Literature summary for 3.4.24.86 extracted from

Huang, A.; Joseph-McCarthy, D.; Lovering, F.; Sun, L.; Wang, W.; Xu, W.; Zhu, Y.; Cui, J.; Zhang, Y.; Levin, J.I.
Structure-based design of TACE selective inhibitors: Manipulations in the S1-S3 pocket (2007), Bioorg. Med. Chem., 15, 6170-6181.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(3S)-4-[[4-(but-2-ynylamino)phenyl]sulfonyl]-N-hydroxy-2,2-dimethylthio-morpholine-3-carboxamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-benzoyl)-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-butyryl)-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(propane-2-sulfonyl)-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-isobutyryl-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-pyridin-4-ylmethyl-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid 1-diethylamide 4-hydroxyamide	-	Homo sapiens
4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-4-carboxylic acid hydroxyamide	-	Homo sapiens
4-[([4-[(1,1-dimethylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)methyl]-N-hydroxy-1-(isopropylsulfonyl)piperidine-4-carboxamide	-	Homo sapiens
4-[4-(4-hydroxy-but-2-ynylamino)-benzenesulfonylmethyl]-4-hydroxycarbamoyl-piperidine-1-carboxylic acid tert-butyl ester	-	Homo sapiens
BMS-561392	-	Homo sapiens
PKF242-484	-	Homo sapiens
Ro 32-7315	-	Homo sapiens
tert-butyl 4-([[4-(but-2-ynylamino)phenyl]sulfonyl]methyl)-4-[(hydroxyamino)-carbonyl]piperidine-1-carboxylate	-	Homo sapiens
tert-butyl 4-[([4-[but-2-ynyl(methyl)amino]phenyl]sulfonyl)methyl]-4-[(hydroxyamino)carbonyl]piperidine-1-carboxylate	-	Homo sapiens
TMI-1	-	Homo sapiens
[N-hydroxy-1-(isopropylsulfonyl)-4-[(4-[(1-methylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)-methyl]piperidine-4-carboxamide	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
26 kDa proTNF-alpha + H2O	-	Homo sapiens	17 kDa soluble TNF-alpha + ?	-	?
p75 tumour necrosis factor receptor + H2O	-	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
ADAM17	-	Homo sapiens
TACE	-	Homo sapiens
tumor necrosis factor alpha-converting enzyme	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000001	-	IC50 below 0.000001 mM	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid 1-diethylamide 4-hydroxyamide
0.0000016	-	-	Homo sapiens	tert-butyl 4-([[4-(but-2-ynylamino)phenyl]sulfonyl]methyl)-4-[(hydroxyamino)-carbonyl]piperidine-1-carboxylate
0.000002	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(propane-2-sulfonyl)-piperidine-4-carboxylic acid hydroxyamide
0.0000023	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-isobutyryl-piperidine-4-carboxylic acid hydroxyamide
0.0000023	-	-	Homo sapiens	(3S)-4-[[4-(but-2-ynylamino)phenyl]sulfonyl]-N-hydroxy-2,2-dimethylthio-morpholine-3-carboxamide
0.0000025	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-benzoyl)-piperidine-4-carboxylic acid hydroxyamide
0.0000033	-	-	Homo sapiens	tert-butyl 4-[([4-[but-2-ynyl(methyl)amino]phenyl]sulfonyl)methyl]-4 [(hydroxyamino)carbonyl]piperidine-1-carboxylate
0.0000035	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-(2-methyl-butyryl)-piperidine-4-carboxylic acid hydroxyamide
0.000004	-	-	Homo sapiens	[N-hydroxy-1-(isopropylsulfonyl)-4-[(4-[(1-methylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)-methyl]piperidine-4-carboxamide
0.0000064	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-1-pyridin-4-ylmethyl-piperidine-4-carboxylic acid hydroxyamide
0.000008	-	-	Homo sapiens	TMI-1
0.00001	-	-	Homo sapiens	4-[4-(4-hydroxy-but-2-ynylamino)-benzenesulfonylmethyl]-4-hydroxycarbamoyl-piperidine-1-carboxylic acid tert-butyl ester
0.000027	-	-	Homo sapiens	4-[([4-[(1,1-dimethylbut-2-yn-1-yl)oxy]phenyl]sulfonyl)methyl]-N-hydroxy-1-(isopropylsulfonyl)piperidine-4-carboxamide
0.000064	-	-	Homo sapiens	4-(4-but-2-ynylamino-benzenesulfonylmethyl)-piperidine-4-carboxylic acid hydroxyamide

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Release 2023.1 (January 2023)