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
3.4.11.18
-
RECOMMENDED NAME
GeneOntology No.
methionyl aminopeptidase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
release of N-terminal amino acids, preferentially methionine, from peptides and arylamides
show the reaction diagram
peptide + H2O = N-terminal amino acid + peptide, preferentially methionine, further reaction: arylamide + H2O = aromatic hydrocarbon + amine
-
-
-
release of N-terminal amino acids, preferentially methionine, from peptides and arylamides
show the reaction diagram
reaction mechanism of monometalated enzyme. Charge-charge interactions involving D97 and D108 position and bind substrate. E204 acts as general base
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
aminopeptidase, methionine
-
-
-
-
c1MetAP-Ia
-
-
c1MetAP-Ia
Synechocystis sp. PCC6803
-
-
-
c2MetAP-Ia
-
-
c2MetAP-Ia
Synechocystis sp. PCC6803
-
-
-
c3MetAP-Ib
-
-
c3MetAP-Ib
Synechocystis sp. PCC6803
-
-
-
CoCoEcMetAP
-
dicobalt form of the methionine aminopeptidase from Escherichia coli
Ebp1
-
-
eMet-AP
-
-
ErbB-3 receptor binding protein
-
-
initiation factor 2 associated 67 kDa glycoprotein
-
-
-
-
L-methionine aminopeptidase
-
-
-
-
MAP
-
-
-
-
MAP-Pfu
P56218
-
MAP1D
-
-
MetAP
-
-
-
-
MetAP
P0AE18
-
MetAP
Mycobacterium smegmatis mc2155
-
-
-
MetAP
Synechocystis sp. PCC6803
-
-
-
MetAP-1
-
-
-
-
MetAP-1
P53582
-
MetAP-2
-
-
-
-
MetAP-2
Q7SXK1
-
MetAP-2
O08663
-
MetAP-2
P38062
-
MetAP1
-
-
-
-
MetAP1
P53582
-
MetAP1
P53582
isozyme
MetAP1D
Q6UB28
-
MetAP2
-
-
-
-
MetAP2
B7XJ30
-
-
MetAP2
P50579
isozyme
MetAP2
-
-
MetAP2
P38062
-
MetAP2
Q28F92
-
methionine amino peptidase type 2
Q8SR45
-
methionine amino peptidase type 2
-
-
methionine amino peptidase type 2
P50579
-
methionine aminopeptidase
-
-
-
-
methionine aminopeptidase
P0AE18
-
methionine aminopeptidase
Escherichia coli K-12 MG1655
-
-
-
methionine aminopeptidase
-
-
methionine aminopeptidase
Halobacterium salinarum RF1
-
-
-
methionine aminopeptidase
-
-
methionine aminopeptidase
P50579, P53582
-
methionine aminopeptidase
Q6UB28
-
methionine aminopeptidase
E0A9F0
nuclear localization signal at C-terminal end
methionine aminopeptidase
-
-
methionine aminopeptidase
Mycobacterium smegmatis mc2155
-
-
-
methionine aminopeptidase
-
-
methionine aminopeptidase
Natronomonas pharaonis NRC-1
-
-
-
methionine aminopeptidase
-
-
methionine aminopeptidase
P56218
-
methionine aminopeptidase
-
-
methionine aminopeptidase
-
-
methionine aminopeptidase
Synechocystis sp. PCC6803
-
-
-
methionine aminopeptidase 1
-
-
methionine aminopeptidase 1b
-
-
methionine aminopeptidase 2
-
-
methionine aminopeptidase 2
Q7SXK1
-
methionine aminopeptidase 2
-
-
methionine aminopeptidase 2
P50579
-
methionine aminopeptidase 2
O08663
-
methionine aminopeptidase 2
-
-
methionine aminopeptidase AbMetAPx
A3M623
-
methionine aminopeptidase AbMetAPx
A3M623
-
-
methionine aminopeptidase AbMetAPy
A3M752
-
methionine aminopeptidase AbMetAPy
A3M752
-
-
methionine aminopeptidase II
Q28F92
-
methionine aminopeptidase type 1
P53582
-
methionine aminopeptidase type 1a
-
-
methionine aminopeptidase type 1c
-
-
methionine aminopeptidase type 2
-
-
methionine aminopeptidase type 2
B7XJ30
-
methionine aminopeptidase type 2
B7XJ30
-
-
methionine aminopeptidase type 2
-
-
methionine aminopeptidase type 2
P50579
-
methionine aminopeptidase type 2
-
-
methionine aminopeptidase type I
-
-
methionine aminopeptidase type II
-
-
methionine aminopeptidase type II
P50579
-
methionine aminopeptidase type II
-
-
methionine aminopeptidase type-2
-
-
methionine aminopeptidase type-2
P38062
-
methionine aminopeptidase-1
-
-
methionine aminopeptidase-1
P53582
-
methionine aminopeptidase-2
-
-
methionine aminopeptidase-2
-
-
methionine aminopeptidase-2
P50579
-
methionine aminopeptidase-2
-
-
methionine aminopeptidase-2
O08663
-
methionine aminopeptidase-2
P38062
-
methionine aminopeptidase-2
-
-
p67
-
-
-
-
p67eIF2
-
-
-
-
peptidase M
-
-
-
-
type 1 methionine aminopeptidase
P53582
-
type 2 methionine aminopeptidase
P50579
-
type I MetAP
-
-
type I methionine aminopeptidase
-
-
methionine aminopetidase-2
O08663
-
additional information
-
EcMetAP2 as a member of the MetAP2c family
additional information
-
MetAP belongs to the dinuclear metallohydrolases
additional information
-
MetAP belongs to the family of dinuclear metallohydrolases
additional information
-
MetAP is one of the dinuclear metallohydrolases
additional information
-
eukaryotes contain both the type I and the type II MetAPs, whereas prokaryotes possess only the type I enzyme
CAS REGISTRY NUMBER
COMMENTARY
61229-81-0
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
isoforms MAP and YflG
-
-
Manually annotated by BRENDA team
marmoset
-
-
Manually annotated by BRENDA team
strain H348
UniProt
Manually annotated by BRENDA team
isoform YpdF, showing Xaa-Pro aminopeptidase activity and limited methionine aminopeptidase activity
-
-
Manually annotated by BRENDA team
K-12 (strain MG1655)
-
-
Manually annotated by BRENDA team
K-12 CM89
-
-
Manually annotated by BRENDA team
strain ATCC 25922
-
-
Manually annotated by BRENDA team
strains AS19, D22 and SM101
-
-
Manually annotated by BRENDA team
type I isoform
SwissProt
Manually annotated by BRENDA team
Escherichia coli K-12 MG1655
-
-
-
Manually annotated by BRENDA team
Halobacterium salinarum RF1
strain RF1
-
-
Manually annotated by BRENDA team
; colon cancer cell lines and patiens with colon tumors
-
-
Manually annotated by BRENDA team
enzyme type II, patients with human colorectal adenocarcinomas
-
-
Manually annotated by BRENDA team
isoform etAP2
-
-
Manually annotated by BRENDA team
MetAP1
UniProt
Manually annotated by BRENDA team
MetAP1 isoform
-
-
Manually annotated by BRENDA team
MetAP2
UniProt
Manually annotated by BRENDA team
methionine aminopeptidase type 2
-
-
Manually annotated by BRENDA team
mitochondrial precursor
UniProt
Manually annotated by BRENDA team
patient with high-risk neuroblastoma
-
-
Manually annotated by BRENDA team
patients with rheumatoid arthritis
-
-
Manually annotated by BRENDA team
type I and type II enzyme
-
-
Manually annotated by BRENDA team
type I enzyme, expressed in Escherichia coli
-
-
Manually annotated by BRENDA team
type I isoform
-
-
Manually annotated by BRENDA team
type II enzyme, Mn(II)-form
UniProt
Manually annotated by BRENDA team
cv. Dongbori
UniProt
Manually annotated by BRENDA team
strain mc2155
-
-
Manually annotated by BRENDA team
Mycobacterium smegmatis mc2155
strain mc2155
-
-
Manually annotated by BRENDA team
isozyme MetAP1c encoded by gene mapB
Uniprot
Manually annotated by BRENDA team
strains H37Ra and H37Rv, two isozymes MtMetAP1a and MtMetAP1c encoded by genes Rv0734 and Rv2861c
-
-
Manually annotated by BRENDA team
two isozymes MtMetAP1a and MtMetAP1c
-
-
Manually annotated by BRENDA team
isozyme MetAP1c encoded by gene mapB
Uniprot
Manually annotated by BRENDA team
strain NRC-1
-
-
Manually annotated by BRENDA team
Natronomonas pharaonis NRC-1
strain NRC-1
-
-
Manually annotated by BRENDA team
strain 3D7, four isozymes MetAP1a, MetAP1b, MetAP1c, and MetAP2
-
-
Manually annotated by BRENDA team
strains 3D7 and Dd2
-
-
Manually annotated by BRENDA team
isoform MetAP-II
Uniprot
Manually annotated by BRENDA team
type II enzyme
-
-
Manually annotated by BRENDA team
isoform Map2
-
-
Manually annotated by BRENDA team
methionine aminopeptidase 1
-
-
Manually annotated by BRENDA team
type I enzyme
-
-
Manually annotated by BRENDA team
Salmonella enterica subsp. enterica serovar Typhimurium TN2529
strain TN2529
-
-
Manually annotated by BRENDA team
isoform I
SwissProt
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
Synechocystis sp. PCC6803
strain PCC6803, three isozymes encoded by lr0786 or map-1, slr0918 or map-2, and sll0555 or map-3
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
malfunction
-
blockade of the isozymes can is lethal to cell proliferation
physiological function
-
MetAP functions in the catalytic removal of N-terminal initiator methionine residues from proteins during sythesis, which is essential for the correct folding and trafficking of proteins
physiological function
-
MetAP is a ubiquitous enzyme required for cell survival and an attractive target for antibacterial and anticancer drug development. MetAP is involved in protein maturation by catalyzing the hydrolytic excision of the N-terminal methionine from nascent proteins
physiological function
-
MetAP is essential for bacterial survival
physiological function
-
MetAP plays a critical role in protein maturation by catalyzing the removal of the N-terminal initiator methionine from nascent proteins
physiological function
-
MetAP2 is a bifunctional protein that plays a critical role in the regulation of post-translational processing and protein synthesis
physiological function
-
methionine aminopeptidase plays an essential role for cell survival
physiological function
-
knockdown perturbed angiogenesis
physiological function
E0A9F0
stronger freezing tolerance (transgenic Arabidopsis plants)
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
cyclophillin A + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
eukaryotic elongation factor-2 + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
GAPDH + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
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
-
-
?
glyceraldehye 3-phosphate dehydrogenase + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
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
Q8SR45
-
-
-
?
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-Met-L-Met + H2O
L-Met + Gly-L-Met-L-Met
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
P0AE18
-
-
-
?
L-Met-L-Ala-L-Ser + H2O
L-Met + L-Ala-L-Ser
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
Q8SR45
-
-
-
?
L-Met-L-Pro-p-nitroanilide + H2O
L-Met + L-Pro-p-nitroanilide
show the reaction diagram
-
-
-
-
?
L-Met-L-Pro-p-nitroanilide + H2O
L-Met + L-Pro-p-nitroanilide
show the reaction diagram
-
-
-
-
?
L-Met-L-Pro-p-nitroanilide + H2O
L-Met + L-Pro-p-nitroanilide
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
p-nitroaniline + L-Met
show the reaction diagram
-
-
-
-
?
L-Met-p-nitroanilide + H2O
L-Met + p-nitroanilide
show the reaction diagram
Mycobacterium smegmatis, Mycobacterium smegmatis mc2155
-
-
-
-
?
L-Met-peptide + H2O
L-Met + peptide
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
P0AE18
-
-
-
?
L-Met-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met-PSI[C(O)S]Gly-L-Phe + H2O
?
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-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
-
fluorogenic substrate
-
-
?
L-methionyl 4-methylcoumarin-7-amide + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
P9WK19
fluorogenic substrate
-
-
?
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
P0AE18
-
-
-
?
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
A3M623, A3M752
-
-
-
?
Met-4-methylcoumaryl-7-amide + H2O
Met + 7-amino-4-methylcoumarin
show the reaction diagram
A3M623, A3M752
-
-
-
?
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-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 + H2O
Met + Ala-Met
show the reaction diagram
Synechocystis sp., Synechocystis sp. PCC6803
-
-
-
-
?
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
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
also cleaves methionine from other tripeptides with a relatively small and/or uncharged penultimate amino acid residue (Pro, Gly, Val, Thr, or Ser) but not if bulky and/or charged (Arg, His, Leu, Met, or Tyr)
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
Synechocystis sp. PCC6803
-
-
-
-
?
Met-Ala-Ser + H2O
L-methionine + 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
Synechocystis sp., Synechocystis sp. PCC6803
-
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-Gly + H2O
Met + Gly-Gly
show the reaction diagram
Synechocystis sp., Synechocystis sp. PCC6803
-
-
-
-
?
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
Gly-Met-Met + Met
show the reaction diagram
P0AE18
-
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Met + Gly-Met-Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Met + Gly-Met-Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Met + Gly-Met-Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Met + Gly-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
L-methionine + Gly-Met-Met
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
L-methionine + Gly-Met-Met
show the reaction diagram
Escherichia coli K-12 MG1655
-
-
-
-
?
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-Lys-bradykinin + H2O
Met + Lys-bradykinin
show the reaction diagram
-
i.e. Met-Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg
-
-
?
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-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
P53582
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q6UB28
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
O08663
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q7SXK1
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
P38062
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q28F92
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the biological function is removing the terminal methionine from nascent peptides
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme catalyzes the removal of an amino-terminal methionine from a newly synthesized polypeptide
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme is responsible for hydrolysis of the initiator methionine residue from the majority of newly synthesized proteins. Potentially important role in the production of recombinant proteins, since failure to correctly remove initiator methionine residues can result in a product that is inactive or immunogenic
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme is directly involved in the regulation of growth factor-stimulated endothelial cell proliferation
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the biological function is removing the terminal methionine from nascent peptides during protein synthesis
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme removes the N-terminal Met from polypeptides, and thus plays a key role in protein synthesis, modification and transport
-
-
?
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-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-p-nitroanilide + H2O
Pro-p-nitroanilide + Met
show the reaction diagram
Q6UB28
-
-
-
?
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
Met + Gly-Phe
show the reaction diagram
-
-
-
-
?
Met-S-Gly-Phe + H2O
L-methionine + ?
show the reaction diagram
E0A9F0
-
-
-
?
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
-
-
-
-
?
methionyl aminomethylcoumarin + H2O
L-methionine + aminomethylcoumarin
show the reaction diagram
-
-
-
-
?
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
-
-
-
-
?
MVLSPAY + H2O
L-Met + VLSPAY
show the reaction diagram
-
-
-
-
?
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
-
MetAP2-specific substrate
-
-
?
thioredoxin-1 + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
MGEIEIY + H2O
L-Met + GEIEIY
show the reaction diagram
-
-
-
-
?
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of glutamic acid, specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of threonine
-
-
-
additional information
?
-
-
residues adjacent to the initiation methionine can significantly influence the methionine cleavage process
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of lysine
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of lysine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of valine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of valine
-
-
-
additional information
?
-
-
not activity with Met(sulfoxide)-Ala-Ser
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of asparagine
-
-
-
additional information
?
-
-
no activity with methionine 4-nitroanilide
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of aspartic acid
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of proline
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of proline
-
-
-
additional information
?
-
-
the enzyme hydrolyzes NH2-terminal methionine from methionyl peptides longer than tetrapeptides and from shorter methionyl peptides with blocked carboxy ends
-
-
-
additional information
?
-
-
the mutant enzyme prefers substrates, having Ser or Pro at P1', over substrates that contain glycine and alanine at that position. The wild-type enzyme prefers substrates that have Ala, Gly, Ser or Pro at P1'. Amino-terminal Met cannot be removed by either the mutant or wild-type enzyme from substrates having large and charged amino acids at P1' position
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of leucine
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of leucine
-
-
-
additional information
?
-
-
while the nature of the P1' residue of peptide substrates dictates the substrate specificity in the active site of metAP2 the P2' residue appears to play a key role in the kinetics of peptidolysis. The catalytic efficiency of dipeptide substrates is at least 250fold lower than those of the tripeptides. When the P1' amino acid of the peptide substrate is sterically large such as with L-Leu, MetAP2 exhibits no detectable activity. L-Nle is the only amino acid residue other than L-Met that can be accomodated at the N-terminus of a substrate
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of isoleucine
-
-
-
additional information
?
-
-
removal of the initiator methionine if the penultimate residue has a small radius of gyration (Gly, Ala, Ser, Thr, Pro, Val and Cys)
-
-
-
additional information
?
-
-
specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of arginine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of serine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of serine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of glycine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of glycine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of alanine
-
-
-
additional information
?
-
-
specificity: the enzyme cleaves amino-terminal methionine when it precedes residues of alanine, specificity: the enzyme does not cleave amino-terminal methionine when it precedes residues of glutamine
-
-
-
additional information
?
-
-
removes methionine from hemoglobin nascent peptides
-
-
-
additional information
?
-
-
together with N-myristoyltransferase, enzyme plays a major role in the process of myristoylation of oncoproteins including the c-src family
-
-
-
additional information
?
-
-
detailed analysis of mutants specificity on oligo- and protein substrates
-
-
-
additional information
?
-
-
enzyme hydrolyzes N-terminal L-methionine when the next amino acid is L-alanine, L-proline, or L-serine with substrate preference in decreasing order: proloine, alanine, serine. enzyme hydrolyzes the Xaa-Po peptide bond when the first amino acid is L-alanine, L-asparagine, or L-methionine
-
-
-
additional information
?
-
-
no activity when using Glu-Ala-Ser and Leu-Ala-Ser peptides as substrates
-
-
-
additional information
?
-
-
peptides with Val or Thr at P1' are much less efficiently cleaved than those with Ala, Cys, Gly, Pro, or Ser in this position
-
-
-
additional information
?
-
-
active site structure and substrate binding, overview
-
-
-
additional information
?
-
B7XJ30
active site structure and substrate binding, overview
-
-
-
additional information
?
-
-
the isozymes act on peptides in the cytosol, that are N-terminal fragments from digestion of hemoglobin in the digestive vacuole. The hemoglobin-derived peptides show leucine and alanine as most abundant amino acids
-
-
-
additional information
?
-
-
active site strutcure and substrate binding, overview
-
-
-
additional information
?
-
-
isozyme substrate specificity, overview
-
-
-
additional information
?
-
-
MetAP carries out the cotranslational N-terminal methionine excision
-
-
-
additional information
?
-
-
substrate specificities of recombinant isozymes, overview, no activity towards tripeptides in which the N-terminal amino acid is not Met, no activity with Pro-Met and X-Gly-Gly peptides
-
-
-
additional information
?
-
-
the enzyme shows preference for synthetic peptides containing leucine and alanine
-
-
-
additional information
?
-
-
substrate specificity is systematically profiled by screening against a combinatorial peptide library and kinetic analysis of individually synthesized peptide substrates
-
-
-
additional information
?
-
Synechocystis sp. PCC6803
-
substrate specificities of recombinant isozymes, overview, no activity towards tripeptides in which the N-terminal amino acid is not Met, no activity with Pro-Met and X-Gly-Gly peptides
-
-
-
additional information
?
-
B7XJ30
active site structure and substrate binding, overview
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
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
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
P53582
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q6UB28
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
O08663
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q7SXK1
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
P38062
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Q28F92
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the biological function is removing the terminal methionine from nascent peptides
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme catalyzes the removal of an amino-terminal methionine from a newly synthesized polypeptide
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme is responsible for hydrolysis of the initiator methionine residue from the majority of newly synthesized proteins. Potentially important role in the production of recombinant proteins, since failure to correctly remove initiator methionine residues can result in a product that is inactive or immunogenic
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme is directly involved in the regulation of growth factor-stimulated endothelial cell proliferation
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the biological function is removing the terminal methionine from nascent peptides during protein synthesis
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
-
the enzyme removes the N-terminal Met from polypeptides, and thus plays a key role in protein synthesis, modification and transport
-
-
?
additional information
?
-
-
together with N-myristoyltransferase, enzyme plays a major role in the process of myristoylation of oncoproteins including the c-src family
-
-
-
additional information
?
-
-
the isozymes act on peptides in the cytosol, that are N-terminal fragments from digestion of hemoglobin in the digestive vacuole. The hemoglobin-derived peptides show leucine and alanine as most abundant amino acids
-
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
-
0.0001-0.001 mM, activity is enhanced 5-10fold
Ca2+
-
isoform MAP, may substitute for Co2+
Ca2+
-
activates, required for enzyme inhibition by inhibitor 1, overview
Cd2+
-
isoform MAP, may substitute for Co2+
Co2+
-
essential for enzyme activity; Mn2+, Cu2+, Zn2+ or Mg2+ cannot substitute
Co2+
-
stimulates
Co2+
-
loosely associated with the enzyme protein; stimulates
Co2+
-
1 mol of wild-type enzyme contains 2 mol of zinc ions and at least 1 mol of cobalt ion, whereas 1 mol of the truncated methionine aminopeptidase DELTA2-69 lacking the putative zinc fingers cotains only a trace amount of zinc ions but still contains one mol of cobalt ion; 1 mol of wild-type enzyme contains at least 1 mol of Co2+
Co2+
-
the active site contains two Co2+, ligated by the side chains of Asp97, Asp108, Glu204, Glu235, and His171 with approximate octahedral coordination
Co2+
-
at low concentrations, 0.01 mM, Co2+ plays a key role in the stimulation of enzyme activity. It is still questionable that Co(II) is the physically relevant divalent cation
Co2+
-
maximal activity is observed after addition of only 1 equivalent of divalent metal ion, the metal binding constant for the first binding event is 0.0003 mM for Co(II)-substituted enzyme. The metal ion resides in a pentacoordinate geometry
Co2+
-
the mutant enzyme contains 0.43 mol of Co2+ per mol. The wild-type enzyme contains 0.75 mol of Co2+ per mol of enzyme
Co2+
-
optimal concentration is 1 mM
Co2+
-
optimal concentration is 0.008 mM
Co2+
-
Co2+-dependent metallopeptidase
Co2+
-
Co2+-dependent metallopeptidase; in mutant enzymes D97A and E204V cobalt content is not detectable, in mutant enzyme H171L and 235V the cobalt content is 3% of that of the wild-type enzyme, in mutant enzyme D108A the cobalt content is 6% of that of the wild-type enzyme
Co2+
-
stimulates activity of MetAP2 with Met-Ala-Ser or Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr 10-20fold, maximal stimulation at 0.01 mM. In presence of 5 mM glutathione 30-40fold stimulation
Co2+
-
inhibitory above 0.0625 mM
Co2+
-
required, both isoform MAP and YflG. YflG shows strong preference for Co2+
Co2+
-
enzyme binds up to 1.1 equivalents of Co2+ in the metal concentration range found in vivo. Dissociation constant is about 0.0025-0.004 mM
Co2+
-
required
Co2+
-
activation requires only one equivalent of Co2+ or Mn2+
Co2+
Q6UB28
significant activation at 0.01 mM, at least two Co2+ ions, which may act cooperatively, are needed to promote catalysis
Co2+
-
the enzyme activity is enhanced by 1 mM Co2+
Co2+
-
the kcat value increases as a function of Co2+ ion concentration and exhibits a maximum after the addition of one equivalent of Co2+
Co2+
-
MetAP requires a divalent metal ion for activation, such as Co2+
Co2+
-
the enzyme contains one Co2+ ion
Co2+
-
the dicobalt form of the methionine aminopeptidase has an active site with one 5-coordinate Co2+ and a more weakly bound 6-coordinate Co2+
Co2+
-
Co2+ also activates
Co2+
-
activity requires divalent cations like Co2+
Co2+
-
requires Zn2+, Co2+, or Mg2+ as cofactor
Co2+
-
determination of metal affinity to the active site of the metalloenzyme by onlinear curve fitting of metal titration curves using the multiple independent binding sites, MIBS, model, overview
Co2+
-
activates
Co2+
-
activates, required for enzyme inhibition by inhibitor 1, overview
Co2+
-
activates
Co2+
-
activates, tight binding to the enzyme
Co2+
-
activates, two metal ions are coordinated by five conserved amino acid residues D97, D108, H171, E204 and E235, activation kinetics, overview
Co2+
-
activates best
Co2+
P9WK19
activates
Co2+
E0A9F0
-
Fe2+
-
maximal activity is observed after addition of only 1 equivalent of divalent metal ion, the metal binding constant for the first binding event is 0.0002 mM for Fe(II)-substituted enzyme. The metal ion resides in a pentacoordinate geometry
Fe2+
-
in vivo metal ions are likely Fe(II) ions
Fe2+
-
optimal concentration is 0.008 mM
Fe2+
-
MetAP requires a divalent metal ion for activation, such as Fe2+
Fe2+
-
native cofactor
Fe2+
-
Fe2+ is the likely metal cofactor used by MetAP in the cellular environment
Fe2+
-
requires Zn2+, Co2+, or Mg2+ as cofactor
Fe2+
-
activates, required for enzyme inhibition by inhibitor 1, overview
Fe2+
-
activates
Fe2+
-
activates, tight binding to the enzyme
Fe2+
P9WK19
activates
Fe2+
-
activates slightly
Fe2+
A3M623, A3M752
activator after removal of divalent metal ions with Chelex-100; activator after removal of divalent metal ions with EDTA
Mg2+
-
slight activation
Mg2+
-
isoform MAP, may substitute for Co2+
Mg2+
-
the enzyme activity is enhanced 2fold by 1 mM Mg2+
Mg2+
-
activates
Mg2+
-
activates, required for enzyme inhibition by inhibitor 1, overview
Mg2+
-
activates slightly
Mn2+
-
activates apoenzyme
Mn2+
-
stimulates activity of MetAP2 with Met-Ala-Ser or Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr 10-20fold, maximal stimulation at 0.001 mM. In presence of 5 mM glutathione 30-40fold stimulation
Mn2+
P56218
enzyme contains 2 Mn-ions residing in a distorted trigonal bipyramidal geometry. A bridging water molecule is displaced by L-methionine
Mn2+
-
may substitute for Co2+
Mn2+
-
activation requires only one equivalent of Co2+ or Mn2+
Mn2+
-
MetAP requires a divalent metal ion for activation, such as Mn2+
Mn2+
-
Mn2+ also activates
Mn2+
-
activity requires divalent cations like Mn2+
Mn2+
-
activates
Mn2+
-
activates, required for enzyme inhibition by inhibitor 1, overview
Mn2+
-
activates
Mn2+
-
activates slightly
Mn2+
P9WK19
activates
Mn2+
-
activates
Na+
-
some positive effect on the enzyme activity at 5 mM
NH4+
-
some positive effect on the enzyme activity at 5 mM
Ni2+
-
enzyme is active at concentrations below 0.002 mM, inhibition at higher concentrations
Ni2+
-
activates apoenzyme with Met-7-amido-4-methylcoumarin as substrate, very poor activity in presence of Met-S-Gly-Phe as substrate
Ni2+
-
may substitute for Co2+
Ni2+
-
activates
Ni2+
-
most efficient activator, tight binding to the enzyme
Ni2+
P9WK19
activates
Ni2+
A3M623, A3M752
activator after removal of divalent metal ions with Chelex-100; activator after removal of divalent metal ions with EDTA, less efficient than Fe2+
Zinc
-
1 mol of wild-type enzyme contains 2 mol of Zn2+, zinc fingers are essential for normal MAP function
Zinc
-
methionine aminopeptidase type 1 requires its N-terminal zinc finger domain for normal function in vivo
Zn2+
-
1 mol of wild-type enzyme contains 2 mol of zinc ions and at least 1 mol of cobalt ion, whereas 1 mol of the truncated methionine aminopeptidase DELTA2-69 lacking the putative zinc fingers cotains only a trace amount of zinc ions but still contains one mol of cobalt ion
Zn2+
-
optimal concentration
Zn2+
-
activates apoenzyme
Zn2+
-
0.0001-0.001 mM, activity of MetAP2 is enhanced 5-10fold; Zn2+ is the best metal cofactor for MetAP1
Zn2+
-
inhibitory above 0.031 mM
Zn2+
-
isoform MAP, may substitute for Co2+
Zn2+
Q6UB28
slight activation
Zn2+
-
methionine aminopeptidase can be recognized as a dizinc enzyme
Zn2+
-
requires Zn2+, Co2+, or Mg2+ as cofactor
Zn2+
-
activates
Mn2+
-
activation constant 0.003 mM
additional information
-
the purified preparations do not contain significant amounts of any metal. Enzymatically important metal is loosely associated and lost during enzyme purification
additional information
-
not activating: Ni2+, Mg2+, Ca2+, Cd2+, Cu2+
additional information
-
activating potencies of divalent metal ions with the three isozymes, overview
additional information
-
MetAP can be activated in vitro by a number of divalent metals
additional information
-
MetAp requires divalent metal ions for catalytic activity
additional information
-
poor activation by Mn2+
additional information
-
MetAP belongs to the dinuclear metallohydrolases, mathematical model and detailed analysis of the stoichiometric activation of MetAP by metal cofactors, overview
additional information
-
MetAPs are metalloproteases
additional information
P9WK19
MetAP is one of the dinuclear metallohydrolases. MetAP1c requires divalent cations for activity. Co2+ and Fe2+ show the tightest binding, while Ni2+ is the most efficient cofactor for the catalysis. Metal binding kinetics, overview
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
((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
(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
-
IC50: 0.0229
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
-
IC50: 0.095 mM
(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
-
-
1,10-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
-
Co(II)-form of enzyme, 50% inhibition at 0.0089 mM
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
-
Co(II)-form of enzyme, 50% inhibition at 0.00046 mM
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
-
Co(II)-form of enzyme, 50% inhibition at 0.00050 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-((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
-
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-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
P0A080
50% inhibition at 0.019 mM, formation of uncleavable tetrahedral intermediate upon binding
2-amino-4-(methylthio)-1-pyridin-2-ylbutan-1-one
P0A080
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-mercaptoethanol
-
-
2-mercaptoethanol
-
complete inhibition at 10 mM
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
P50579
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
-
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-((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
P50579
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
-
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-(2,3-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
-
IC50: 0.0016 mM
-
3-(2-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
0.015 mM
-
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
-
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-methyl-1,3-thiazol-4-yl)phenol
-
-
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-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
-
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-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
-
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-(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
-
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-(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
P0A080
50% inhibition at 0.007 mM, formation of uncleavable tetrahedral intermediate upon binding
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-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
-
IC50: 0.00089 mM
3-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 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-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
-
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-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
-
IC50: 0.00187 mM
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00486 mM
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
-
IC50: 0.00192 mM
-
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0537
-
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
-
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-[(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
-
IC50: 0.0021 mM
-
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0099 mM
-
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
-
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-(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
-
specific inhibition of Fe2+-loaded MetAP
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
-
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-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
A3M623, A3M752
;
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
-
; 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
A3M623, A3M752
;
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
-
-
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
-
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
A3M623, A3M752
;
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-chlorophenyl)furan-2-carboxylic acid
-
-
5-(2-chlorophenyl)furan-2-carboxylic acid
A3M623, A3M752
;
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
-
Co(II)-form of enzyme, 50% inhibition at 0.00515 mM
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
-
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
-
Co(II)-form of enzyme, 50% inhibition at 0.00431 mM
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
P50579
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
-
Co(II)-form of enzyme, 50% inhibition at 0.00716 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
-
Co(II)-form of enzyme, 50% inhibition at 0.00122 mM
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
-
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-(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-[(2,4-dichlorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
A3M623, A3M752
;
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-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
A3M623, A3M752
;
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
5-[(4-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
A3M623, A3M752
;
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
-
potent and selective inhibitor
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-amido-4-methylcoumarin
-
product inhibition
-
7-amino-4-methylcoumarin
-
-
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+
A-357300
-
reversible
A-357300
-
-
A-357300
-
-
A-357300
-
potent MetAP2 inhibitor
A-800141
-
-
A-800141
-
-
A-800141
-
potent MetAP2 inhibitor
actinonin
-
12.6% relative activity at 0.05 mM
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
bengamide B
-
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
bengamide E
Q7SXK1
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
-
44.9% relative activity at 0.05 mM
butaneboronic acid
-
substrate analog
Ca2+
-
50% inhibition at 2 mM, 52% inhibition at 4 mM
Ca2+
-
slight inhibition
Co2+
-
1.0 mM CoCl2, 58% inhibition
Co2+
-
inhibitory above 0.0625 mM, activating below
Co2+
-
in excess, a third Co2+ ion binds to the active site regions and results in inhibition
Co2+
Q6UB28
inhibitory at 0.1 mM
Cu2+
-
52% inhibition at 2 mM, 88% inhibition at 4 mM
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
EDTA
-
-
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
E0A9F0
-
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
Fe2+
-
1 mM, complete inhibition
fumagalone
-
-
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
-
fumagillin covalently modifies a conserved active-site histidine in the Escherichia coli methionine aminopeptidase
fumagillin
-
irreversible
fumagillin
-
IC50 above 0.1 mM
fumagillin
-
inhibition of type II enzyme
fumagillin
-
Co(II)-form of enzyme, 50% inhibition at 0.000915 mM
fumagillin
-
MetAP2-specific inhibitor
fumagillin
-
irreversible inhibition
fumagillin
-
selectively inhibits MetAP2
fumagillin
-
10 nM
fumagillin
Q7SXK1
specific inhibitor
fumagillin
-
-
fumagillin
P50579, P53582
higher affinity to MetAP2 than to MetAP1; lower affinity to MetAP1 than to MetAP2
fumagillin
-
-
fumagillin
-
-
fumagillin
-
potent MetAP2 inhibitor
fumagillin
-
targets MetAP2, no binding to MetAP1 isozymes
fumagillin
-
binding structure, overview
fumagillin
B7XJ30
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
-
binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview
fumagillin
-
inhibitor of MetAP2
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
-
selective inhibitor
fumarranol
-
-
fumarranol
-
binds to MetAP2 noncovalently and reversibly
Hg2+
-
1 mM, complete inhibition
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
IV-43
-
MetAP1-specific inhibitor
IV-43
-
reversible MetAP-1 inhibitor
IV-43
-
-
L-Met
-
product inhibition
L-Met-(RS)-sulfoxide
-
-
L-methionine
P56218
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+
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
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)-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
-
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)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-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
-
Co(II)-form of enzyme, 50% inhibition at 0.0071 mM
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 0.000063 mM, binds to an additional Co2+ ion at the entrance of the active site
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
-
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-cyclopentyl-N-(thiazol-2-yl)oxalamide
-
potent and selective inhibitor
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)-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-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
-
-
Ni2+
-
1 mM, complete inhibition
Nitrilotriacetic acid
-
-
norleucine phosphonate
-
-
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
P50579, P53582
higher affinity to MetAP2 than to MetAP1; lower affinity to MetAP1 than to MetAP2
ovalicin
-
-
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
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
-
-
PPI-2458
-
-
PPI-2458
-
irreversible
PPI-2458
-
1-10 nM, selective non-reversible inhibition of MetAP-2
PPI-2458
-
potent inhibitor, 80% inhibition at 100 mg/kg
PPI-2458
-
potent selective inhibitor of MetAP2
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
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
-
-
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
-
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
Q7SXK1
specific inhibitor
TNP-470
-
selective covalent MetAP-2 inhibitor
TNP-470
-
potent selective inhibitor of MetAP2
TNP-470
-
irreversible inhibitor
TNP-470
P50579, P53582
;
TNP-470
-
potent MetAP2 inhibitor
TNP-470
-
a fumagillin derivative, targets MetAP2, no binding to MetAP1 isozymes
TNP-470
-
AGM-1470
TNP-470
-
binding structure, overview
TNP-470
B7XJ30
binding structure, overview
TNP-470
-
binding structure, specificity determinants lie in the S1 hydrophobic methionine binding subsite, overview
TNP-470
-
inhibitor of MetAP2 and anticancer drug
XC-11
-
a pyridinyl-pyrimidine inhibitor selective for MetAP1b
Zn2+
-
0.1 mM, complete inhibition
Zn2+
-
71% inhibition at 5 mM
Zn2+
-
inhibitory above 0.031 mM, activating below
Zn2+
-
slight inhibition
[(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
-
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
Mn2+
-
1 mM, complete inhibition
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
-
a set of inhibitors displayed completely different inhibitory profiles on the two mycobacterial MetAPs in both potency and metalloform selectivity
-
additional information
-
identification of pyridinyl-pyrimidine inhibitors with selectivity to isozyme MetAP1b before MetAP1a and MetAP1c
-
additional information
-
inhibitor synthesis, pharmacokinetics, and molecular modelling
-
additional information
P9WK19
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
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
2-mercaptoethanol
-
activates
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.14
L-Leu-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
0.35
L-Leu-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70A, pH 7.0, 22C
0.6
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97N, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
1.1
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97A, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
1.3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Mn2+
1.5
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H79A, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
1.8
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H79A, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
1.8
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97E, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
3.1
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
3.2
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
12
L-Met-L-Ala-L-Ser
-
wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
15
L-Met-L-Ala-L-Ser
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
0.74
L-Met-L-Pro-4-nitroanilide
-
wild-type, pH 7.5, 22C
1.8
L-Met-L-Pro-4-nitroanilide
-
truncated mutant lacking N-terminal 89 amino acids, pH 7.5, 22C
1
L-Met-L-Ser-L-Ser-L-His-L-Arg-L-Trp-L-Asp-L-Trp
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C; wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
0.59
L-Met-p-nitroanilide
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
3
L-Met-p-nitroanilide
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
0.35
L-Met-PSI[C(O)S]Gly-L-Phe
P0AE18
wild-type, pH 7.0, 22C
0.68
L-Met-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
1.24
L-Met-PSI[C(O)S]Gly-L-Phe
-
Co(II)-form of enzyme, 22C, pH 7.0
1.28
L-Met-PSI[C(O)S]Gly-L-Phe
-
N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
1.88
L-Met-PSI[C(O)S]Gly-L-Phe
-
wild-type, pH 7.0, 22C
6.75
L-Met-PSI[C(O)S]Gly-L-Phe
-
Zn(II)-form of enzyme, 22C, pH 7.0
8.81
L-Met-PSI[C(O)S]Gly-L-Phe
-
N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
16
L-Met-PSI[C(O)S]Gly-L-Phe
-
Mn(II)-form of enzyme, 22C, pH 7.0
0.011
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Ni2+
0.082
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Co2+
0.161
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Fe2+
0.17
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Mn2+
0.24
L-Phe-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
0.111
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.115
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.13
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.144
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.154
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.155
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.161
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.168
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.67
Met-4-nitroanilide
-
pH 7.5, 30C
0.12
Met-7-amido-4-methylcoumarin
-
pH 7.5, 30C, in presence of 0.01 mM CoCl2
1.24
Met-7-amido-4-methylcoumarin
-
pH 7.0, Ni2+-substituted enzyme
4.32
Met-7-amido-4-methylcoumarin
-
pH 7.0, Co2+-substituted enzyme
6.27
Met-7-amido-4-methylcoumarin
-
pH 7.0, Mn2+-substituted enzyme
1.5
Met-Ala-Ala
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
2.1
Met-Ala-Ala
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
5.2
Met-Ala-Ala
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
0.625
Met-Ala-His-Thr-Leu-Pro-Glu-Glu-Leu
-
-
0.05
Met-Ala-Met-Lys-Ser
-
at 30C
0.018
Met-Ala-Ser
-
pH 7.5, 37C, isozyme MetAP1a
0.38
Met-Ala-Ser
-
pH 7.5, 30C
0.394
Met-Ala-Ser
-
pH 7.5, 37C, isozyme MetAP1c
1.36
Met-Ala-Ser
-
pH 7.5, 30C
1.95
Met-Ala-Ser
-
pH 8.5, 37C, recombinant MetAP2
2.08
Met-Ala-Ser
-
pH 8.5, 37C
2.1
Met-Ala-Ser
-
37C truncated mutant enzyme DELTA2-69; truncated enzyme
2.67
Met-Ala-Ser
-
37C, wild-type enzyme
3
Met-Ala-Ser
-
pH 7.4
3.3
Met-Ala-Ser
-
pH 7.5, 30C
4.54
Met-Ala-Ser
-
pH 7.4, 37C mutant enzyme D219N
0.139
Met-Ala-Ser-Trp
-
pH 7.25, 30C
1.9
Met-Gly-Gly
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
2.3
Met-Gly-Gly
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
5.8
Met-Gly-Gly
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
0.058
Met-Gly-Met-Met
-
pH 7.5, 37C, isozyme MetAP1c
0.2144
Met-Gly-Met-Met
-
wild-type enzyme
0.328
Met-Gly-Met-Met
-
pH 7.5, 37C, isozyme MetAP1a
0.34
Met-Gly-Met-Met
-
pH 7.5, 30C
0.457
Met-Gly-Met-Met
-
mutant enzyme C70S
0.6559
Met-Gly-Met-Met
-
mutant enzyme W221L
0.9
Met-Gly-Met-Met
-
at 30C
1.2
Met-Gly-Met-Met
-
Mn2+-activated enzyme, pH 7.5, 21C
1.95
Met-Gly-Met-Met
-
pH 7.5, 30C, Fe(II)-substituted enzyme
2
Met-Gly-Met-Met
-
wild-type enzyme and mutant enzyme H178A, Fe(II) loaded, pH 7.5
2.85
Met-Gly-Met-Met
-
pH 7.5, 30C
3.16
Met-Gly-Met-Met
-
pH 7.5, 30C, Co(II)-substituted enzyme
3.2
Met-Gly-Met-Met
-
wild-type enzyme and mutant enzyme H178A, Co(II) loaded, pH 7.5
5
Met-Gly-Met-Met
-
37C, truncated mutant enzyme DELTA2-69
5.1
Met-Gly-Met-Met
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
6.56
Met-Gly-Met-Met
-
37C, wild-type enzyme
13.9
Met-Gly-Met-Met
-
pH 7.4, 37C mutant enzyme D219N
18.3
Met-Gly-Met-Met
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
0.3273
Met-peptide
-
-
-
2.8
Met-Pro
-
pH 7.5, 30C
0.06
Met-Pro-4-nitroanilide
-
wild-type enzyme, Co(II) loaded, pH 7.5
0.09
Met-Pro-4-nitroanilide
-
wild-type enzyme, Fe(II) loaded, pH 7.5
0.12
Met-Pro-4-nitroanilide
-
mutant enzyme H178A, Co(II) loaded, pH 7.5
0.13
Met-Pro-4-nitroanilide
-
mutant enzyme H178A, Fe(II) loaded, pH 7.5
0.75
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Mn2+
1.41
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Co2+
3.26
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Zn2+
0.28
Met-Pro-His-Thr-Leu-Pro-Glu-Glu
-
-
0.18
Met-Pro-p-nitroanilide
-
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
0.576
Met-Pro-p-nitroanilide
Q6UB28
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
0.86
Met-S-Gly-Phe
-
pH 7.0, Co2+-substituted enzyme
2.01
Met-S-Gly-Phe
-
pH 7.0, Zn2+-substituted enzyme
3.89
Met-S-Gly-Phe
-
pH 7.0, Mn2+-substituted enzyme
0.85
Met-Ser
-
pH 7.5, 30C
1.3
Met-Thr
-
pH 7.5, 30C
1.2
Met-Val
-
pH 7.5, 30C
2
Nle-4-nitroanilide
-
pH 7.5, 30C
0.222
Met-Val-His-Thr-Leu-Pro-Glu-Glu-Leu
-
-
additional information
additional information
-
Km-values of truncated enzsme
-
additional information
additional information
-
-
-
additional information
additional information
P9WK19
metal binding kinetics, overview
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
4.04
L-Leu-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
20.8
L-Leu-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70A, pH 7.0, 22C
0.001
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97N, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
0.002
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97E, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
0.003
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H79A, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
0.003
L-Met-Gly-L-Met-L-Met
-
mutant enzyme D97A, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
1.8
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H79A, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
4.6
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Mn2+
4.8
L-Met-Gly-L-Met-L-Met
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
18.3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer (pH 7.5) containing 150 mM KCl, in the presence of 3 equivalents of Co2+
18.3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
18.3
L-Met-Gly-L-Met-L-Met
-
wild type enzyme, Co2+-loaded, in 25 mM HEPES buffer, at 30C and pH 7.5
3
L-Met-L-Ala-L-Ser
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
11
L-Met-L-Ala-L-Ser
-
wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
0.11
L-Met-L-Pro-4-nitroanilide
-
wild-type, pH 7.5, 22C
0.425
L-Met-L-Pro-4-nitroanilide
-
truncated mutant lacking N-terminal 89 amino acids, pH 7.5, 22C
70
L-Met-L-Ser-L-Ser-L-His-L-Arg-L-Trp-L-Asp-L-Trp
-
mutant enzyme H63A, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
84
L-Met-L-Ser-L-Ser-L-His-L-Arg-L-Trp-L-Asp-L-Trp
-
wild type enzyme, in 25 mM HEPES buffer, pH 7.5, and 150 mM KCl, at 30C
0.006
L-Met-p-nitroanilide
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
0.97
L-Met-PSI[C(O)S]Gly-L-Phe
-
N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
3.6
L-Met-PSI[C(O)S]Gly-L-Phe
-
Co(II)-form of enzyme, 22C, pH 7.0
6.47
L-Met-PSI[C(O)S]Gly-L-Phe
-
wild-type, pH 7.0, 22C
7.31
L-Met-PSI[C(O)S]Gly-L-Phe
-
N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
12.8
L-Met-PSI[C(O)S]Gly-L-Phe
-
Zn(II)-form of enzyme, 22C, pH 7.0
15.8
L-Met-PSI[C(O)S]Gly-L-Phe
-
Mn(II)-form of enzyme, 22C, pH 7.0
16.61
L-Met-PSI[C(O)S]Gly-L-Phe
-
N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
22.5
L-Met-PSI[C(O)S]Gly-L-Phe
P0AE18
wild-type, pH 7.0, 22C
30.8
L-Met-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
0.014
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Fe2+
0.045
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Ni2+
0.07
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Mn2+
0.36
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Co2+
3.3
L-Phe-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
4.55
L-Phe-PSI[C(O)S]Gly-L-Phe
P0AE18
mutant C70S, pH 7.0, 22C
0.0000508
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.000055
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
0.000137
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.000159
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
0.000263
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.000305
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.000312
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
0.000449
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
0.158
Met-4-nitroanilide
-
pH 7.5, 30C
0.00164
Met-7-amido-4-methylcoumarin
-
pH 7.0, Ni2+-substituted enzyme
0.0059
Met-7-amido-4-methylcoumarin
-
pH 7.0, Mn2+-substituted enzyme
0.0114
Met-7-amido-4-methylcoumarin
-
pH 7.0, Co2+-substituted enzyme
0.0633
Met-7-amido-4-methylcoumarin
-
pH 7.5, 30C, in presence of 0.01 mM CoCl2
15.57
Met-Ala-Ala
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
20.02
Met-Ala-Ala
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
22.07
Met-Ala-Ala
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
3.9
Met-Ala-Met-Lys-Ser
-
at 30C
0.00325
Met-Ala-Ser
-
pH 7.4, 37C mutant enzyme D219N
0.0517
Met-Ala-Ser
-
pH 7.4, MetAP2
3.5
Met-Ala-Ser
-
pH 7.5, 30C
11.7
Met-Ala-Ser
-
calculated with 29.5 kDa as molecular mass, pH 7.5, 30C
19.6
Met-Ala-Ser
-
37C, wild-type enzyme
19.8
Met-Ala-Ser
-
pH 7.5, 37C, isozyme MetAP1a, with Co2+
74.3
Met-Ala-Ser
-
pH 7.5, 37C, isozyme MetAP1c, with Co2+
1516
Met-Ala-Ser
-
calculated with 33.1 kDa as molecular mass, pH 7.5, 30C
8.45
Met-Ala-Ser-Trp
-
pH 7.25, 30C
0.0683
Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr
-
pH 7.4, MetAP2
15.25
Met-Gly-Gly
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
19.87
Met-Gly-Gly
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
21.87
Met-Gly-Gly
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
0.0427
Met-Gly-Met-Met
-
pH 7.4, 37C mutant enzyme D219N
0.54
Met-Gly-Met-Met
-
mutant enzyme H178A, Co(II) loaded, pH 7.5
0.56
Met-Gly-Met-Met
-
mutant enzyme H178A, Fe(II) loaded, pH 7.5
0.67
Met-Gly-Met-Met
-
mutant enzyme W221L
0.78
Met-Gly-Met-Met
-
mutant enzyme C70S
1.16
Met-Gly-Met-Met
-
wild-type enzyme
2.83
Met-Gly-Met-Met
-
pH 7.5, 30C
9.63
Met-Gly-Met-Met
-
calculated with 29.5 kDa as molecular mass, pH 7.5, 30C
11.5
Met-Gly-Met-Met
-
pH 7.5, 37C, isozyme MetAP1a
18.3
Met-Gly-Met-Met
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
23.6
Met-Gly-Met-Met
-
37C, wild-type enzyme
28
Met-Gly-Met-Met
-
wild-type enzyme, Fe(II) loaded, pH 7.5
38
Met-Gly-Met-Met
-
at 30C
39
Met-Gly-Met-Met
-
wild-type enzyme, Co(II) loaded, pH 7.5
39.4
Met-Gly-Met-Met
-
pH 7.5, 37C, isozyme MetAP1c
188
Met-Gly-Met-Met
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
0.232
Met-peptide
-
-
-
0.13
Met-Pro
-
pH 7.5, 30C
1.75
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Mn2+
2.67
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Zn2+
11.9
Met-Pro-4-nitroanilide
-
pH 7.5, in presence of Co2+
0.002
Met-Pro-p-nitroanilide
-
mutant enzyme H178A, Co(II) loaded, pH 7.5
0.0065
Met-Pro-p-nitroanilide
Q6UB28
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
0.01
Met-Pro-p-nitroanilide
-
mutant enzyme H178A, Fe(II) loaded, pH 7.5
0.59
Met-Pro-p-nitroanilide
-
wild-type enzyme, Co(II) loaded, pH 7.5
1.4
Met-Pro-p-nitroanilide
-
wild-type enzyme, Fe(II) loaded, pH 7.5
1.82
Met-Pro-p-nitroanilide
-
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
11.1
Met-S-Gly-Phe
-
pH 7.0, Zn2+-substituted enzyme
20.2
Met-S-Gly-Phe
-
pH 7.0, Co2+-substituted enzyme
42.5
Met-S-Gly-Phe
-
pH 7.0, Mn2+-substituted enzyme
0.00617
Met-Ser
-
pH 7.5, 30C
0.01
Met-Thr
-
pH 7.5, 30C
0.0133
Met-Val
-
pH 7.5, 30C
0.0733
Nle-4-nitroanilide
-
pH 7.5, 30C
0.057
L-Met-p-nitroanilide
-
in 25 mM HEPES buffer at 30C (pH 7.5) with 150 mM KCl
additional information
L-Met-PSI[C(O)S]Gly-L-Phe
-
wild-type, pH 7.0, 22C
5.33
Met-Val-Ser-His-Arg-Trp-Asp-Trp
-
pH 7.25, 30C
additional information
additional information
-
turnover-numbers of truncated enzyme
-
additional information
additional information
-
-
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.41
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Mn2+
8868
0.87
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Fe2+
8868
4.39
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Co2+
8868
40.91
L-methionine-4-methylcoumarin-7-amide
-
recombinant isozyme MetAP1a in presence of Ni2+
8868
1.7
MAEIEIY
-
pH 7.4, temperature not specified in the publication
0
14
MAEIEIY
-
pH 7.4, temperature not specified in the publication
0
5.3
MAEWEIY
-
pH 7.4, temperature not specified in the publication
0
10
MAGAIHY
-
pH 7.4, temperature not specified in the publication
0
13.5
MAGIEIY
-
pH 7.4, temperature not specified in the publication
0
41
MAHAIHY
-
pH 7.4, temperature not specified in the publication
0
3.58
MAHIEIY
-
pH 7.4, temperature not specified in the publication
0
14.5
MAHIEIY
-
pH 7.4, temperature not specified in the publication
0
1.3
MAPIEIY
-
pH 7.4, temperature not specified in the publication
0
6.6
MARIEIY
-
pH 7.4, temperature not specified in the publication
0
18.9
MARIEIY
-
pH 7.4, temperature not specified in the publication
0
9.6
MAWIEIY
-
pH 7.4, temperature not specified in the publication
0
0.00033
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
4141
0.000479
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Mn2+, pH not specified in the publication, temperature not specified in the publication
4141
0.000948
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
4141
0.00105
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Co2+, pH not specified in the publication, temperature not specified in the publication
4141
0.0017
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
4141
0.00217
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.020 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
4141
0.00275
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.005 mM Ni2+, pH not specified in the publication, temperature not specified in the publication
4141
0.00278
Met-4-methylcoumaryl-7-amide
A3M623, A3M752
after removal of divalent metal ions activated with 0.0025 mM Fe2+, pH not specified in the publication, temperature not specified in the publication
4141
3
Met-Ala-Ala
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
12110
9.53
Met-Ala-Ala
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
12110
14.72
Met-Ala-Ala
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
12110
3.32
Met-Ala-Ser
-
pH 7.5, 30C
2345
1156
Met-Ala-Ser
-
pH 7.5, 30C
2345
2.63
Met-Gly-Gly
-
recombinant isozyme c2MetAP-Ia, pH 7.2, 37C
8245
8.63
Met-Gly-Gly
-
recombinant isozyme c1MetAP-Ia, pH 7.2, 37C
8245
11.52
Met-Gly-Gly
-
recombinant isozyme c3MetAP-Ib, pH 7.2, 37C
8245
3.47
Met-Gly-Met-Met
-
pH 7.5, 30C
2027
0.18
MGEIEIY
-
pH 7.4, temperature not specified in the publication
0
4.1
MGEIEIY
-
pH 7.4, temperature not specified in the publication
0
0.16
MPEIEIY
-
pH 7.4, temperature not specified in the publication
0
3
MPEIEIY
-
pH 7.4, temperature not specified in the publication
0
28
MSDFIGY
-
pH 7.4, temperature not specified in the publication
0
0.029
MTEIEIY
-
pH 7.4, temperature not specified in the publication
0
1.5
MTEIEIY
-
pH 7.4, temperature not specified in the publication
0
0.13
MVAAAAY
-
pH 7.4, temperature not specified in the publication
0
0.38
MVEIEIY
-
pH 7.4, temperature not specified in the publication
0
0.028
MVGVKPY
-
pH 7.4, temperature not specified in the publication
0
0.064
MVHQVLY
-
pH 7.4, temperature not specified in the publication
0
0.007
MVKIEIY
-
pH 7.4, temperature not specified in the publication
0
0.015
MVLSPAY
-
pH 7.4, temperature not specified in the publication
0
0.013
MVNPTVY
-
pH 7.4, temperature not specified in the publication
0
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.002
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.003
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.02
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.003
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.008
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.44
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.75
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.000001
3-(anilino)-5-(3-methyl-2-butenylthio)-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000015
3-(N-methyl-anilino)-5-benzylthio-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000066
3-anilino-5-(3-methyl-butylthio)-methylthio-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.0000005
3-anilino-5-benzylthio-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.01
3-anilino-5-benzylthio-1-methyl-1,2,4-triazole
-
IC50 above 0.01 mM, in 50 mM HEPES-Na+ (pH 7.5), with 100 mM NaCl
0.0013
3-anilino-5-benzylthio-2-methyl-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.001
3-anilino-5-methylthio-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000003
3-[2-(isopropyl)-anilino]-5-(furan-2-ylmethylthio)-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.000024
3-[2-(isopropyl)-anilino]-5-(furan-3-ylmethylthio)-1,2,4-triazole
-
in 50 mM HEPES (pH 7.5), with 100 mM NaCl
0.00000004
5-(benzylsulfanyl)-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000017
5-(benzylsulfanyl)-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000043
5-(benzylsulfanyl)-N-(4-chlorophenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000005
5-(benzylsulfanyl)-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000007
5-(benzylsulfanyl)-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00074
5-(benzylsulfanyl)-N-biphenyl-2-yl-4H-1,2,4-triazol-3-amine
-
apparent value
0.162
5-[(2E)-hepta-2,6-dien-4-yn-1-ylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
0.00000015
5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000033
5-[(cyclohexylmethyl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000083
5-[(cyclohexylmethyl)sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000031
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0001
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000012
5-[[(2-methyl-2,5-dihydro-1,3-thiazol-4-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000036
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000035
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000078
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000023
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000013
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000065
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.000061
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.01
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
Ki above 0.01 mM, apparent value
0.0000024
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.000004
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000021
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000033
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.29
7-amino-4-methylcoumarin
-
pH 7.5, 30C
0.0000016
fumagillin
-
pH 7.5, 30C
0.02
L-Met
-
pH 7.5, 30C
0.18
L-Met-(RS)-sulfoxide
-
pH 7.5, 30C
150
L-methionine
P56218
pH 7.5
0.0000005
methyl 4-([5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000027
methyl 4-([5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000009
methyl 4-([5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000009
methyl 4-([5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000038
methyl 4-[(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000008
methyl 4-[(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.00000041
methyl 4-[(5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.00001
methyl 4-[(5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.000135
methyl 4-[(5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000013
methyl 4-[(5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000007
methyl 4-[[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]amino]benzoate
-
apparent value
0.0000037
N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000038
N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000025
N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000009
N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000024
N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000096
N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000021
N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000007
N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000013
N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.001
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.001 mM, apparent value
0.000018
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000052
N-(4-chlorophenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000052
N-(4-chlorophenyl)-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000004
N-(4-chlorophenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000025
N-(4-chlorophenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000048
N-(4-chlorophenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000018
N-(4-chlorophenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfany]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000061
N-(4-chlorophenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.01
N-(4-chlorophenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000023
N-(4-chlorophenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000016
N-(4-methoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000018
N-(4-methoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000061
N-(4-methoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000016
N-(4-methoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000034
N-(4-methoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000078
N-(4-methylphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000057
N-(4-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000052
N-(4-methylphenyl)-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000078
N-(4-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000065
N-(4-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000287
N-(5-chloroquinolin-8-yl)methanesulfonamide
-
Co(II)-form of enzyme
0.0287
N-(5-chloroquinolin-8-yl)methanesulfonamide
-
-
0.0000091
N-(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
apparent value
0.0000015
N-(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
apparent value
0.0343
N-(quinolin-8-yl)methanesulfonamide
-
-
0.00035
N-biphenyl-2-yl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.002
N-biphenyl-2-yl-5-[(2-methoxybenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.00048
N-biphenyl-2-yl-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00065
N-biphenyl-2-yl-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.002
N-biphenyl-2-yl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.0017
N-biphenyl-2-yl-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000075
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000343
N-quinolin-8-ylmethanesulfonamide
-
Co(II)-form of enzyme
0.0000015
N-[4-(chloromethyl)phenyl]-5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000004
N-[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000003
N-[5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000017
N-[5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000005
N-[5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.000003
N-[5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000057
N-[5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0004
thiabendazole
-
pH 7.5, 37C
0.000000245
[(1R)-1-carbamoyl-2-methyl-propyl]-carbamic acid-(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiranyl]-1-oxaspiro(2,5)oct-6-yl ester
-
recombinant MetAP-2, in 50 mM Hepes, 100 mM MnCl2, 100 mM NaCl, 0.005% (w/v) bovine serum albumin, 0.006% (w/v) 3-[(3-cholamidopropyl)dimethylammonio]propanesulphonic acid, at pH 7.5
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.02
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.027
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.032
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.034
((2RS,3R)-3-amino-2-hydroxy-5-ethylthio)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.0013
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.045
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Co2+, pH 7.5, 22C
0.067
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.068
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.141
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Ni2+, pH 7.5, 22C
0.179
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[(1-isobutyrylpiperidin-3-yl)-methyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.00054
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.0042
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.0045
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.0069
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.0079
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Co2+, pH 7.5, 22C
0.033
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Ni2+, pH 7.5, 22C
0.075
(2R,3R,4S,5R,E)-3,4,5-trihydroxy-N-[2-(mesityloxy)ethyl]-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Ni2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.00062
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.0037
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.014
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Fe2+, pH 7.5, 22C
0.021
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Co2+, pH 7.5, 22C
0.049
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.05
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Co2+, pH 7.5, 22C
0.114
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Ni2+, pH 7.5, 22C
0.12
(2R,3R,4S,5R,E)-N-(2-amino-2-oxoethyl)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamide
-
apoenyme activated by Ni2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Ni2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Ni2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Ni2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
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
-
apoenyme activated by Co2+, pH 7.5, 22C
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
-
apoenyme activated by Fe2+, pH 7.5, 22C
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
-
apoenyme activated by Mn2+, pH 7.5, 22C
0.0229
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
-
IC50: 0.0229 mM
0.095
(3R)-amino-(2S)-hydroxyheptanoyl-Ala-Leu methyl ester
-
IC50: 0.095 mM
0.0123
(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
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
in HUVEC
0.00021
(5,5-Dimethyl-4,5-dihydro-thiazol-2-yl)-(3-methyl-pyridin-2-yl)-amine
-
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
-
-
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
-
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
-
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
-
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
-
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
-
in HUVEC
0.009
1-(1H-benzimidazol-2-yl)thiourea
-
pH not specified in the publication, temperature not specified in the publication
0.0359
1-(1H-benzimidazol-2-yl)thiourea
-
pH not specified in the publication, temperature not specified in the publication
0.00312
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylmorpholin-4-yl)ethanone
-
-
0.00154
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(2-sulfanylphenyl)ethanone
-
-
0.00124
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-fluoro-2-sulfanylphenyl)ethanone
-
-
0.00102
1-(5-chloro-6-methyl-2-pyridin-2-yl-3,4-dihydropyrimidin-4-yl)-2-(4-methoxy-2-sulfanylphenyl)ethanone
-
-
0.0011
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
MetAP1
0.0081
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
MetAP2
0.00046
1-benzyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.00099
1-benzyl-2-(pyridin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0005
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0243
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0324
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.00118
1-[2-pyridin-2-yl-6-(trifluoromethyl)-3,4-dihydropyrimidin-4-yl]propane-2-thiol
-
-
0.00008
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
-
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
-
pH not specified in the publication, temperature not specified in the publication
0.0023
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
pH not specified in the publication, temperature not specified in the publication
0.0034
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
pH not specified in the publication, temperature not specified in the publication
0.0101
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
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
-
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
-
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
-
pH not specified in the publication, temperature not specified in the publication
0.00078
2-(1H-benzimidazol-2-yl)pyridin-3-ol
-
pH not specified in the publication, temperature not specified in the publication
0.0044
2-(1H-benzimidazol-2-yl)pyridin-3-ol
-
pH not specified in the publication, temperature not specified in the publication
0.0001
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
-
in HUVEC
0.000016
2-(2-aminoethoxy)-3-ethyl-6-[[(2-propylphenyl)sulfonyl]amino]benzoic acid
-
-
0.000046
2-(2-aminoethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
-
0.000024
2-(2-aminoethoxy)-6-[([2-[3-(diethylamino)propyl]-4-fluorophenyl]sulfonyl)amino]-3-ethylbenzoic acid
-
-
0.0058
2-(carboxymethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
-
0.0046
2-(pyrazin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0329
2-(pyrazin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.00097
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
pH not specified in the publication, temperature not specified in the publication
0.0049
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
pH not specified in the publication, temperature not specified in the publication
0.0093
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
-
pH not specified in the publication, temperature not specified in the publication
0.00057
2-(pyridin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0133
2-(pyridin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0199
2-(pyridin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.0284
2-(pyridin-2-yl)-1H-benzimidazole
-
pH not specified in the publication, temperature not specified in the publication
0.00043
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
pH not specified in the publication, temperature not specified in the publication
0.0329
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
pH not specified in the publication, temperature not specified in the publication
0.033
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
pH not specified in the publication, temperature not specified in the publication
0.0373
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
-
pH not specified in the publication, temperature not specified in the publication
0.00024
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
-
pH not specified in the publication, temperature not specified in the publication
0.022
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
-
pH not specified in the publication, temperature not specified in the publication
0.0401
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
-
pH not specified in the publication, temperature not specified in the publication
0.0484
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
-
pH not specified in the publication, temperature not specified in the publication
0.00011
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0188
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0267
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0276
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.00055
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.008
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0103
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0228
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
-
pH not specified in the publication, temperature not specified in the publication
0.0013
2-butyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
-
0.000015
2-chloro-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
-
0.00006
2-ethenyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
-
0.000038
2-ethoxy-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
-
0.000011
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methoxybenzoic acid
-
-
0.000016
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
-
0.00107
2-pyridin-2-yl-4-(trifluoromethyl)-6-[2-(trifluoromethyl)benzyl]-1,6-dihydropyrimidine
-
-
0.0039
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
-
-
0.000009
2-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
-
0.0011
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
-
-
0.02
2-[([4-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]phenyl]sulfinyl)oxy]hydrazinecarboximidamide
-
-
0.0296
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
-
IC50 for Co-EcMetAP1: 0.0296 mM
0.0365
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
-
IC50 for Zn-EcMetAP1: 0.0365 mM
0.0441
2-[2-(2-amino-4-methylsulfanyl-butyrylsulfanyl)-3-phenyl-propionylamino]-3-hydroxy-propionic acid
-
IC50 for Mn-EcMetAPa: 0.0441 mM
0.0286
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
-
IC50 for Co-EcMetAP1: 0.0286 mM
0.0357
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
-
IC50 for Ni-EcMetAP1: 0.0357 mM
0.0443
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
-
IC50 for Mn-EcMetAPa: 0.0443 mM
0.0498
2-[2-(2-Amino-4-methylsulfanyl-butyrylsulfanyl)-5-methyl-hexanoylamino]-3-hydroxy-propionic acid
-
IC50 for Zn-EcMetAP1: 0.0498 mM
0.0125
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
-
IC50 for Ni-EcMetAP1: 0.0125 mM
0.0167
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
-
IC50 for Zn-EcMetAP1: 0.0167 mM
0.0229
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
-
IC50 for Co-EcMetAP1: 0.0229 mM
0.0252
2-[2-(3-Amino-2-hydroxy-heptanoylamino)-propionylamino]-4-methyl-pentanoic acid methyl ester
-
IC50 for Mn-EcMetAPa: 0.0252 mM
0.037
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
0.011
2-[[(4-chlorophenyl)sulfonyl]amino]-5-methylbenzoic acid
-
-
0.00001
2-[[(4-fluorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
-
0.00002
2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6-dihydronaphthalene-1-carboxylic acid
-
-
0.00035
3,5-dimethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
-
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
-
in HUVEC
0.015
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
0.044
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Co2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
1
3-((2-naphthylmethyl)sulfanyl)-4H-1,2,4-triazole
-
Mn2+-loaded wild type enzyme, in 25 mM HEPES buffer, pH 7.5, containing 150 mM KCl, at 30C
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
-
in HUVEC
0.000034
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000034 mM
0.00492
3-(2,2,2-trifluoroacetylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00492 mM
0.00034
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00034 mM
0.00054
3-(2,2-dimethylpropionylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00054 mM
0.00068
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00068 mM
-
0.00078
3-(2,2-dimethylpropionyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00078 mM
-
0.0016
3-(2-acetyloxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0016 mM
-
0.00028
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00028 mM
0.1
3-(2-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
0.00083
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00083 mM
-
0.016
3-(2-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.016 mM
-
0.00089
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00089 mM
-
0.0013
3-(2-iodobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0013 mM
-
0.00055
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00055 mM
-
0.0017
3-(2-methoxybenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0017 mM
-
0.00028
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00028 mM
0.0109
3-(2-methylbut-2-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0109 mM
0.00039
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00039 mM
-
0.0044
3-(2-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0044 mM
-
0.0021
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
-
IC50: 0.0021 mM
-
0.1
3-(2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiatol-2-ylamide
-
IC50 above 0.1 mM
-
0.0025
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0025 mM
-
0.0034
3-(3-bromo-4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0034 mM
-
0.00071
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00071 mM
0.1
3-(3-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
0.000095
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000095 mM
-
0.1
3-(3-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
-
0.0017
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0017 mM
-
0.00302
3-(3-methoxy-2-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00302 mM
-
0.00022
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00022 mM
-
0.00077
3-(3-methylbut-2-enoylamino)pyridien-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00077 mM
-
0.00049
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00049 mM
-
0.0026
3-(3-methylbut-2-enoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0026 mM
-
0.00015
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00015 mM
0.00467
3-(3-methylbut-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00467 mM
0.0006
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0006 mM
-
0.1
3-(3-nitrobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
-
0.00136
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00136 mM
0.1
3-(4-fluorobenzoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
0.0011
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0011 mM
-
0.062
3-(4-fluorobenzoyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.062 mM
-
0.00014
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00014 mM
0.00024
3-(4-methylpent-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00024 mM
0.00031
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00031 mM
0.000671
3-(5-methylhex-4-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000671 mM
0.00013
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00013 mM
0.00038
3-(but-3-enoylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00038 mM
0.00087
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00087 mM
0.1
3-(cyclohexanecarbonylamino)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 above 0.1 mM
0.00032
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00032 mM
-
0.00239
3-(cyclohexanecarbonyloxy)pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00239 mM
-
0.0082
3-acetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0082 mM
-
0.0328
3-aminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 1.7 mM, IC50: 0.0328 mM
0.00089
3-benzoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00089 mM
0.00103
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00103 mM
-
0.00122
3-benzoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00122 mM
-
0.0001
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Co-EcMetAP1: 0.0001 mM
0.00076
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Ni-EcMetAP1: 0.00076 mM
0.0224
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Zn-EcMetAP1: 0.0224 mM
0.0233
3-But-3-enoylamino-pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50 for Mn-EcMetAPa: 0.0233 mM
0.000015
3-ethyl-2-methoxy-6-[[(2-[[2-(1-methylpyrrolidin-2-yl)ethyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
-
0.000018
3-ethyl-2-methoxy-6-[[(2-[[3-(2-methylpiperidin-1-yl)propyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
-
0.000067
3-ethyl-2-methyl-6-[(pyridin-2-ylsulfonyl)amino]benzoic acid
-
-
0.00032
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00032 mM
0.00033
3-formylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00033 mM
0.000038
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000038 mM
0.00062
3-hexanoylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00062 mM
0.000174
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000174 mM
-
0.00102
3-hexanoyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00102 mM
-
0.00187
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00187 mM
0.00486
3-hydroxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00486 mM
0.0015
3-imino-4-[(E)-(4-methoxyphenyl)diazenyl]-3H-pyrazol-5-amine
-
-
0.00025
3-imino-4-[(E)-[2-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
-
-
0.00025
3-imino-4-[(E)-[3-(trifluoromethyl)phenyl]diazenyl]-3H-pyrazol-5-amine
-
-
0.00192
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00192 mM
-
0.0537
3-iso-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0537 mM
-
0.00004
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00004 mM
0.00082
3-phenylacetylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00082 mM
0.000054
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.000054 mM
-
0.0002
3-phenylacetyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0002 mM
-
0.00026
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00026 mM
0.00035
3-propionylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00035 mM
0.00038
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00038 mM
-
0.0054
3-propionyloxypyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0054 mM
-
0.00018
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00018 mM
-
0.00335
3-tert-butoxycarbonylaminopyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.00335 mM
-
0.00058
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
P9WK19
pH 7.5, 37C, with Ni2+
0.002
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
P9WK19
pH 7.5, 37C, with Co2+
0.25
3-[(4-fluorobenzyl)sulfanyl]-4H-1,2,4-triazole
-
above, recombinant isozyme MetAP1a in presence of different divalent metal ions, overview
0.002
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]-2-hydroxybenzoic acid
-
-
0.00175
3-[(E)-(5-amino-3-imino-3H-pyrazol-4-yl)diazenyl]benzoic acid
-
-
0.000009
3-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
-
-
0.000019
3-[(phenylsulfonyl)amino]naphthalene-2-carboxylic acid
-
-
0.0021
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0021 mM
-
0.0099
3-[3-(2-methoxyphenyl)acryloyloxy]pyridine-2-carboxylic acid thiazol-2-ylamide
-
IC50: 0.0099 mM
-
0.000015
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
-
-
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
-
in HUVEC
0.0166
4-(1,3-thiazol-2-yl)benzene-1,2-diol
-
Fe2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.05 mM FeCl2 with 0.1 mM ascorbic acid
0.0161
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
-
using Fe2+-activated MetAP enzyme
0.0195
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
-
using Co2+-activated MetAP enzyme
0.0246
4-(1-benzyl-1H-1,2,3-triazol-4-yl)benzene-1,2-diol
-
using Mn2+-activated MetAP enzyme
0.1
4-(1-methyl-1H-imidazol-2-yl)benzene-1,2-diol
-
IC50 above 0.1 mM, using Fe2+, Co2+, or Mn2+-activated MetAP enzymes
0.0202
4-(2,5-dichlorothiophen-3-yl)benzene-1,2-diol
-
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
-
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
-
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
-
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
-
IC50 above 0.1 mM, Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2; 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
-
Co2+-loaded wild type enzyme, in 50 mM MOPS (pH 7.0), 0.01 mM CoCl2; 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
-
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
-
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
A3M623, A3M752
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
-
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
-
using Fe2+-activated MetAP enzyme
0.024
4-(2-methyl-1,3-thiazol-4-yl)benzene-1,2-diol
A3M623, A3M752
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
A3M623, A3M752
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
A3M623, A3M752
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
A3M623, A3M752
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
A3M623, A3M752
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
A3M623, A3M752
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
A3M623, A3M752
after removal of divalent metal ions activated with 0.02 mM Mn2+, pH not specified in the publication, temperature not specified in th