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Literature summary for 3.4.24.B4 extracted from

  • Noe, M.C.; Snow, S.L.; Wolf-Gouveia, L.A.; Mitchell, P.G.; Lopresti-Morrow, L.; Reeves, L.M.; Yocum, S.A.; Liras, J.L.; Vaughn, M.
    3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase (2004), Bioorg. Med. Chem. Lett., 14, 4727-4730.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R,4S)-1-((4-[(2-chlorobenzyl)oxy]phenyl)sulfonyl)-N,4-dihydroxypiperidine-2-carboxamide i.e. rTACE, 50% inhibition at 12 nM Homo sapiens
(3S)-N,3-dihydroxy-4-[(3'-methylbiphenyl-4-yl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 0.43 nM, not inhibitory to aggrecanase Homo sapiens
(3S)-N,3-dihydroxy-4-[(4'-methylbiphenyl-4-yl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 0.39 nM, not inhibitory to aggrecanase Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(2,4-dichlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition of enzyme at 0.95 nM, 50% inhibition of aggrecanase at 8.1 nM Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(2-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 2.7 nM Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(3-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 2.4 nM Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(3-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 5 nM Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(4-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 0.88 nM, selective for enzyme Homo sapiens
(3S)-N,3-dihydroxy-4-[(4-(4-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide 50% inhibition at 1.3 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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