Information on EC 3.4.11.18 - methionyl aminopeptidase and Organism(s) Homo sapiens

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Homo sapiens


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


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
3.4.11.18
-
RECOMMENDED NAME
GeneOntology No.
methionyl aminopeptidase
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
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-
-
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
Ac/N-end rule pathway
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Arg/N-end rule pathway (eukaryotic)
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CAS REGISTRY NUMBER
COMMENTARY hide
61229-81-0
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
14-3-3gamma protein + H2O
?
show the reaction diagram
-
14-3-3gamma is a shared substrate between isoform MetAP1 and MetAP2 in HUVEC cells
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-
?
cyclophillin A + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
eukaryotic elongation factor-2 + H2O
?
show the reaction diagram
-
MetAP2-specific substrate
-
-
?
glyceraldehye 3-phosphate dehydrogenase + H2O
?
show the reaction diagram
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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-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 + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met-L-Ala-L-Ser + H2O
L-Met + L-Ala-L-Ser
show the reaction diagram
-
-
-
-
?
L-Met-L-Ala-L-Ser-L-Trp + H2O
?
show the reaction diagram
-
-
-
-
?
L-Met-L-Pro-4-nitroanilide + H2O
L-Met + L-Pro-4-nitroanilide
show the reaction diagram
-
-
-
-
?
L-Met-L-Pro-p-nitroanilide + H2O
L-Met + L-Pro-p-nitroanilide
show the reaction diagram
-
-
-
-
?
L-Met-N-myristoyltransferase + H2O
L-Met + N-myristoyltransferase
show the reaction diagram
-
-
-
-
?
L-Met-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
L-methionine-7-amido-4-methylcoumarin + H2O
L-methionine + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Nle-L-Ala-L-Ser + H2O
?
show the reaction diagram
-
-
-
-
?
L-Phe-L-Ala-L-Ser-L-Trp + H2O
?
show the reaction diagram
-
-
-
-
?
L-Phe-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
L-Thr-PSI[C(O)S]Gly-L-Phe + H2O
?
show the reaction diagram
-
-
-
-
?
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
-
-
-
-
?
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-nitroanilide + H2O
Met + 4-nitroaniline
show the reaction diagram
-
-
-
-
?
Met-7-amido-4-methylcoumarin + H2O
Met + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Met-Ala + H2O
Met + Ala
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser + H2O
Met + Ala-Ser
show the reaction diagram
-
-
-
-
?
Met-Ala-Ser-Lys-(biotin)-Gly + H2O
Met + Ala-Ser-Lys-(biotin)-Gly
show the reaction diagram
-
-
-
-
?
Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr + H2O
Met + Gly-Ala-Gln-Phe-Ser-Lys-Thr
show the reaction diagram
-
-
-
-
?
Met-Gly-Met-Met + H2O
Gly-Met-Met + Met
show the reaction diagram
-
-
-
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?
Met-Gly-Met-Met + H2O
Met + Gly-Met-Met
show the reaction diagram
-
-
-
-
?
Met-peptide + H2O
Met + peptide
show the reaction diagram
Met-Pro + H2O
Met + Pro
show the reaction diagram
-
-
-
-
?
Met-Pro-p-nitroanilide + H2O
Pro-p-nitroanilide + Met
show the reaction diagram
-
-
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?
Met-Ser + H2O
Met + Ser
show the reaction diagram
-
-
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?
Met-Thr + H2O
Met + Thr
show the reaction diagram
-
-
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-
?
Met-Val + H2O
Met + Val
show the reaction diagram
-
-
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?
MGEIEIY + H2O
L-Met + GEIEIY
show the reaction diagram
-
-
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?
MGKVKVGV + H2O
L-Met + GKVKVGV
show the reaction diagram
N-terminal peptide of glyceraldehyde 3-phosphate dehydrogenase
-
-
?
MGNLKSVA + H2O
L-Met + GNLKSVA
show the reaction diagram
N-terminal peptide of endothelial nitric oxide synthase
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-
?
MPEIEIY + H2O
L-Met + PEIEIY
show the reaction diagram
-
-
-
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?
MTEIEIY + H2O
L-Met + TEIEIY
show the reaction diagram
-
-
-
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?
MVAAAAY + H2O
L-Met + VAAAAY
show the reaction diagram
-
-
-
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?
MVEIEIY + H2O
L-Met + VEIEIY
show the reaction diagram
-
-
-
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?
MVGVKPY + H2O
L-Met + VGVKPY
show the reaction diagram
-
-
-
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?
MVHQVLY + H2O
L-Met + VHQVLY
show the reaction diagram
-
-
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?
MVKIEIY + H2O
L-Met + VKIEIY
show the reaction diagram
-
-
-
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?
MVKQIESK + H2O
L-Met + VKQIESK
show the reaction diagram
N-terminal peptide of thioredoxin-1
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-
?
MVLSPAY + H2O
L-Met + VLSPAY
show the reaction diagram
-
-
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?
MVNPTVFF + H2O
L-Met + VNPTVFF
show the reaction diagram
N-terminal peptide of cyclophilin A
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?
MVNPTVY + H2O
L-Met + VNPTVY
show the reaction diagram
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?
Nle-4-nitroanilide + H2O
Nle + 4-nitroaniline
show the reaction diagram
-
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?
proto-oncogene c-Src + H2O
?
show the reaction diagram
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?
SH3 binding glutamic acid rich-like protein + H2O
?
show the reaction diagram
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MetAP2-specific substrate
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?
thioredoxin-1 + H2O
?
show the reaction diagram
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MetAP2-specific substrate
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?
additional information
?
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NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
Met-peptide + H2O
Met + peptide
show the reaction diagram
additional information
?
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together with N-myristoyltransferase, enzyme plays a major role in the process of myristoylation of oncoproteins including the c-src family
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
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0.0001-0.001 mM, activity is enhanced 5-10fold
Mn2+
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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
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
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-
(3E)-3-(furan-2-ylmethylidene)-5-(hydroxymethyl)-1-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-one
-
no activity at 0.1 mM
(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
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(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
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-
(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
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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
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-
(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
-
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(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
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-
(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
-
-
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
-
-
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
-
-
(S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
-
-
1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
-
-
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
-
;
1-methoxy-5-(methoxymethyl)-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-one
-
no activity at 0.1 mM
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
1-phenyl-2,4-dithiobiuret
-
-
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
-
-
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
-
-
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
-
-
2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 41 nM
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
-
-
2-(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-(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-ethyl-1-phenyl-2-isodithiobiuret
-
-
2-methyl-6-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 6 nM
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
-
-
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
-
-
2-[[(4-chlorophenyl)sulfonyl]amino]-5-methylbenzoic acid
-
-
2-[[(4-fluorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
-
-
2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6-dihydronaphthalene-1-carboxylic acid
-
-
3,5-dimethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
-
3,8-dihydroindeno(1,2-d)(1,2,3)triazole
-
Co(II)-form, Ki,app-value 52 nM
3-(((2-(((1'-methyl-1,4'-bipiperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000055 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((2-(((1-(1-methylethyl)piperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000046 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00095 mM
3-(((2-(((1-methylpiperidin-4-yl)methyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00013 mM
3-(((2-(((2-(diethylamino)ethyl)carbamoyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((2-((1E)-3-((2-hydroxyethyl)(methyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000024 mM
3-(((2-((1E)-3-(4-methylpiperazin-1-yl)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000042 mM
3-(((2-((1E)-3-(diethylamino)but-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00007 mM
3-(((2-((1E)-3-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00026 mM
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000006 mM
3-(((2-((1E)-3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000019 mM; 50% inhibition of enzyme at 0.000027 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((1E)-3-(dimethylamino)prop-1-en-1-yl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000036 mM
3-(((2-((1E)-3-(dimethylamino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000081 mM
3-(((2-((1E)-3-(ethyl(2-hydroxyethyl)amino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000038 mM
3-(((2-((1E)-3-(ethyl(methyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000009 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000023 mM
3-(((2-((1E)-3-(methyl(1-methylethyl)amino)prop-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000027 mM
3-(((2-((1E)-4-(diethylamino)but-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000049 mM; 50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00017 mM
3-(((2-((1E)-5-(diethylamino)pent-1-en-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00012 mM; 50% inhibition of enzyme at 0.000028 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000033 mM
3-(((2-((2-(1-(1-methylethyl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000062 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00035 mM
3-(((2-((2-(1-(1-methylpiperidin-4-yl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000070 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0005 mM
3-(((2-((2-(1-(cyclohexylmethyl)pyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0015 mM
3-(((2-((2-(1-piperidin-4-ylpyrrolidin-2-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0013 mM
3-(((2-((2-(1H-imidazol-1-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0029 mM
3-(((2-((2-(2-oxopyrrolidin-1-yl)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000040 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0014 mM
3-(((2-((2-(bis(1-methylethyl)amino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00064 mM
3-(((2-((2-(diethylamino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00054 mM
3-(((2-((2-(diethylamino)ethyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000031 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00052 mM
3-(((2-((2-(dimethylamino)ethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000048 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0013 mM
3-(((2-((2-(dimethylamino)ethyl)sulfanyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000030 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0007 mM
3-(((2-((2-pyridin-2-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000053 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0020 mM
3-(((2-((2-pyridin-4-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000016 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0085 mM
3-(((2-((2-pyrrolidin-1-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0022 mM
3-(((2-((2-pyrrolidin-2-ylethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000022 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00014 mM
3-(((2-((3-((2-hydroxyethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00028 mM
3-(((2-((3-((2-tert-butoxy-2-oxoethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0043 mM
3-(((2-((3-((tert-butoxycarbonyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000077 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0049 mM
3-(((2-((3-(1,4'-bipiperidin-1'-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000058 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0011 mM
3-(((2-((3-(1-methylpyrrolidin-2-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000096 mM
3-(((2-((3-(4-methylpiperazin-1-yl)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000026 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00041 mM
3-(((2-((3-(bis(1-methylethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000052 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((3-(bis(2-hydroxyethyl)amino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000026 mM, 50% inhibition of proliferation of HT-1080 cells at 0.001 mM
3-(((2-((3-(diethylamino)-1-methylpropyl)carbamoyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000067 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00012 mM
3-(((2-((3-(diethylamino)-1-methylpropyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0026 mM
3-(((2-((3-(diethylamino)propyl)amino)-4-methylphenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0021 mM
3-(((2-((3-(diethylamino)propyl)amino)-5-(trifluoromethyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00069 mM, 50% inhibition of proliferation of HT-1080 cells at 0.100 mM
3-(((2-((3-(diethylamino)propyl)amino)-5-methylphenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000066 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00066 mM
3-(((2-((3-(diethylamino)propyl)amino)-6-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.014 mM; 50% inhibition of enzyme at 0.00018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0083 mM
3-(((2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0014 mM
3-(((2-((3-(diethylamino)propyl)carbamoyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000025 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00055 mM
3-(((2-((3-(dimethylamino)-2,2-dimethylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00061 mM
3-(((2-((3-(dimethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000014 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00019 mM
3-(((2-((3-(ethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00011 mM
3-(((2-((3-aminopropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00016 mM
3-(((2-((3-morpholin-4-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000022 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00032 mM
3-(((2-((3-piperazin-1-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00051 mM
3-(((2-((3-pyrrolidin-1-ylpropyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000085 mM
3-(((2-((4-(diethylamino)-1-methylbutyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00021 mM
3-(((2-((4-(dimethylamino)butyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000012 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00046 mM
3-(((2-((piperidin-3-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000035 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00029 mM
3-(((2-((piperidin-4-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00046 mM
3-(((2-((pyridin-4-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000035 mM, 50% inhibition of proliferation of HT-1080 cells at 0.017 mM
3-(((2-((pyrrolidin-3-ylmethyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000034 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00038 mM
3-(((2-(3,3,4,5,5-pentamethylpiperazin-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000091 mM, 50% inhibition of proliferation of HT-1080 cells at 0.015 mM
3-(((2-(3-(diethylamino)propoxy)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000018 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0062 mM
3-(((2-(3-(diethylamino)propyl)-4-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000017 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000024 mM
3-(((2-(3-(diethylamino)propyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000009 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000073 mM
3-(((2-(3-(dimethylamino)propyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000035 mM
3-(((2-(4-(diethylamino)butyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000019 mM, 50% inhibition of proliferation of HT-1080 cells at 0.000068 mM
3-(((2-(4-benzylpiperazin-1-yl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000020 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0016 mM
3-(((2-(5-(diethylamino)pentyl)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000045 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00035mM
3-(((2-aminophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000013 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0062 mM
3-(((3-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000015 mM, 50% inhibition of proliferation of HT-1080 cells at 0.00037 mM
3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
-
-
3-(((4-chloro-2-((3-(diethylamino)propyl)amino)-5-fluorophenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00079 mM, 50% inhibition of proliferation of HT-1080 cells at 0.013 mM
3-(((4-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.00011 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0031 mM
3-(((5-chloro-2-((3-(diethylamino)propyl)amino)phenyl)sulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000056 mM, 50% inhibition of proliferation of HT-1080 cells at 0.010 mM
3-((4-methylpent-3-enoyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0149 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.00068 mM
3-((5-methylhex-4-enoyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0074 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0010 mM
3-((cyclopent-1-en-1-ylcarbonyl)amino)-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition above 100 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition above 100 mM
3-((phenylsulfonyl)amino)-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
50% inhibition of enzyme at 0.000010 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0024 mM
3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
-
-
3-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 280 nM
3-(1H-1,2,3-triazol-5-yl)phenol
-
Co(II)-form, Ki,app-value 300 nM
3-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 260 nM
3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-{[(2-nitrophenyl)methyl]sulfanyl}-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-methylbenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(3-methoxybenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,4-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2,6-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(2-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(3-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(3-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(4-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(4-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
-
-
3-(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-(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-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-hydroxy-N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0081 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0035 mM
3-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 52 nM
3-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
-
-
3-[(phenylsulfonyl)amino]naphthalene-2-carboxylic acid
-
-
3-[2-(isopropyl)-anilino]-5-(furan-2-ylmethylthio)-1,2,4-triazole
-
-
3-[2-(isopropyl)-anilino]-5-(furan-3-ylmethylthio)-1,2,4-triazole
-
-
3-[2-(isopropyl)-anilino]-5-(thiophen-2-ylmethylthio)-1,2,4-triazole
-
-
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
-
-
4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
-
-
4-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 337 nM
4-(1H-1,2,3-triazol-5-yl)phenol
-
Co(II)-form, Ki,app-value above 1000 nM
4-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value above 1000 nM
4-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 8 nM, Mn(II)-form, 0.014 mM, 50% reduction of viability of human umbilical vein endothelial cell above 0.03 mM
4-[4-(4-methoxyphenyl)piperazin-1-yl]-2-(pyridin-2-yl)quinazoline
-
EC50 value in presence of Co(II) is 0.0001 mM, superior inhibitory potency and selectivity for isoform MetAP1
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-(1-benzofuran-2-yl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 26% inhibition at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM
5-(2-methoxyphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 150 nM
5-(2-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 112 nM
5-(3,4-dibromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, 0.016 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM
5-(3-bromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 4 nM
5-(3-iodophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 16 nM
5-(3-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 18 nM
5-(4-bromophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM
5-(4-chlorophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 6 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.005 mM
5-(4-ethylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 30 nM
5-(4-iodophenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, not inhibitory at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.02 mM
5-(4-methylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 4400 nM, 50% reduction of viability of human umbilical vein endothelial cell at 0.03 mM
5-(4-propylphenyl)-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value above 1000 nM
5-(benzylsulfanyl)-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-(benzylsulfanyl)-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-(benzylsulfanyl)-N-(4-chlorophenyl)-4H-1,2,4-triazol-3-amine
-
-
5-(benzylsulfanyl)-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-(benzylsulfanyl)-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-(benzylsulfanyl)-N-biphenyl-2-yl-4H-1,2,4-triazol-3-amine
-
-
5-(hydroxymethyl)-1-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]bicyclo[3.1.0]hexan-2-ol
-
no activity at 0.1 mM
5-biphenyl-2-yl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value above 1000 nM
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
-
-
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
-
-
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-chloro-2-(5-chloropyridin-2-yl)-6-methyl-N-((R)-2-phenyl-2-(4-phenylbutylamino)ethyl)pyrimidin-4-amine
-
compound shows 500fold specificity for isoform AP1 over isoform AP2
5-chloro-2-(5-chloropyridin-2-yl)-N-(2,4-diphenylbutyl)-6-methylpyrimidin-4-amine
-
compound shows 3175fold specificity for isoform AP1 over isoform AP2
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
-
;
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
;
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
-
;
5-demethylovalicin
-
IC50: 17.7 nM, inhibition of recombinant enzyme
5-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
-
-
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-4-oxobicyclo[3.1.0]hexane-1-carbaldehyde
-
-
5-methyl-2-((phenylsulfonyl)amino)benzoic acid
50% inhibition of enzyme at 0.0014 mM, 50% inhibition of proliferation of HT-1080 cells at 0.0072 mM
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine
-
Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.015 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
-
-
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
-
-
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-phenyl-1H-1,2,3-triazole
-
Co(II)-form, Ki,app-value 70 nM
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
-
-
5-[(2E)-hepta-2,6-dien-4-yn-1-ylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[(cyclohexylmethyl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[(cyclohexylmethyl)sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[(cyclohexylmethyl)sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[(2-methyl-2,5-dihydro-1,3-thiazol-4-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
-
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
-
6-(1,5-dimethylhex-4-en-1-yl)-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
-
-
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
-
-
7-amino-4-methylcoumarin
-
; product inhibition
8-(pyridin-2-yl)-7H-purine
-
-
8-hydroxy quinoline
-
-
A-310840
-
IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+
A-311263
-
IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+
A-357300
A-800141
bengamide A
bengamide B
-
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
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
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
fumagalone
-
-
fumagillin
fumagillol
-
i.e. (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-ol
fumarranol
-
selective inhibitor
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
L-Met
-
product inhibition
L-Met-(RS)-sulfoxide
-
-
L-Nle
-
product inhibition
LAF 389
-
nonselective inhibitor for both MetAP1 and MetAP2; nonselective inhibitor for both MetAP1 and MetAP2
methyl 4-([5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
-
methyl 4-([5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
-
methyl 4-([5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
-
methyl 4-([5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
-
methyl 4-[(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[(5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[(5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[(5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[(5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
-
methyl 4-[[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]amino]benzoate
-
-
Mg2+
-
1.0 mM MgCl2, 21% inhibition
Mn2+
-
0.1 mM MnCl2, 26% inhibition. 5.0 mM, 36% inhibition
N-((R)-2-(5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-ylamino)-1-phenylethyl)-3-phenylpropanamide
-
compound shows 323fold specificity for isoform AP1 over isoform AP2
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
-
-
N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4,5-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-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methylphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methylphenyl)-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(4-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
-
N-(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
-
N-(quinolin-8-yl)benzenesulfonamide
-
-
N-1,3-thiazol-2-ylpyridine-2-carboxamide
-
wild-type, 50% inhibition at 0.0104 mM, mutant lacking N-terminal 66 amino acids, 50% inhibition at 0.0049 mM
N-benzyl-3-(1H-1,2,3-triazol-5-yl)aniline
-
Co(II)-form, Ki,app-value 29 nM
N-biphenyl-2-yl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(2-methoxybenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-biphenyl-2-yl-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-[4-(chloromethyl)phenyl]-5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
-
N-[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
N-[5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
-
ovalicin
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
-
-
PPI-2458
quinolin-8-yl benzenesulfonate
-
-
quinolin-8-yl benzoate
-
-
tert-butyl [2-(4,5-dihydro-1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate
-
-
thiabendazole
-
-
TNP-470
Zn2+
-
0.1 mM, complete inhibition
[(1R)-1-carbamoyl-2-methyl-propyl]-carbamic acid-(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-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-methylbut-2-enyl)oxiranyl]-1-oxaspiro(2,5)oct-6-yl ester
-
PPI-2458, potent inhibitor
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.74 - 1.8
L-Met-L-Pro-4-nitroanilide
1.28 - 8.81
L-Met-PSI[C(O)S]Gly-L-Phe
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
0.38 - 2.08
Met-Ala-Ser
0.34
Met-Gly-Met-Met
-
pH 7.5, 30C
2.8
Met-Pro
-
pH 7.5, 30C
0.576
Met-Pro-p-nitroanilide
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
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
additional information
additional information
-
Km-values of truncated enzsme
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.11 - 0.425
L-Met-L-Pro-4-nitroanilide
0.97 - 16.61
L-Met-PSI[C(O)S]Gly-L-Phe
0.158
Met-4-nitroanilide
-
pH 7.5, 30C
0.0633
Met-7-amido-4-methylcoumarin
-
pH 7.5, 30C, in presence of 0.01 mM CoCl2
0.0517 - 3.5
Met-Ala-Ser
0.0683
Met-Gly-Ala-Gln-Phe-Ser-Lys-Thr
-
pH 7.4, MetAP2
2.83
Met-Gly-Met-Met
-
pH 7.5, 30C
0.13
Met-Pro
-
pH 7.5, 30C
0.0065
Met-Pro-p-nitroanilide
in 40 mM HEPES, pH 8.0, and 100 mM NaCl, at 23C
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
additional information
L-Met-PSI[C(O)S]Gly-L-Phe
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1.7
MAEIEIY
-
pH 7.4, temperature not specified in the publication
5.3
MAEWEIY
-
pH 7.4, temperature not specified in the publication
10
MAGAIHY
-
pH 7.4, temperature not specified in the publication
41
MAHAIHY
-
pH 7.4, temperature not specified in the publication
3.58
MAHIEIY
-
pH 7.4, temperature not specified in the publication
1.3
MAPIEIY
-
pH 7.4, temperature not specified in the publication
6.6
MARIEIY
-
pH 7.4, temperature not specified in the publication
9.6
MAWIEIY
-
pH 7.4, temperature not specified in the publication
0.18
MGEIEIY
-
pH 7.4, temperature not specified in the publication
0.16
MPEIEIY
-
pH 7.4, temperature not specified in the publication
0.029
MTEIEIY
-
pH 7.4, temperature not specified in the publication
0.13
MVAAAAY
-
pH 7.4, temperature not specified in the publication
0.028
MVGVKPY
-
pH 7.4, temperature not specified in the publication
0.064
MVHQVLY
-
pH 7.4, temperature not specified in the publication
0.007
MVKIEIY
-
pH 7.4, temperature not specified in the publication
0.015
MVLSPAY
-
pH 7.4, temperature not specified in the publication
0.013
MVNPTVY
-
pH 7.4, temperature not specified in the publication
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
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 - 0.0000078
5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
0.00000023
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000013
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000065
5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.000061
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.01
5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
Ki above 0.01 mM, apparent value
0.0000024
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.000004
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(3,4-dimethoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000021
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methoxyphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000033
5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-N-(4-methylphenyl)-4H-1,2,4-triazol-3-amine
-
apparent value
0.29
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
0.0000005
methyl 4-([5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000027
methyl 4-([5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000009
methyl 4-([5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000009
methyl 4-([5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]amino)benzoate
-
apparent value
0.0000038
methyl 4-[(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000008
methyl 4-[(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.00000041
methyl 4-[(5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.00001
methyl 4-[(5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.000135
methyl 4-[(5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000013
methyl 4-[(5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-yl)amino]benzoate
-
apparent value
0.0000007
methyl 4-[[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]amino]benzoate
-
apparent value
0.0000037
N-(2-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000038
N-(2-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000025
N-(2-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000009
N-(3,4-dimethoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000024
N-(3,4-dimethoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000096
N-(3,4-dimethoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000021
N-(3,4-dimethoxyphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000007
N-(3,4-dimethoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000013
N-(3,4-dimethoxyphenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.001
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.001 mM, apparent value
0.000018
N-(3,4-dimethoxyphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000052
N-(4-chlorophenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000052
N-(4-chlorophenyl)-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000004
N-(4-chlorophenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000025
N-(4-chlorophenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000048
N-(4-chlorophenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000018
N-(4-chlorophenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfany]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000061
N-(4-chlorophenyl)-5-[[2-(2-fluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.01
N-(4-chlorophenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000023
N-(4-chlorophenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000016
N-(4-methoxyphenyl)-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000018
N-(4-methoxyphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000061
N-(4-methoxyphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000016
N-(4-methoxyphenyl)-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.000034
N-(4-methoxyphenyl)-5-[[2-(2-methoxyphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000078
N-(4-methylphenyl)-5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000057
N-(4-methylphenyl)-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000052
N-(4-methylphenyl)-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000078
N-(4-methylphenyl)-5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000065
N-(4-methylphenyl)-5-[[2-(2-methylphenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000091
N-(5-[[(2-methyl-1,3-thiazolidin-4-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
apparent value
0.0000015
N-(5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-yl)pyridin-3-amine
-
apparent value
0.00035
N-biphenyl-2-yl-5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.002
N-biphenyl-2-yl-5-[(2-methoxybenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.002
N-biphenyl-2-yl-5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.00048
N-biphenyl-2-yl-5-[(3-methylbut-2-en-1-yl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00065
N-biphenyl-2-yl-5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.002
N-biphenyl-2-yl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
Ki above 0.002 mM, apparent value
0.0017
N-biphenyl-2-yl-5-[[(5-methylisoxazol-3-yl)methyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000075
N-phenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.0000015
N-[4-(chloromethyl)phenyl]-5-[[2-(3,4-difluorophenyl)ethyl]sulfanyl]-4H-1,2,4-triazol-3-amine
-
apparent value
0.00000004
N-[5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000003
N-[5-[(2-fluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000017
N-[5-[(2-methylbenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000005
N-[5-[(3,4-difluorobenzyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.000003
N-[5-[(cyclohexylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.0000057
N-[5-[(pyridin-2-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridin-3-amine
-
apparent value
0.000000245
[(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 hide
LITERATURE
IMAGE
0.0000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (2R)-3-methyl-1-(2-(1-methylpyrrolidin-2-yl)ethylamino)-1-oxobutan-2-ylcarbamate
Homo sapiens;
-
above, in HUVEC
0.000000095
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-1-amino-3-methyl-1-oxobutan-2-ylcarbamate
Homo sapiens;
-
in HUVEC
0.0000017
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-(morpholinoamino)-1-oxobutan-2-ylcarbamate
Homo sapiens;
-
in HUVEC
0.0000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl (R)-3-methyl-1-oxo-1-(2-(pyrrolidin-1-yl)ethylamino)butan-2-ylcarbamate
Homo sapiens;
-
in HUVEC
0.0000017
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-amino-2-methyl-1-oxopropan-2-ylcarbamate
Homo sapiens;
-
in HUVEC
0.0000007
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 1-carbamoylcyclopentylcarbamate
Homo sapiens;
-
in HUVEC
0.0000002
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(1-methylpyrrolidin-2-yl)ethylcarbamate
Homo sapiens;
-
above, in HUVEC
0.0000001
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 2-(pyrrolidin-1-yl)ethylcarbamate
Homo sapiens;
-
in HUVEC
0.00000006
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl isopropylcarbamate
Homo sapiens;
-
in HUVEC
0.0000007
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl morpholinocarbamate
Homo sapiens;
-
in HUVEC
0.0000011
(3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl tert-butylcarbamate
Homo sapiens;
-
in HUVEC
0.00000025
(3R,5S,6R)-5-methoxy-4-[(3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-1-oxaspiro[2.5]oct-6-yl (chloroacetyl)carbamate
Homo sapiens;
-
in HUVEC
0.000027
(8S)-2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Homo sapiens;
-
-
0.000000036
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-2-phenylacetate
Homo sapiens;
-
in HUVEC
0.00000004
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-3-methylbutanoate
Homo sapiens;
-
in HUVEC
0.000000038
(R)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-4-methylpentanoate
Homo sapiens;
-
in HUVEC
0.000000018
(S)-methyl 2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanoate
Homo sapiens;
-
in HUVEC
0.0000013
1-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonyl)-piperidine-4-carboxylic acid
Homo sapiens;
-
in HUVEC
0.0011 - 0.0081
1-(5-chloro-6-methyl-2-pyridin-2-ylpyrimidin-4-yl)-4-(2,4-dichlorobenzyl)-1,4-diazepane
0.0243 - 0.0324
1-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0398
2-(1,3-thiazol-2-yl)-1H-imidazo[4,5-b]pyridine
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0101
2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-amine
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.019
2-(1,3-thiazol-4-yl)-1H-imidazo[4,5-c]pyridine
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0001
2-(2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)ethyl)-1,1-dimethylpyrrolidinium iodide
Homo sapiens;
-
in HUVEC
0.0329
2-(pyrazin-2-yl)-1H-benzimidazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0093
2-(pyridin-2-yl)-1H-benzimidazol-5-amine
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0133 - 0.0284
2-(pyridin-2-yl)-1H-benzimidazole
0.0329 - 0.0373
2-(pyridin-2-yl)-1H-benzimidazole-5-carbonitrile
0.0401 - 0.0484
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyrazine
0.0267 - 0.0276
2-(pyridin-2-yl)-1H-imidazo[4,5-b]pyridine
0.008 - 0.0103
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine
0.0039
2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-5-bromobenzoic acid
Homo sapiens;
-
-
0.0011
2-[(phenylsulfonyl)amino]-5-propylbenzoic acid
Homo sapiens;
-
-
0.011
2-[[(4-chlorophenyl)sulfonyl]amino]-5-methylbenzoic acid
Homo sapiens;
-
-
0.00001
2-[[(4-fluorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
Homo sapiens;
-
-
0.00002
2-[[(4-fluorophenyl)sulfonyl]amino]-8-methyl-5,6-dihydronaphthalene-1-carboxylic acid
Homo sapiens;
-
-
0.00035
3,5-dimethyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens;
-
-
0.0001
3-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)-N,N,N-trimethylpropan-1-aminium iodide
Homo sapiens;
-
in HUVEC
0.000015
3-((R)-2-(((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)-carbonylamino)-3-methylbutanamido)benzoic acid
Homo sapiens;
-
in HUVEC
0.01178
3-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-{[(2-nitrophenyl)methyl]sulfanyl}-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00093
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.01766
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(2-methylbenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.03071
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(3-methoxybenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00224
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-fluorobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.01239
3-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-5-(4-nitrobenzylthio)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00395
3-(2,4-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0048
3-(2,6-difluorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00537
3-(2-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00184
3-(2-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00591
3-(3-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00192
3-(3-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00729
3-(4-bromobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00345
3-(4-chlorobenzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.00601
3-(benzylthio)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-4-phenyl-4H-1,2,4-triazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.000009
3-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-2-carboxylic acid
Homo sapiens;
-
-
0.000019
3-[(phenylsulfonyl)amino]naphthalene-2-carboxylic acid
Homo sapiens;
-
-
0.000015
3-[[(4-fluorophenyl)sulfonyl]amino]naphthalene-2-carboxylic acid
Homo sapiens;
-
-
0.0000007
4-((((3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yloxy)carbonylamino)methyl)benzoic acid
Homo sapiens;
-
in HUVEC
0.0388
5,6-dimethyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0284 - 0.0326
5,6-dimethyl-2-(pyridin-2-yl)-1H-benzimidazole
0.0091
5-bromo-2-[[(4-chlorophenyl)sulfonyl]amino]benzoic acid
Homo sapiens;
-
-
0.01
5-butyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens;
-
-
0.028 - 0.047
5-chloro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0002
5-chloro-2-(5-chloropyridin-2-yl)-6-methyl-N-((R)-2-phenyl-2-(4-phenylbutylamino)ethyl)pyrimidin-4-amine
Homo sapiens;
-
22C, pH not specified in the publication
0.000063
5-chloro-2-(5-chloropyridin-2-yl)-N-(2,4-diphenylbutyl)-6-methylpyrimidin-4-amine
Homo sapiens;
-
22C, pH not specified in the publication
0.0181 - 0.0488
5-chloro-2-(pyridin-2-yl)-1H-benzimidazole
0.0004 - 0.0008
5-chloro-4-methyl-2-pyridin-2-yl-6-pyrrolidin-1-ylpyrimidine
0.0006 - 0.0076
5-chloro-6-methyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
0.0033
5-chloro-N,6-dimethyl-N-(2-phenylethyl)-2-pyridin-2-ylpyrimidin-4-amine
Homo sapiens;
-
MetAP1; MetAP2
0.0000177
5-demethylovalicin
Homo sapiens;
-
IC50: 17.7 nM, inhibition of recombinant enzyme
0.00009
5-ethyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens;
-
-
0.0384 - 0.0458
5-fluoro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0149 - 0.0347
5-fluoro-2-(pyridin-2-yl)-1H-benzimidazole
0.0132
5-methoxy-6-[2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]-4-oxobicyclo[3.1.0]hexane-1-carbaldehyde
Homo sapiens;
-
-
0.0355 - 0.0406
5-methyl-2-(1,3-thiazol-4-yl)-1H-benzimidazole
0.0077 - 0.0326
5-methyl-2-(pyridin-2-yl)-1H-benzimidazole
0.001
5-methyl-2-[(phenylsulfonyl)amino]benzoic acid
Homo sapiens;
-
-
0.0485
5-nitro-2-(1,3-thiazol-4-yl)-1H-benzimidazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0288
5-nitro-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0441
5-tert-butyl-2-(pyridin-2-yl)-1H-benzimidazole
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0575
6-(1,5-dimethylhex-4-en-1-yl)-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens;
-
-
0.0338
6-[(1E)-1,5-dimethylhexa-1,4-dien-1-yl]-5-(hydroxymethyl)-1-methoxybicyclo[3.1.0]hexan-2-one
Homo sapiens;
-
-
0.0339 - 0.0364
8-(pyridin-2-yl)-7H-purine
0.0056 - 0.0215
8-hydroxy quinoline
0.000031
A-310840
Homo sapiens;
-
IC50: 0.000031 mM for enzyme with Zn2+, 0.000043 mM for enzyme with Ni2+, 0.000069 mM for enzyme with Co2+, 0.000026 for enzyme with Fe2+, 0.0578 mM for enzyme with Mn2+
0.000121
A-311263
Homo sapiens;
-
IC50: 0.000121 mM for enzyme with Zn2+, 0.000107 mM for enzyme with Ni2+, 0.000149 mM for enzyme with Co2+, 0.00011 mM for enzyme with Fe2+, 0.000055 mM for enzyme with Mn2+
0.00015
A-357300
Homo sapiens;
-
-
0.00002
A-800141
Homo sapiens;
-
-
0.0019 - 0.0105
bengamide A
0.0179 - 0.0293
bengamide B
0.0268 - 0.05
bengamide G
0.0371 - 0.05
bengamide L
0.0054 - 0.05
bengamide M
0.0402 - 0.05
bengamide N
0.0027 - 0.05
bengamide O
0.008
fumagalone
Homo sapiens;
-
-
0.00323
fumarranol
Homo sapiens;
-
-
0.000093
N-((R)-2-(5-chloro-2-(5-chloropyridin-2-yl)-6-methylpyrimidin-4-ylamino)-1-phenylethyl)-3-phenylpropanamide
Homo sapiens;
-
22C, pH not specified in the publication
0.0081 - 0.0258
N-(1,3-thiazol-2-yl)pyridine-2-carboxamide
0.0029
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(2,2-dimethylpropanoyl)amino]pyridine-2-carboxamide
Homo sapiens;
-
MetAP1
0.0035
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[(3-phenylpropanoyl)amino]pyridine-2-carboxamide
Homo sapiens;
-
MetAP1
0.0064
N-(4,5-dihydro-1,3-thiazol-2-yl)-3-[[(1E)-2-methylpropylidene]amino]pyridine-2-carboxamide
Homo sapiens;
-
MetAP1
0.0398 - 0.0449
N-(quinolin-8-yl)benzenesulfonamide
0.041
phenyl[2-(1,3-thiazol-4-yl)-1H-benzimidazol-5-yl]methanone
Homo sapiens;
-
pH not specified in the publication, temperature not specified in the publication
0.0412 - 0.0417
quinolin-8-yl benzenesulfonate
0.0348 - 0.0428
quinolin-8-yl benzoate
0.0015
tert-butyl [2-(4,5-dihydro-1,3-thiazol-2-ylcarbamoyl)pyridin-3-yl]carbamate
Homo sapiens;
-
MetAP1
0.0447 - 0.0478
thiabendazole
0.000001 - 0.00105
TNP-470
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
1.3
-
substrate L-Nle-L-Ala-L-Ser, N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
1.4
substrate MVKQIESK , oxidized enzyme, pH 7.2, 25C
2.8
substrate MVNPTVFF, oxidized enzyme, pH 7.2, 25C
3.1
substrate MVNPTVFF, reduced enzyme, pH 7.2, 25C
3.4
substrate MGNLKSVA, oxidized enzyme, pH 7.2, 25C
4.7
substrate MVKQIESK , reduced enzyme, pH 7.2, 25C
7.3
-
substrate L-Thr-PSI[C(O)S]Gly-L-Phe, wild-type, pH 7.0, 22C
7.8
substrate MGNLKSVA, reduced enzyme, pH 7.2, 25C
8.8
-
substrate L-Thr-PSI[C(O)S]Gly-L-Phe, N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
9.4
-
substrate L-Ala-PSI[C(O)S]Gly-L-Phe, N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
12.1
-
substrate L-Thr-PSI[C(O)S]Gly-L-Phe, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
15
substrate MGKVKVGV, oxidized enzyme, pH 7.2, 25C
18
substrate MGKVKVGV, reduced enzyme, pH 7.2, 25C
18.4
-
substrate L-Met-PSI[C(O)S]Gly-L-Phe, N-terminally truncated mutant lacking 135 amino acids, pH 7.0, 22C
22
-
substrate L-Phe-L-Ala-L-Ser-L-Trp, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
23
-
substrate L-Leu-L-Ala-L-Ser-L-Trp, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
30
-
substrate L-Leu-L-Ala-L-Ser-L-Trp, wild-type, pH 7.0, 22C; substrate L-Phe-L-Ala-L-Ser-L-Trp, wild-type, pH 7.0, 22C
42.7
-
substrate L-Met-PSI[C(O)S]Gly-L-Phe, wild-type, pH 7.0, 22C
100
-
substrate L-Met-L-Ala-L-Ser, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
141
-
substrate L-Nle-L-Ala-L-Ser, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
142
-
substrate L-Met-L-Ala-L-Ser, wild-type, pH 7.0, 22C
146
-
substrate L-Met-PSI[C(O)S]Gly-L-Phe, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
183
-
substrate L-Nle-L-Ala-L-Ser, wild-type, pH 7.0, 22C
201
-
substrate L-Met-L-Ala-L-Ser-L-Trp, N-terminally truncated mutant, lacking 66 amino acids, pH 7.0, 22C
396
-
substrate L-Met-L-Ala-L-Ser-L-Trp, wild-type, pH 7.0, 22C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
cell line derived from a patient with high-risk neuroblastoma
Manually annotated by BRENDA team
-
neonatal dermal microvascular
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
non-Hodgkin's lymphoma cell lines
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
UNIPROT
ORGANISM
Homo sapiens;
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
44199
-
x * 44199, MALDI-TOF, x * 44207, calculated
44207
-
x * 44199, MALDI-TOF, x * 44207, calculated
50000
-
SDS-PAGE
52790
-
MALDI-MS
52830
-
calculation from nucleotide sequence
54700
-
analytical ultracentrifugation
additional information
-
two-cobalt-dependent MetAP families, presently composed of the prokaryote and yeast sequence (and represented by the Escherichia coli structure) (type I), and by human MetAP, the yeast open reading frame, and the partial prokaryotic sequence (type II)
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
isoform MetAP2 is post-translationally regulated by an allosteric disulfide bond, which controls substrate specificity and catalytic efficiency. Isoform MetAP2 contains a single Cys228-Cys448 disulfide bond that has an -RH-staple configuration and links two beta-loop structures, which are hallmarks of allosteric disulfide bonds. The disulfide bond exists in oxidized and reduced states in the recombinant enzyme. The disulfide has a standard redox potential of -261 mV and is efficiently reduced by the protein reductant, thioredoxin, with a rate constant of 16180 per M and s. The MetAP2 disulfide bond also exists in oxidized and reduced states in glioblastoma tumor cells, and stressing the cells by oxygen or glucose deprivation results in more oxidized enzyme. Oxidized and reduced isoforms have different catalytic efficiencies for hydrolysis of MetAP2 peptide substrates
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
1.8 resolution crystal structure of free enzyme and enzyme complexed with fumagillin. Crystals are grown in 1 to 2 weeks at 4C from sitting drops, with a protein concentration of 12 mg/ml
-
complexed with inhibitor, sitting drop vapour diffusion method with 15-20% tert-butyl alcohol containing 0.4-0.1 M aqueous sodium citrate at pH 5.5
-
crystal structure of N-terminally truncated MetAP1 in complex with inhibitor 4-[4-(4-methoxyphenyl)piperazin-1-yl]-2-(pyridin-2-yl)quinazoline and Co(II); N-terminally truncated isoform AP1 in complex with inhibitor 5-chloro-2-(5-chloropyridin-2-yl)-6-methyl-N-((R)-2-phenyl-2-(4-phenylbutylamino)ethyl)pyrimidin-4-amine. Both pyridine nitrogen N1 and pyrimidine nitrogen N1 are bound to Co3, displaying a near-perfect octahedral coordination which is completed by the nitrogen atom from the side chain of His212 and three water molecules
-
MetAP1 in complex with ovalicin, hanging drop vapour diffusion method, with 4%-6% PEG 10000 or 12%-16% PEG monomethyl ether 2000, in 100 mM HEPES at pH 5.4-6.2
sitting drop vapour diffusion method, in complex with L-methionine and D-methionine at 1.9 and 2.0 A resolution, respectively
-
truncated MetAP1 lacking N-terminal 89 amino acids
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
recombinant full-lenth enzyme is not stable during purification and storage at 4C, and a smaller but active protein appears that corresponds to N-terminally truncated protein lacking amino acids 1-66
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
4C, MetAP2 is stable for several months
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
commercial preparation
-
glutathione agarose chromatography
-
Mono Q column chromatography and Q-Sepharose column chromatography
-
Ni-NTA Superflow resin chromatography
recombinant enzyme
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
; expressed in Sf21 insect cells
-
adenoviral transfer of c-Myc increaseds the expression of MetAP2 in human umbilical vein endothelial cells and reveals that cellular proliferation may involve a cross-talk between c-Myc and MetAP2
-
commercial preparation
-
expressed in Escherichia coli BL21(DE3) cells
expressed in Escherichia coli; expressed in Escherichia coli
-
expressed in Escherichia coli; expressed in Sf9 cells
-
expressed in HeLa cells
-
expressed in NIH-3T3 cells and NL20 cell line
-
expressed in Saccharomyces cerevisiae strain S228C (ATCC 201388)
-
expressed with a baculovirus expression system
-
full-length and truncated forms of hMetAP2
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
expressed preferentially in cord blood CD34+ cells
-
the 3,5-bis(benzylidene)-4-piperidone derivative 2-(3-[3,5-bis[4-nitrobenzylidene]-4-oxopiperidin-1-yl]-3-oxopropylsulfanyl) ethanesulfonic acid, or NC2213, downregulates the enzyme in HT-29 cells
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A362T
-
type II enzyme, mutation results in resistance to ovalicin, TNP-470 and fumagillin when expressed in yeast
C202A
-
hydrolysis of Met-PSI[C(O)S]Gly-Phe similar to wild-type, relaxed specificity
F197A
-
no hydrolysis of Met-PSI[C(O)S]Gly-Phe
F308A
-
increase of kcat- and of KM-value for Met-PSI[C(O)S]Gly-Phe
H211A
-
reduction of kcat- and of KM-value for Met-PSI[C(O)S]Gly-Phe
H231N
-
enzymatically inactive
P191A
-
hydrolysis of Met-Ala-Ser similar to wild-type
T334A
-
type I enzyme, mutation renders the resistant wild-type enzyme sensitive to ovalicin
W352A
-
increase of kcat- and of KM-value for Met-PSI[C(O)S]Gly-Phe
Y194A
-
no hydrolysis of Met-PSI[C(O)S]Gly-Phe
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine