Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.24.86 extracted from

  • Mazzola, R.D.; Zhu, Z.; Sinning, L.; McKittrick, B.; Lavey, B.; Spitler, J.; Kozlowski, J.; Neng-Yang, S.; Zhou, G.; Guo, Z.; Orth, P.; Madison, V.; Sun, J.; Lundell, D.; Niu, X.
    Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors, Part II Optimization of the S3 pocket (2008), Bioorg. Med. Chem. Lett., 18, 5809-5814.
    View publication on PubMed
Search for more literature for 3.4.24.86

Inhibitors

Inhibitors Comment Organism Structure
(1R,2S)-1-(3-fluoro-4-[[2-(1-methyl-1H-pyrazol-5-yl)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-(3-fluoro-4-[[2-(methylamino)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[3-fluoro-4-[(2-morpholin-4-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[3-fluoro-4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[3-fluoro-4-[(2-pyrrolidin-1-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-N2-hydroxy-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N1-(piperidin-4-ylmethyl)cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
(1S,2R)-2-[[(3R)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
(1S,2R)-2-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
(1S,2R)-N-hydroxy-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
(1S,2R)-N-hydroxy-2-[[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
(1S,2S)-2-((S)-cyano(4-((2-phenylquinolin-4-yl)methoxy)phenyl)methyl)-N-hydroxycyclopropanecarboxamide
-
 Homo sapiens
ethyl (1R,2S)-1-[3-bromo-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-1-[3-chloro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-1-[3-fluoro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(2-methylpropyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(trifluoromethyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylpyridin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P78536
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information affinity for TACE is measured by an internally quenched peptide substrate with its sequence derived from the pro-TNF-alpha cleavage site using a catalytic domain of recombinant human TACE enzyme Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
TACE
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000014
-
 (1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000014
-
 (1R,2S)-1-[3-fluoro-4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000015
-
 (1R,2S)-1-[3-fluoro-4-[(2-pyrrolidin-1-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000015
-
 (1R,2S)-1-(3-fluoro-4-[[2-(1-methyl-1H-pyrazol-5-yl)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000018
-
 (1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000021
-
 (1R,2S)-1-[3-fluoro-4-[(2-morpholin-4-ylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000025
-
 (1S,2R)-N-hydroxy-2-[[(3S)-3-hydroxypyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
0.00000028
-
 (1R,2S)-N2-hydroxy-N1,N1-dimethyl-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.0000003
-
 (1S,2R)-N-hydroxy-2-[[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]carbonyl]-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
0.00000036
-
 (1R,2S)-1-[3-fluoro-4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N2-hydroxy-N1,N1-dimethylcyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000038
-
 (1S,2R)-2-[[(3R)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
0.00000054
-
 (1S,2R)-2-[[(3S)-3-(dimethylamino)pyrrolidin-1-yl]carbonyl]-N-hydroxy-2-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxamide
-
 Homo sapiens
0.00000063
-
 (1R,2S)-N2-hydroxy-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]-N1-(piperidin-4-ylmethyl)cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.00000076
-
 (1R,2S)-1-(3-fluoro-4-[[2-(methylamino)quinolin-4-yl]methoxy]benzyl)-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.000001
-
 (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-N2-hydroxycyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.000002
-
 ethyl (1R,2S)-1-[4-[(2-ethylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
0.000003
-
 (1R,2S)-N2-hydroxy-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropane-1,2-dicarboxamide
-
 Homo sapiens
0.000003
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(trifluoromethyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
 Homo sapiens
0.000004
-
 (1S,2S)-2-((S)-cyano(4-((2-phenylquinolin-4-yl)methoxy)phenyl)methyl)-N-hydroxycyclopropanecarboxamide
-
 Homo sapiens
0.000005
-
 ethyl (1R,2S)-1-[3-fluoro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
0.000006
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-methylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
0.000012
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
0.000018
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-(4-[[2-(2-methylpropyl)quinolin-4-yl]methoxy]benzyl)cyclopropanecarboxylate
-
 Homo sapiens
0.000022
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-pyridin-3-ylquinolin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
0.000037
-
 ethyl (1R,2S)-2-(hydroxycarbamoyl)-1-[4-[(2-phenylpyridin-4-yl)methoxy]benzyl]cyclopropanecarboxylate
-
 Homo sapiens
0.000158
-
 ethyl (1R,2S)-1-[3-chloro-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens
0.000381
-
 ethyl (1R,2S)-1-[3-bromo-4-[(2-methylquinolin-4-yl)methoxy]benzyl]-2-(hydroxycarbamoyl)cyclopropanecarboxylate
-
 Homo sapiens