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Literature summary for 3.4.24.82 extracted from

  • Hu, Y.; Xing, L.; Thomason, J.R.; Xiang, J.; Ipek, M.; Guler, S.; Li, H.; Sabatini, J.; Chockalingam, P.; Reifenberg, E.; Sheldon, R.; Morris, E.A.; Georgiadis, K.E.; Tam, S.
    Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition (2011), Bioorg. Med. Chem. Lett., 21, 6800-6803.
    View publication on PubMed
Search for more literature for 3.4.24.82

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-([[3'-(acetylamino)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-([[3'-(aminomethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-([[3'-(hydroxymethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-([[4'-(acetylamino)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-([[4'-(carbamoyloxy)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-([[4'-(hydroxymethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-[(biphenyl-4-ylsulfonyl)amino]-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-[[(3'-carbamoylbiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-[[(3'-cyanobiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-[[(3'-hydroxybiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
-
 Homo sapiens
(2R)-2-[[(4'-hydroxybiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
-
 Homo sapiens
(2R)-3-methyl-2-[([4'-[(methylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)amino]butanoic acid
-
 Homo sapiens
3-[[(4'-[[(1R)-1-carboxy-2-methylpropyl]sulfamoyl]biphenyl-4-yl)oxy]methyl]benzoic acid
-
 Homo sapiens
N-([3'-[(acetylamino)methyl]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(2-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(2-methylpyridin-4-yl)methoxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(2-methylquinolin-4-yl)methoxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-bromobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-chlorobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-fluorobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-hydroxybenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(3-nitrobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(4-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(benzoylamino)methyl]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(benzylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(phenylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-([4'-[(phenylsulfonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
 Homo sapiens
N-[(4'-phenoxybiphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[1-[3-(trifluoromethyl)phenyl]ethoxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[2-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[2-(trifluoromethyl)pyridin-4-yl]methoxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[3-(methoxycarbonyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[3-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[4-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[6-(trifluoromethyl)pyridin-2-yl]methoxy]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[(4'-[[acetyl(methyl)amino]methyl]biphenyl-4-yl)sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(benzyloxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(cyclohexylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(naphthalen-1-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(naphthalen-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(pyridin-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(pyridin-3-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(pyridin-4-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(quinolin-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens
N-[[4'-(quinolin-4-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
aggrecan + H2O Homo sapiens aggrecanase-1 is responsible for the cleavage of aggrecan interglobular domain at the Glu373-Ala374 peptide bond fragments of aggrecan
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan + H2O aggrecanase-1 is responsible for the cleavage of aggrecan interglobular domain at the Glu373-Ala374 peptide bond Homo sapiens fragments of aggrecan
-
 ?

Synonyms

Synonyms Comment Organism
agg-1
-
 Homo sapiens
aggrecanase-1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00031
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[3-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0004
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-chlorobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.00042
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-([[4'-(carbamoyloxy)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.00042
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-bromobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0005
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(2-methylquinolin-4-yl)methoxy]biphenyl-4-yl]sulfonyl)-D-valine
0.00054
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-nitrobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.00076
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[3-(methoxycarbonyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0008
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(naphthalen-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0008
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.001
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(quinolin-4-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0014
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(naphthalen-1-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0014
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(4-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0019
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[4-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0021
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-([[3'-(hydroxymethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.0022
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[2-(trifluoromethyl)pyridin-4-yl]methoxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0024
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(2-methylpyridin-4-yl)methoxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0026
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-fluorobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0027
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[1-[3-(trifluoromethyl)phenyl]ethoxy]biphenyl-4-yl)sulfonyl]-D-valine
0.003
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-[(biphenyl-4-ylsulfonyl)amino]-3-methylbutanoic acid
0.0037
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(3-hydroxybenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0041
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-([[4'-(carbamoyloxy)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.0046
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-[[(4'-hydroxybiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
0.0047
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[6-(trifluoromethyl)pyridin-2-yl]methoxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0055
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(benzyloxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0056
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(phenylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0072
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-([[3'-(aminomethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.0082
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(phenylsulfonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.0084
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-[[(3'-carbamoylbiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
0.0085
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(pyridin-4-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.009
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-[[(3'-hydroxybiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
0.0091
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-[[2-(trifluoromethyl)benzyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
0.0106
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(quinolin-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.0132
-
 pH and temperature not specified in the publication Homo sapiens N-[(4'-phenoxybiphenyl-4-yl)sulfonyl]-D-valine
0.015
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-([[4'-(hydroxymethyl)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.015
-
 pH and temperature not specified in the publication Homo sapiens N-([4'-[(2-cyanobenzyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.02
-
 IC50 around 0.02 mM, pH and temperature not specified in the publication Homo sapiens (2R)-2-([[3'-(acetylamino)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.022
-
 IC50 around 0.022 mM, pH and temperature not specified in the publication Homo sapiens 3-[[(4'-[[(1R)-1-carboxy-2-methylpropyl]sulfamoyl]biphenyl-4-yl)oxy]methyl]benzoic acid
0.025
-
 IC50 around 0.025 mM, pH and temperature not specified in the publication Homo sapiens N-([4'-[(benzylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
0.03
-
 IC50 around 0.03 mM, pH and temperature not specified in the publication Homo sapiens N-[[4'-(pyridin-3-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.033
-
 pH and temperature not specified in the publication Homo sapiens N-[[4'-(pyridin-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.04
-
 pH and temperature not specified in the publication Homo sapiens (2R)-2-[[(3'-cyanobiphenyl-4-yl)sulfonyl]amino]-3-methylbutanoic acid
0.05
-
 IC50 around 0.05 mM, pH and temperature not specified in the publication Homo sapiens (2R)-3-methyl-2-[([4'-[(methylcarbamoyl)oxy]biphenyl-4-yl]sulfonyl)amino]butanoic acid
0.075
-
 IC50 above 0.075 mM, pH and temperature not specified in the publication Homo sapiens N-[[4'-(cyclohexylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
0.1
-
 IC50 around 0.1 mM, pH and temperature not specified in the publication Homo sapiens N-([4'-[(benzoylamino)methyl]biphenyl-4-yl]sulfonyl)-D-valine
0.1
-
 IC50 around 0.1 mM, pH and temperature not specified in the publication Homo sapiens (2R)-2-([[4'-(acetylamino)biphenyl-4-yl]sulfonyl]amino)-3-methylbutanoic acid
0.2
-
 IC50 above 0.2 mM, pH and temperature not specified in the publication Homo sapiens N-[(4'-[[acetyl(methyl)amino]methyl]biphenyl-4-yl)sulfonyl]-D-valine
0.2
-
 IC50 above 0.2 mM, pH and temperature not specified in the publication Homo sapiens N-([3'-[(acetylamino)methyl]biphenyl-4-yl]sulfonyl)-D-valine