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Literature summary extracted from

  • Lu, Z.; Ott, G.R.; Anand, R.; Liu, R.Q.; Covington, M.B.; Vaddi, K.; Qian, M.; Newton, R.C.; Christ, D.D.; Trzaskos, J.; Duan, J.J.
    Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1 substituents (2008), Bioorg. Med. Chem. Lett., 18, 1958-1962.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.24.86 (3S,4S)-3-[([4-[(2-cyclopropylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-3-[([4-[(2-ethyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-3-[([4-[(2-ethylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-3-[([4-[(2-tert-butylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[([4-[(2-methylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide substance exhibits excellent oral bioavailability in pharmacokinetic studies Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-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-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
-
 Sus scrofa
3.4.24.86 (3S,4S)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]pyrrolidine-3-carboxamide
-
 Sus scrofa

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.24.86 blood cellular suppression of TNF-alpha is measured using human whole blood (WBA) stimulated with lipopolysaccharide (LPS) Sus scrofa
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.24.86 TNF-alpha + H2O
-
 Sus scrofa ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.24.86 TACE
-
 Sus scrofa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.24.86 0.000001
-
 (3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
-
 Sus scrofa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-3-[([4-[(2-cyclopropylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[([4-[(2-methylimidazo[1,2-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-3-[([4-[(2-ethyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.000001
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]-1-prop-2-yn-1-ylpyrrolidine-3-carboxamide
3.4.24.86 0.0000015
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[[(4-[[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000016
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1-benzofuran-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000017
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000018
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]pyrrolidine-3-carboxamide
3.4.24.86 0.000002
-
-
 Sus scrofa (3S,4S)-3-[([4-[(2-ethylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000021
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)-1-benzofuran-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000022
-
-
 Sus scrofa (3S,4S)-N-hydroxy-4-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]pyrrolidine-3-carboxamide
3.4.24.86 0.0000028
-
-
 Sus scrofa (3S,4S)-3-[([4-[(2-tert-butylpyrazolo[1,5-a]pyridin-3-yl)methyl]phenyl]carbonyl)amino]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.0000032
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[[(4-[[2-(1-methylethyl)imidazo[1,2-a]pyridin-3-yl]methyl]phenyl)carbonyl]amino]tetrahydro-2H-pyran-4-carboxamide
3.4.24.86 0.000006
-
-
 Sus scrofa (3S,4S)-N-hydroxy-3-[([4-[(2-methyl-1H-indol-3-yl)methyl]phenyl]carbonyl)amino]tetrahydro-2H-pyran-4-carboxamide