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3.4.22.70: sortase A

This is an abbreviated version!
For detailed information about sortase A, go to the full flat file.

Word Map on EC 3.4.22.70

Reaction

The enzyme catalyses a cell wall sorting reaction in which a surface protein with a sorting signal containing a LPXTG motif is cleaved between the Thr and Gly residue. The resulting threonine carboxyl end of the protein is covalently attached to a pentaglycine cross-bridge of peptidoglycan. =

Synonyms

C60.001, sortase A, sortase A transpeptidase, sortase SrtA, sortase transpeptidase, SrtA, SrtA protein, SrtA sortase

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.70 sortase A

Inhibitors

Inhibitors on EC 3.4.22.70 - sortase A

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1E)-N'-[(1E)-(4-[(E)-[(diaminomethylene)hydrazono]methyl]phenyl)methylene]ethanehydrazonamide
-
-
(2-(trimethylammonium)ethyl)methanethiosulfonate
-
inhibition at 5 mM, inhibition is relieved by supplementing the reaction with 10 mM dithiothreitol
(2-methyl-1H-indol-3-yl)(oxo)acetic acid
-
-
(2-sulfonatoethyl)methanethiosulfonate
-
-
(2E)-2,3-bis(4-methoxyphenyl)acrylamide
-
IC50: 0.476 mM
(2E)-2,3-bis(4-methoxyphenyl)acrylonitrile
-
IC50: 0.187 mM
(2E)-2-(2-furoyl)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]acrylonitrile
-
-
(2E)-3-(2-furyl)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]acrylamide
-
-
(2E)-3-[(methyl[4-[(5-nitropyridin-2-yl)oxy]phenyl]oxido-l4-sulfanylidene)amino]-2-(2-thienylcarbonyl)acrylonitrile
-
-
(2E)-4-([4-[(2-hydroxybenzoyl)amino]phenyl]amino)-4-oxobut-2-enoic acid
-
-
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-furyl)acrylamide
-
-
(2E)-N-(3-formyl-4-morpholin-4-ylphenyl)-3-(2-thienyl)acrylamide
-
-
(2E)-N-[3-(hydroxymethyl)-4-morpholin-4-ylphenyl]-3-(2-thienyl)acrylamide
-
-
(2Z)-2,3-bis(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0279mM
(2Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.009244 mM
(2Z)-3-(2-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0362 mM
(2Z)-3-(3,4-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.02296 mM
(2Z)-3-(3,5-dimethoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.025463 mM
(2Z)-3-(3-methoxyphenyl)-2-(4-methoxyphenyl)acrylonitrile
-
IC50: 0.0174 mM
(4E)-5-methyl-4-[[(4-nitrophenyl)amino]methylidene]-2-phenyl-2,4-dihydro-3H-pyrazole-3-thione
-
-
(5R)-3,5-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 68.98 mg/L
(5Z)-3-(2,4-dimethylphenyl)-5-(3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-(3-chlorophenyl)-5-(4-methyl-3-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-benzyl-5-benzylidene-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-3-ethyl-5-(2-nitrobenzylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-chlorophenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(3-methylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-(4-nitrophenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-2-hydroxy-5-nitrobenzylidene)-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-bromo-4-hydroxy-5-nitrobenzylidene)-3-(2,4-dimethylphenyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-(3-chlorobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-methyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-benzylidene-3-propyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(6-hydroxy-1H-indol-3-yl)(oxo)acetic acid
-
-
(6-methoxy-1H-indol-3-yl)(oxo)acetic acid
-
-
(6-methyl-1H-inden-3-yl)[4-(6-methyl-1H-indol-3-yl)-1H-imidazol-2-yl]methanone
-
IC50: 15.67 mg/Ll
(6R)-3,6-bis(6-bromo-1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 86.34 mg/L
(6R)-6-(6-bromo-1H-indol-3-yl)-3-(1H-indol-3-yl)-5,6-dihydropyrazin-2(1H)-one
-
IC50: 34.04 mg/L
(Z)-3-(2,5-dimethoxyphenyl)-2-(4-methoxyphenyl) acrylonitrile
-
potential of this inhibitor for the treatment of Staphylococcus aureus infections
1,2-bis(5-hydroxy-1H-indol-3-yl)ethane-1,2-dione
-
-
1-(3,4-dichlorophenyl)-3-(dimethylamino)propan-1-one
-
-
1-(3-methoxyphenyl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-(4-bromophenyl)-3-(3-methylpiperidin-1-yl)propan-1-one
-
-
1-(4-chlorophenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(4-fluorophenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(4-methoxyphenyl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-(4-methylphenyl)-3-morpholin-4-ylpropan-1-one
-
-
1-(naphthalen-2-yl)-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-pentyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-phenyl-2,3,4,9-tetrahydro-1H-beta-carbolin-7-ol
-
-
1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
1-phenyl-4,9-dihydro-3H-beta-carboline
-
-
1-[4-(2-aminopyrimidin-4-yl)phenyl]-3-(4-chlorophenyl)urea
-
-
1H-indol-3-yl(oxo)acetic acid
-
-
2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
2-(1-oxoisoindolin-2-yl)acetic acid
-
-
2-(1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(2-methyl-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(3,5-dichlorophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3,5-dichlorophenyl)-5-ethoxy-4-sulfanylpyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4,5-dichloropyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-4-chloro-5-ethoxypyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-5-chloro-4-ethoxypyridazin-3(2H)-one
-
-
2-(3-bromophenyl)-5-chloro-4-methoxypyridazin-3(2H)-one
-
-
2-(3-chlorophenyl)-4-methoxy-5-sulfanylpyridazin-3(2H)-one
-
-
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
-
-
2-(4-nitrophenyl)-4,5-dichloropyridazin-3-one
-
-
2-(6-hydroxy-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-(6-methoxy-1H-indol-3-yl)-2-oxo-N-phenylacetamide
-
-
2-cyclohexyl-4-(ethylsulfanyl)-5-sulfanylpyridazin-3(2H)-one
-
-
2-ethyl-4-hydroxy-5-(methylsulfanyl)pyridazin-3(2H)-one
-
-
2-hydroxy-1-(5-hydroxy-1H-indol-3-yl)ethanone
-
-
2-hydroxy-N-[4-[([[(4-methylphenyl)sulfonyl]amino]carbonyl)amino]phenyl]benzamide
-
-
2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzamide
-
-
2-phenyl-4,5-dichloro-pyridazin-3-one
-
-
3,3,3-trifluoro-1-(phenylsulfonyl)-1-propene
-
IC50: 0.19 mM, irreversible
3,5-bis[[2-(4-nitrophenyl)-2-oxoethyl]thio]isothiazole-4-carbonitrile
-
-
3-(2-aminoethyl)-1H-indol-5-ol
-
-
3-(3-oxo-1,2-benzothiazol-2(3H)-yl)propanoic acid
-
-
3-(dimethylamino)-1-(2-thienyl)propan-1-one
-
-
3-(dimethylamino)-1-(3-nitrophenyl)propan-1-one
-
-
3-anilino-1-(3-nitrophenyl)propan-1-one
-
-
4,5-dichloro-2-(3,5-dichlorophenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
4,5-dichloro-2-cyclohexylpyridazin-3(2H)-one
-
-
4-(benzyloxy)-5-hydroxy-2-phenylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(3-fluorophenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(3-methylphenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-(4-nitrophenyl)-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-2-phenyl-5-sulfanylpyridazin-3(2H)-one
-
-
4-(ethylsulfanyl)-5-hydroxy-2-phenylpyridazin-3(2H)-one
-
-
4-chloro-2-(3,5-dichlorophenyl)-5-ethoxypyridazin-3(2H)-one
-
-
4-chloro-2-cyclohexyl-5-ethoxypyridazin-3(2H)-one
-
-
4-chloro-5-(methylsulfanyl)-2-phenylpyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-(4-nitrophenyl)pyridazin-3(2H)-one
-
-
4-chloro-5-ethoxy-2-phenylpyridazin-3-one
-
-
4-ethoxy-2-phenyl-5-sulfanylpyridazin-3(2H)-one
-
-
4-ethoxy-5-(2-pyridyldithio)-2-phenylpyridazin-3-one
-
-
4-ethoxy-5-(methyldithio)-2-phenylpyridazin-3-one
-
-
4-ethoxy-5-mercapto-2-phenylpyridazin-3-one
-
-
4-hydroxy-5-(methylsulfanyl)-2-phenylpyridazin-3(2H)-one
-
-
4-hydroxymercuribenzoate
-
-
5-chloro-2-(3,5-dichlorophenyl)-4-ethoxypyridazin-3(2H)-one
-
-
5-chloro-2-(3,5-dichlorophenyl)-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-2-(3-fluorophenyl)-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-2-cyclohexyl-4-ethoxypyridazin-3(2H)-one
-
-
5-chloro-2-cyclohexyl-4-methoxypyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(3-fluorophenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-(4-nitrophenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-ethoxy-2-phenylpyridazin-3-one
-
-
5-chloro-4-methoxy-2-(3-methylphenyl)pyridazin-3(2H)-one
-
-
5-chloro-4-methoxy-2-phenylpyridazin-3(2H)-one
-
-
5-ethoxy-2-(3-fluorophenyl)-4-sulfanylpyridazin-3(2H)-one
-
-
5-ethoxy-2-(3-methylphenyl)-4-sulfanylpyridazin-3(2H)-one
-
-
5-ethoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
-
-
5-hydroxy-1H-indole-3-carbaldehyde
-
-
5-hydroxy-4-methoxy-2-phenylpyridazin-3(2H)-one
-
-
5-methoxy-2-phenyl-4-sulfanylpyridazin-3(2H)-one
-
-
5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoic acid
-
-
6-hydroxy-2,3,4,9-tetrahydro-1H-beta-carbolin-1-one
-
-
6-hydroxydihydro-beta-carboline
-
-
7-hydroxy-2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
7-methoxy-1-pentyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
7-methoxy-1-phenyl-2,3,4,9-tetrahydro-1H-beta-carboline
-
-
7-methoxy-1-phenyl-4,9-dihydro-3H-beta-carboline
-
-
7-methoxy-2,3,4,9-tetrahydro-1H-beta-carboline-1-carboxylic acid
-
-
aminoadamantan
-
-
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CH2Cl
-
irreversible inhibitor of recombinant enzyme
benzyloxycarbonyl-Leu-Pro-Ala-Thr-CHN2
-
irreversible inhibitor of recombinant enzyme
berberine chloride
beta-sitosterol-3-O-glucopyranoside
bis(4-ethoxy-2-phenyl-5-pyridazyl)disulfide
-
-
cis-1,2-bis(phenylsulfonyl)ethylene
-
IC50: 0.00113 mM, irreversible
demethylaaptamine
-
-
demethyloxyaaptamine
-
-
divinyl sulfone
-
IC50: 0.00106 mM, irreversible
ethyl 4-[3-(4-bromophenyl)-3-oxopropyl]piperazine-1-carboxylate
-
-
ethyl vinyl sulfone
-
IC50: 0.00471 mM, irreversible
galangin
-
IC50 for recombinant SrtA(DELTA24): 0.123 mM, no antibacterial activity against Staphylococcus aureus
galangin-3-methyl ether
-
IC50 for recombinant SrtA(DELTA24): 0.1179 mM, no antibacterial activity against Staphylococcus aureus
iodoacetamide
-
active site Cys184 of sortase A can be alkylated by iodoacetamide resulting in irreversible modified enzyme. The selenol and thiol of mutant Sec-sortase and mutant Hcy-sortase are sensitive to alkylation as well
isoaaptamine
-
the suppression of fibronectin-binding activity by isoaaptamine highlights its potential for the treatment of Staphylococcus aureus infections via inhibition of SrtA activity
isorhamnetin
-
IC50 for recombinant SrtA(DELTA24): 0.05886 mM, no antibacterial activity against Staphylococcus aureus
isorhamnetin 3-O-beta-D-rutinoside
-
-
kaempferol
-
IC50 for recombinant SrtA(DELTA24): 0.07794 mM, no antibacterial activity against Staphylococcus aureus
kaempferol-3-rutinoside
-
-
maltol 3-O-(4'-O-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
-
-
maltol-3-O-(4'-O-cis-p-coumaroyl-6'-O-(3-hydroxy-3-methylglutaroyl))-beta-glucopyranoside
-
-
methyl (2E)-2,3-bis(4-methoxyphenyl)acrylate
-
IC50: 0.231 mM
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-phenyltetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,3S,7aS)-2-ethenesulfonyl-5-oxo-3-pyridin-3-yl-tetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,3S,7aS)-3-(3,4-dimethoxyphenyl)-2-ethenesulfonyl-5-oxotetrahydropyrrolizine-7a-carboxylate
-
-
methyl (2S,4S,5S)-4-ethenesulfonyl-2-(2-methoxycarbonylethyl)-5-pyridin-3-yl-pyrrolidine-2-carboxylate
-
-
methyl (2Z)-2,3-bis(4-methoxyphenyl)acrylate
-
IC50: 0.909 mM
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(2-fluorophenyl)-L-prolinate
-
-
methyl (4S,5S)-4-(ethenylsulfonyl)-5-(3-fluorophenyl)-L-prolinate
-
-
methyl (4S,5S)-4-(ethenylsulfonyl)-5-phenyl-L-prolinate
-
-
methyl 1-aminoadamantan-3-carboxylate
-
-
methyl 2-morpholin-4-yl-5-[[(2E)-3-(2-thienyl)prop-2-enoyl]amino]benzoate
-
-
methyl 3-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
-
-
methyl 3-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamido)adamantane-1-carboxylate
-
-
methyl 4-[3-(dimethylamino)propanoyl]benzenesulfinate
-
-
methyl 5-hydroxy-1H-indole-3-carboxylate
-
-
methyl 5-[[(2E)-3-(2-furyl)prop-2-enoyl]amino]-2-morpholin-4-ylbenzoate
-
-
methyl vinyl sulfone
-
IC50: 0.00624 mM, irreversible
morin
-
IC50 for recombinant SrtA(DELTA24): 0.03739 mM, no antibacterial activity against Staphylococcus aureus
myricetin
-
IC50 for recombinant SrtA(DELTA24): 0.04403 mM, no antibacterial activity against Staphylococcus aureus
N'-(2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetyl)adamantane-1-carbohydrazide
-
-
N'-(3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
-
-
N'-(3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanoyl)adamantane-1-carbohydrazide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3,5-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-2-(3-oxobenzo[d]isothiazol-2(3H)-yl)acetamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxy-5,7-dimethyladamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-hydroxyadamantan-1-yl)-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(3-ydroxyadamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-(adamantan-1-yl)-3-(4-fluoro-3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
N-adamantan-1-yl-3-(3-oxobenzo[d]isothiazol-2(3H)-yl)propanamide
-
-
NH2-YALPE-AlaPsi(PO2H-CH2)Gly-EE-NH2
-
nonhydrolyzable phosphinic peptidomimetic inhibitor of SrtA derived from the LPXTG substrate sequence, simple reversible competitive inhibitor
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoic acid
-
-
phenyl vinyl sulfone
psammaplin A1
-
potential of this inhibitor for the treatment of Staphylococcus aureus infections
quercetin
-
IC50 for recombinant SrtA(DELTA24): 0.0527 mM, no antibacterial activity against Staphylococcus aureus
quercetin-3,3'-dimethyl ether
-
IC50 for recombinant SrtA(DELTA24): 0.05361 mM, no antibacterial activity against Staphylococcus aureus
[2-(trimethylammonium)ethyl]methanethiosulfonate
-
the inhibitor interferes with the cleavage of sorting signals at the LPXTG motif
[4-(6-bromo-1H-indol-3-yl)-1H-imidazol-2-yl](1H-indol-3-yl)methanone
-
IC50: 19.44 mg/L
[4-(6-bromo-1H-indol-3-yl)-1H-imidazol-2-yl](6-hydroxy-1H-indol-3-yl)methanone
-
IC50: 16.7 mg/L
additional information
-