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Literature summary for 3.4.24.81 extracted from

  • Madoux, F.; Dreymuller, D.; Pettiloud, J.P.; Santos, R.; Becker-Pauly, C.; Ludwig, A.; Fields, G.B.; Bannister, T.; Spicer, T.P.; Cudic, M.; Scampavia, L.D.; Minond, D.
    Discovery of an enzyme and substrate selective inhibitor of ADAM10 using an exosite-binding glycosylated substrate (2016), Sci. Rep., 6, 11 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
2-(2,4-dioxo-3-phenyl-1,3-thiazolidin-5-yl)-N-(4-ethoxyphenyl)acetamide
-
Homo sapiens
3-[[1-[(2-(hydroxymethyl)-1-pyrrolidinyl)carbonyl]-2-methylpropyl]carbamoyl]octanohydroxamic acid actinonin Homo sapiens
4-(1H-indol-3-yl)-4-oxobutanoic acid
-
Homo sapiens
5-[(4-chlorophenyl)methyl]-5-phenylimidazolidine-2,4-dione
-
Homo sapiens
ADAM10 prodomain
-
Homo sapiens
GI254023X
-
Homo sapiens
marimastat
-
Homo sapiens
N-(3-chloro-4-methylphenyl)-2-[2-(3-methoxybenzoyl)hydrazinyl]-2-oxoacetamide selective, non-competitive inhibitor Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ contains zinc Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O14672
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
CXCL16 + H2O
-
Homo sapiens ?
-
?
E(Edans)-PLAQAVRSSS[O-(beta-D-Glc-(1->3)-alpha-D-GlcNAc]-K(Dabcyl) + H2O
-
Homo sapiens E(Edans)-PLAQA + VRSSS[O-(beta-D-Glc-(1->3)-alpha-D-GlcNAc]-K(Dabcyl)
-
ir
HER2 + H2O
-
Homo sapiens ?
-
?
syndecan + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
ADAM10
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000883
-
N-(3-chloro-4-methylphenyl)-2-[2-(3-methoxybenzoyl)hydrazinyl]-2-oxoacetamide at pH 7.5 and 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0065
-
at pH 7.5 and 25°C Homo sapiens N-(3-chloro-4-methylphenyl)-2-[2-(3-methoxybenzoyl)hydrazinyl]-2-oxoacetamide
0.032
-
at pH 7.5 and 25°C Homo sapiens 5-[(4-chlorophenyl)methyl]-5-phenylimidazolidine-2,4-dione
0.07
-
IC50 above 0.07 mM, at pH 7.5 and 25°C Homo sapiens 4-(1H-indol-3-yl)-4-oxobutanoic acid
0.07
-
IC50 above 0.07 mM, at pH 7.5 and 25°C Homo sapiens 2-(2,4-dioxo-3-phenyl-1,3-thiazolidin-5-yl)-N-(4-ethoxyphenyl)acetamide
0.07
-
IC50 above 0.07 mM, at pH 7.5 and 25°C Homo sapiens 3-[[1-[(2-(hydroxymethyl)-1-pyrrolidinyl)carbonyl]-2-methylpropyl]carbamoyl]octanohydroxamic acid