show the reaction diagram
Met-Gly-Met-Met + H2O
Met + Gly-Met-Met
show the reaction diagram
Met-Gly-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Gly-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-Ile-Phe-ricin A + H2O
Met + Ile-Phe-ricin A
show the reaction diagram
-
-
-
-
?
Met-Leu-Gly + H2O
Met + Leu-Gly
show the reaction diagram
-
substrate of isozymes c1MetAP-Ia and c3MetAP-Ib, no activity with isozyme c2MetAP-Ia
-
-
?
Met-Leu-Phe + H2O
Met + Leu-Phe
show the reaction diagram
-
-
-
-
?
Met-Lys-bradykinin + H2O
Met + Lys-bradykinin
show the reaction diagram
Met-Met-Ala + H2O
Met + Met-Ala
show the reaction diagram
-
substrate of isozymes c1MetAP-Ia and c3MetAP-Ib, no activity with isozyme c2MetAP-Ia
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Met-Phe-Gly + H2O
Met + Phe-Gly
show the reaction diagram
-
-
-
-
?
Met-Pro + H2O
Met + Pro
show the reaction diagram
-
-
-
-
?
Met-Pro-4-nitroanilide + H2O
Met + Pro-4-nitroanilide
show the reaction diagram
Met-Pro-Gly + H2O
?
show the reaction diagram
-
-
-
-
?
Met-Pro-Gly-Gly + H2O
Met + Pro-Gly-Gly
show the reaction diagram
-
-
-
-
?
Met-Pro-His-Thr-Leu-Pro-Glu-Glu + H2O
Met + Pro-His-Thr-Leu-Pro-Glu-Glu
show the reaction diagram
-
-
-
-
?
Met-Pro-p-nitroanilide + H2O
Pro-p-nitroanilide + Met
show the reaction diagram
Met-Pro-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Pro-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-Pro-Thr-Ser-Ser-Ser-Thr-Lys-Lys-Thr-Gln-Leu-Cys + H2O
Met + Pro-Thr-Ser-Ser-Ser-Thr-Lys-Lys-Thr-Gln-Leu-Cys
show the reaction diagram
-
-
-
-
?
Met-S-Gly-Phe + H2O
L-methionine + ?
show the reaction diagram
-
-
-
?
Met-S-Gly-Phe + H2O
Met + Gly-Phe
show the reaction diagram
-
-
-
-
?
Met-Ser + H2O
Met + Ser
show the reaction diagram
-
-
-
-
?
Met-Ser-Gly + H2O
?
show the reaction diagram
-
-
-
-
?
Met-Ser-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Ser-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-Thr + H2O
Met + Thr
show the reaction diagram
-
-
-
-
?
Met-Thr-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Thr-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-Val + H2O
Met + Val
show the reaction diagram
-
-
-
-
?
Met-Val-His-Thr-Leu-Pro-Glu-Glu-Leu + H2O
Met + Val-His-Thr-Leu-Pro-Glu-Glu-Leu
show the reaction diagram
-
-
-
-
?
Met-Val-Ser-His-Arg-Trp-Asp-Trp + H2O
Met + Val-Ser-His-Arg-Trp-Asp-Trp
show the reaction diagram
-
-
-
-
?
Met-[2-mercapto-ethanoyl]-Phe + H2O
[2-mercapto-ethanoyl]-Phe + Met
show the reaction diagram
-
-
-
-
?
methionyl 2-naphthylamide + H2O
Met + 2-naphthylamine
show the reaction diagram
-
-
-
-
?
MGEIEIY + H2O
L-Met + GEIEIY
show the reaction diagram
MGKVKVGV + H2O
L-Met + GKVKVGV
show the reaction diagram
N-terminal peptide of glyceraldehyde 3-phosphate dehydrogenase
-
-
?
MGNLKSVA + H2O
L-Met + GNLKSVA
show the reaction diagram
N-terminal peptide of endothelial nitric oxide synthase
-
-
?
MPEIEIY + H2O
L-Met + PEIEIY
show the reaction diagram
MSDFIGY + H2O
L-Met + SDFIGY
show the reaction diagram
-
-
-
-
?
MTEIEIY + H2O
L-Met + TEIEIY
show the reaction diagram
MVAAAAY + H2O
L-Met + VAAAAY
show the reaction diagram
-
-
-
-
?
MVEIEIY + H2O
L-Met + VEIEIY
show the reaction diagram
MVGVKPY + H2O
L-Met + VGVKPY
show the reaction diagram
-
-
-
-
?
MVHQVLY + H2O
L-Met + VHQVLY
show the reaction diagram
-
-
-
-
?
MVKIEIY + H2O
L-Met + VKIEIY
show the reaction diagram
-
-
-
-
?
MVKQIESK + H2O
L-Met + VKQIESK
show the reaction diagram
N-terminal peptide of thioredoxin-1
-
-
?
MVLSPAY + H2O
L-Met + VLSPAY
show the reaction diagram
-
-
-
-
?
MVNPTVFF + H2O
L-Met + VNPTVFF
show the reaction diagram
N-terminal peptide of cyclophilin A
-
-
?
MVNPTVY + H2O
L-Met + VNPTVY
show the reaction diagram
-
-
-
-
?
Nle-4-nitroanilide + H2O
Nle + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
proto-oncogene c-Src + H2O
?
show the reaction diagram
-
-
-
-
?
SH3 binding glutamic acid rich-like protein + H2O
?
show the reaction diagram
thioredoxin-1 + H2O
?
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
glutathione-S-transferase + H2O
?
show the reaction diagram
-
removal of Met(init) from glutathione-S-transferase. Processing of glutathione-S-transferase in yeast relies almost entirely on MetAP1 function
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Cd2+
-
isoform MAP, may substitute for Co2+
Na+
-
some positive effect on the enzyme activity at 5 mM
NH4+
-
some positive effect on the enzyme activity at 5 mM
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((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
-
-
1,10-phenanthroline
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-(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-4-(2-methyl-1,3-thiazol-4-yl)benzamide
-
-
2-hydroxyethyl disulfide
-
inhibition is through covalent modifiction of residue C105
2-mercaptoethanol
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-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-(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-[[(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-hydroxy quinoline
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+
A-357300
A-800141
actinonin
amastatin
bengamide A
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
bestatin
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
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
fumagalone
-
-
fumagillin
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
fumarranol
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-Met-(RS)-sulfoxide
-
-
L-methionine
weak, competitive
L-MetStaCys
L-MetStaVal
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
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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
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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
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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
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N-(2-methoxybenzyl)-6-(4-methylnaphthalen-1-yl)picolinamide
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N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
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N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine