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Literature summary for 3.4.24.82 extracted from

  • Xiang, J.S.; Hu, Y.; Rush, T.S.; Thomason, J.R.; Ipek, M.; Sum, P.E.; Abrous, L.; Sabatini, J.J.; Georgiadis, K.; Reifenberg, E.; Majumdar, M.; Morris, E.A.; Tam, S.
    Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 311-316.
    View publication on PubMed
Search for more literature for 3.4.24.82

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-(biphenyl-4-ylsulfonyl)-3-(1H-indol-2-yl)propanoic acid IC50: 0.0028 mM Rattus norvegicus
(2R)-2-(biphenyl-4-ylsulfonyl)-3-phenylpropanoic acid IC50: 0.0043 mM Rattus norvegicus
(2R)-2-(biphenyl-4-ylsulfonyl)pentanedioic acid IC50: 0.0011 mM Rattus norvegicus
(2R)-2-(biphenyl-4-ylsulfonyl)propanoic acid IC50: 0.0055 mM Rattus norvegicus
3-[(biphenyl-4-ylsulfonyl)amino]-4-methylpentanoic acid IC50: 0.1 mM Rattus norvegicus
N-(biphenyl-3-ylsulfonyl)-D-valine IC50: 0.1 mM Rattus norvegicus
N-(biphenyl-4-ylsulfonyl)-D-valine IC50: 0.003 mM Rattus norvegicus
N-(biphenyl-4-ylsulfonyl)-L-valine IC50: 0.1 mM Rattus norvegicus
N-(biphenyl-4-ylsulfonyl)-N-(pyridin-3-ylmethyl)-D-valine IC50: 0.012 mM Rattus norvegicus
N-(biphenyl-4-ylsulfonyl)-N-methyl-D-valine IC50: 0.0016 mM Rattus norvegicus
N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)-D-valine IC50: 0.0075 mM Rattus norvegicus
N-([4'-[(1-benzofuran-2-ylcarbonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine IC50: 0.00035 mM Rattus norvegicus
N-([4'-[(furan-2-yloxy)carbonyl]biphenyl-4-yl]sulfonyl)-D-valine IC50: 0.0116 mM Rattus norvegicus
N-([4'-[(Z)-2-(1-benzofuran-2-yl)ethenyl]biphenyl-4-yl]sulfonyl)-D-valine IC50: 0.0004 mM Rattus norvegicus
N-([4'-[2-(1-benzofuran-2-yl)-2-oxoethyl]biphenyl-4-yl]sulfonyl)-D-valine IC50: 0.0038 mM Rattus norvegicus
N-[(2'-aminobiphenyl-4-yl)sulfonyl]-D-valine IC50: 0.05 mM Rattus norvegicus
N-[(2'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine IC50: 0.02 mM Rattus norvegicus
N-[(2-aminobiphenyl-4-yl)sulfonyl]-D-valine IC50: 0.03 mM Rattus norvegicus
N-[(3'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine IC50: 0.009 mM Rattus norvegicus
N-[(4'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine IC50: 0.0046 mM Rattus norvegicus
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)carbonyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine IC50: 0.000086 mM Rattus norvegicus
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)oxy]methyl]biphenyl-4-yl)sulfonyl]-D-valine IC50: 0.0007 mM Rattus norvegicus
N-[[4'-(1-benzofuran-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine IC50: 0.0014 mM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cartilage
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan + H2O
-
 Rattus norvegicus fragments of aggrecan
-
 ?

Synonyms

Synonyms Comment Organism
agg-1
-
 Rattus norvegicus
aggrecanase-1
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000086
-
 IC50: 0.000086 mM Rattus norvegicus N-[(4'-[[(3-methyl-1-benzofuran-2-yl)carbonyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
0.00035
-
 IC50: 0.00035 mM Rattus norvegicus N-([4'-[(1-benzofuran-2-ylcarbonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0004
-
 IC50: 0.0004 mM Rattus norvegicus N-([4'-[(Z)-2-(1-benzofuran-2-yl)ethenyl]biphenyl-4-yl]sulfonyl)-D-valine
0.0007
-
 IC50: 0.0007 mM Rattus norvegicus N-[(4'-[[(3-methyl-1-benzofuran-2-yl)oxy]methyl]biphenyl-4-yl)sulfonyl]-D-valine
0.0011
-
 IC50: 0.0011 mM Rattus norvegicus (2R)-2-(biphenyl-4-ylsulfonyl)pentanedioic acid
0.0014
-
 IC50: 0.0014 mM Rattus norvegicus N-[[4'-(1-benzofuran-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0016
-
 IC50: 0.0016 mM Rattus norvegicus N-(biphenyl-4-ylsulfonyl)-N-methyl-D-valine
0.0028
-
 IC50: 0.0028 mM Rattus norvegicus (2R)-2-(biphenyl-4-ylsulfonyl)-3-(1H-indol-2-yl)propanoic acid
0.003
-
 IC50: 0.003 mM Rattus norvegicus N-(biphenyl-4-ylsulfonyl)-D-valine
0.0038
-
 IC50: 0.0038 mM Rattus norvegicus N-([4'-[2-(1-benzofuran-2-yl)-2-oxoethyl]biphenyl-4-yl]sulfonyl)-D-valine
0.0043
-
 IC50: 0.0043 mM Rattus norvegicus (2R)-2-(biphenyl-4-ylsulfonyl)-3-phenylpropanoic acid
0.0046
-
 IC50: 0.0046 mM Rattus norvegicus N-[(4'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
0.0055
-
 IC50: 0.0055 mM Rattus norvegicus (2R)-2-(biphenyl-4-ylsulfonyl)propanoic acid
0.0075
-
 IC50: 0.0075 mM Rattus norvegicus N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)-D-valine
0.009
-
 IC50: 0.009 mM Rattus norvegicus N-[(3'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
0.0116
-
 IC50: 0.0116 mM Rattus norvegicus N-([4'-[(furan-2-yloxy)carbonyl]biphenyl-4-yl]sulfonyl)-D-valine
0.012
-
 IC50: 0.012 mM Rattus norvegicus N-(biphenyl-4-ylsulfonyl)-N-(pyridin-3-ylmethyl)-D-valine
0.02
-
 IC50: 0.02 mM Rattus norvegicus N-[(2'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
0.03
-
 IC50: 0.03 mM Rattus norvegicus N-[(2-aminobiphenyl-4-yl)sulfonyl]-D-valine
0.05
-
 IC50: 0.05 mM Rattus norvegicus N-[(2'-aminobiphenyl-4-yl)sulfonyl]-D-valine
0.1
-
 IC50: 0.1 mM Rattus norvegicus N-(biphenyl-3-ylsulfonyl)-D-valine
0.1
-
 IC50: 0.1 mM Rattus norvegicus N-(biphenyl-4-ylsulfonyl)-L-valine
0.1
-
 IC50: 0.1 mM Rattus norvegicus 3-[(biphenyl-4-ylsulfonyl)amino]-4-methylpentanoic acid