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Literature summary extracted from

  • Chen, X.; Ghavimi, B.; Corbett, R.L.; Xue, C.; Liu, R.; Covington, M.B.; Qian, M.; Vaddi, K.G.; Christ, D.D.; Hartman, K.D.; Ribadeneira, M.D.; Trzaskos, J.M.; Newton, R.C.; Decicco, C.P.; Duan, J.J.
    A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1 group for the beta-amino hydroxamic acid derived TACE inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 1865-1870.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.86 (3R,4R)-4-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-4-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-N-hydroxy-4-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-N-hydroxy-4-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3R,4R)-N-hydroxy-4-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
 Sus scrofa
3.4.24.86 N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
-
 Sus scrofa
3.4.24.86 N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
 Sus scrofa
3.4.24.86 N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
 Sus scrofa
3.4.24.86 N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydrofuran-3-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
-
 Sus scrofa
3.4.24.86 tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
 Sus scrofa
3.4.24.86 tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
-
 Sus scrofa

Organism

EC Number Organism UniProt Comment Textmining
3.4.24.86 Sus scrofa
-
-
-

Synonyms

EC Number Synonyms Comment Organism
3.4.24.86 TACE
-
 Sus scrofa
3.4.24.86 tumor necrosis factor alpha-converting enzyme
-
 Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.86 0.000001
-
-
 Sus scrofa (3R,4R)-4-([[4-(2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-1-but-2-yn-1-yl-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
3.4.24.86 0.000001
-
 IC50 below 0.000001 mM Sus scrofa (3R,4R)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000011
-
-
 Sus scrofa (3S,4S)-1-(butylsulfonyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000012
-
-
 Sus scrofa (3R,4R)-4-[([4-[(2,3-dimethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000012
-
-
 Sus scrofa (3R,4R)-4-[[(4-[[2-(dimethylamino)quinolin-4-yl]methyl]phenyl)carbonyl]amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000013
-
-
 Sus scrofa (3R,4R)-4-([[4-(2,3-dihydrofuro[2,3-b]quinolin-4-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000013
-
-
 Sus scrofa (3R,4R)-4-[([4-[(2-cyclopropylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000013
-
-
 Sus scrofa tert-butyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
3.4.24.86 0.0000015
-
-
 Sus scrofa (3R,4R)-N-hydroxy-4-[([4-[(3-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000015
-
-
 Sus scrofa (3S,4S)-1-(2,2-dimethylpropanoyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000016
-
-
 Sus scrofa (3R,4R)-N-hydroxy-4-[([4-[(2-morpholin-4-ylquinolin-4-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000016
-
-
 Sus scrofa (3S,4S)-1-(2,2-dimethylpropyl)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000016
-
-
 Sus scrofa (3S,4S)-N-hydroxy-1-(2-methylpropyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000017
-
-
 Sus scrofa (3R,4R)-4-[([4-[(2-ethylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000018
-
-
 Sus scrofa N-[2-(hydroxycarbamoyl)cyclopentyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
3.4.24.86 0.000002
-
-
 Sus scrofa N-[4-[2-(hydroxyamino)-2-oxoethyl]tetrahydrofuran-3-yl]-4-[(2-methylquinolin-4-yl)methyl]benzamide
3.4.24.86 0.0000022
-
-
 Sus scrofa (3R,4R)-N-hydroxy-4-[[(4-[[2-(trifluoromethyl)quinolin-4-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000025
-
-
 Sus scrofa (3S,4S)-N-hydroxy-1-methyl-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000026
-
-
 Sus scrofa (3R,4R)-4-([[4-(1,3-dihydrofuro[3,4-b]quinolin-9-ylmethyl)phenyl]carbonyl]amino)-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.0000033
-
-
 Sus scrofa methyl (3S,4S)-3-(hydroxycarbamoyl)-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-1-carboxylate
3.4.24.86 0.0000035
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)oxy]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000043
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
3.4.24.86 0.0000078
-
-
 Sus scrofa (3R,4R)-4-[([4-[(3-ethyl-2-methylquinolin-4-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-3-carboxamide
3.4.24.86 0.000097
-
-
 Sus scrofa N-[1-[2-(hydroxyamino)-2-oxoethyl]cyclohexyl]-4-[(2-methylquinolin-4-yl)methyl]benzamide