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Literature summary for 3.4.24.86 extracted from

  • Ott, G.R.; Asakawa, N.; Liu, R.; Covington, M.B.; Qian, M.; Vaddi, K.; Newton, R.C.; Trzaskos, J.M.; Christ, D.D.; Galya, L.; Scholz, T.; Marshall, W.; Duan, J.J.
    alpha,beta-cyclic-beta-Benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) (2008), Bioorg. Med. Chem. Lett., 18, 1288-1292.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
-
Sus scrofa
(3S,4S)-1-(furan-2-ylmethyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-1-acetyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-1-cyclobutyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-1-(1-methylethyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-1-(2-methylprop-2-en-1-yl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-1-(2-methylpropanoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-phenylpyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-prop-2-en-1-ylpyrrolidine-3-carboxamide
-
Sus scrofa
(3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
Sus scrofa
(5R,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
-
Sus scrofa
(5S,6S)-N-hydroxy-5-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,3,5,6-tetrahydro-4aH-cyclopenta[b][1,4]dioxine-6-carboxamide
-
Sus scrofa
(5S,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
-
Sus scrofa
(7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,4-dioxaspiro[4.4]nonane-7-carboxamide
-
Sus scrofa
1-methylethyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
Sus scrofa
methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
Sus scrofa
N-[(1R,2S)-2-(hydroxycarbamoyl)-4-oxocyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
Sus scrofa
N-[(1R,2S)-4,4-difluoro-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
Sus scrofa
N-[(1R,2S)-4-aziridin-1-yl-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
Sus scrofa
N-[(1R,2S)-4-hydroxy-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
-
Sus scrofa

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Synonyms

Synonyms Comment Organism
TACE
-
Sus scrofa
TNF-alpha converting enzyme
-
Sus scrofa
tumor necrosis factor-alpha converting enzyme
-
Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000004
-
-
Sus scrofa (3S,4S)-N-hydroxy-1-(1-methylethyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.00000063
-
-
Sus scrofa N-[(1R,2S)-4,4-difluoro-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
0.00000094
-
-
Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-prop-2-en-1-ylpyrrolidine-3-carboxamide
0.000001
-
-
Sus scrofa (3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
0.000001
-
-
Sus scrofa (3S,4S)-1-cyclobutyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.000001
-
-
Sus scrofa (5R,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
0.000001
-
-
Sus scrofa (5S,6S)-N-hydroxy-5-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-2,3,5,6-tetrahydro-4aH-cyclopenta[b][1,4]dioxine-6-carboxamide
0.000001
-
-
Sus scrofa (5S,7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-oxaspiro[4.4]nonane-7-carboxamide
0.000001
-
-
Sus scrofa (7S,8R)-N-hydroxy-8-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1,4-dioxaspiro[4.4]nonane-7-carboxamide
0.000001
-
-
Sus scrofa methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
0.000001
-
IC50 below 0.000001 mM Sus scrofa N-[(1R,2S)-4-aziridin-1-yl-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
0.0000011
-
-
Sus scrofa (3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000013
-
-
Sus scrofa (3S,4S)-1-acetyl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000015
-
-
Sus scrofa (3S,4S)-N-hydroxy-1-(2-methylprop-2-en-1-yl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000015
-
-
Sus scrofa 1-methylethyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
0.0000016
-
-
Sus scrofa (3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000016
-
-
Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]-1-phenylpyrrolidine-3-carboxamide
0.0000018
-
-
Sus scrofa N-[(1R,2S)-2-(hydroxycarbamoyl)-4-oxocyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
0.000002
-
-
Sus scrofa (3S,4S)-1-(furan-2-ylmethyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000021
-
-
Sus scrofa (3S,4S)-N-hydroxy-1-(2-methylpropanoyl)-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
0.0000023
-
-
Sus scrofa (3R,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]tetrahydrofuran-3-carboxamide
0.0000046
-
-
Sus scrofa N-[(1R,2S)-4-hydroxy-2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
0.0000063
-
-
Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methoxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide