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Literature summary for 3.4.24.86 extracted from

  • Condon, J.S.; Joseph-McCarthy, D.; Levin, J.I.; Lombart, H.; Lovering, F.E.; Sun, L.; Wang, W.; Xu, W.; Zhang, Y.
    Identification of potent and selective TACE inhibitors via the S1 pocket (2007), Bioorg. Med. Chem. Lett., 17, 34-39.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(1,3-benzoxazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
1-(1H-benzimidazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
1-ethylpropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
1-methyl-2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
1-methylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
1-[(4-acetylpiperazin-1-yl)sulfonyl]-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-(dimethylsulfamoyl)-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dichlorothiophen-3-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dimethyl-1,3-thiazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)carbonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)methyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethyl-1H-pyrazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(5-chlorothiophen-2-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(morpholin-4-ylsulfonyl)piperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(piperidin-1-ylsulfonyl)piperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(pyrrolidin-1-ylsulfonyl)piperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-2-ylpiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-4-ylpiperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[(2-methyl-1H-imidazol-4-yl)sulfonyl]piperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
Homo sapiens
4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
-
Homo sapiens
cyclohexyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
cyclohexylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
cyclopentyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
cyclopropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
pyridin-4-ylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens
tert-butyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
TACE
-
Homo sapiens
tumor necrosis factor alpha-converting enzyme
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(morpholin-4-ylsulfonyl)piperidine-4-carboxamide
0.000001
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(pyrrolidin-1-ylsulfonyl)piperidine-4-carboxamide
0.000001
-
IC50 above 0.000001 mM Homo sapiens 1-(1H-benzimidazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
0.000001
-
IC50 above 0.000001 mM Homo sapiens cyclohexylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.000001
-
IC50 above 0.000001 mM Homo sapiens tert-butyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.000001
-
IC50 below 0.000001 mM Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dichlorothiophen-3-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
0.000001
-
IC50 below 0.000001 mM Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(2,5-dimethyl-1,3-thiazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
0.000001
-
IC50 below 0.000001 mM Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethyl-1H-pyrazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
0.0000011
-
-
Homo sapiens 1-(1,3-benzoxazol-2-yl)-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
0.0000012
-
-
Homo sapiens 1-ethylpropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000012
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-(piperidin-1-ylsulfonyl)piperidine-4-carboxamide
0.0000013
-
-
Homo sapiens cyclopentyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.00000133
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-2-ylpiperidine-4-carboxamide
0.0000014
-
-
Homo sapiens 1-methyl-2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000014
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
0.0000015
-
-
Homo sapiens 1-[(4-acetylpiperazin-1-yl)sulfonyl]-4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxypiperidine-4-carboxamide
0.0000015
-
-
Homo sapiens 1-methylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000015
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl]piperidine-4-carboxamide
0.0000016
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)methyl]-N-hydroxypiperidine-4-carboxamide
0.0000016
-
-
Homo sapiens cyclopropyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000017
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dichloropyridin-4-yl)carbonyl]-N-hydroxypiperidine-4-carboxamide
0.0000018
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-(dimethylsulfamoyl)-N-hydroxypiperidine-4-carboxamide
0.000002
-
-
Homo sapiens pyridin-4-ylmethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000022
-
-
Homo sapiens 2-morpholin-4-ylethyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.0000022
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(3,5-dimethylisoxazol-4-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
0.0000028
-
-
Homo sapiens cyclohexyl 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-4-(hydroxycarbamoyl)piperidine-1-sulfinate
0.000003
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-[(2-methyl-1H-imidazol-4-yl)sulfonyl]piperidine-4-carboxamide
0.0000056
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-N-hydroxy-1-pyridin-4-ylpiperidine-4-carboxamide
0.000007
-
-
Homo sapiens 4-([[4-(but-2-yn-1-yloxy)phenyl]sulfonyl]methyl)-1-[(5-chlorothiophen-2-yl)sulfonyl]-N-hydroxypiperidine-4-carboxamide