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(1R,2R,3S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,3-dimethylcyclopropanecarboxylate
-
-
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
-
-
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[5-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-([[4'-(acetylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-([[4'-(dimethylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-([[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-([[6-(4-chlorophenyl)pyridin-3-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-2-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-3-ylethyl)amino]-2-phenylcyclopropanecarboxylate
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-4-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
-
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,3-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,4-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-imidazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-tetrazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2,5-dioxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazinan-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopiperidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2H-1,2,3-triazol-2-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(3-methoxy-2-oxopyridin-1(2H)-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(4H-1,2,4-triazol-4-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(7H-purin-7-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(9H-purin-9-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
-
(1S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,2-dimethylcyclopropanecarboxylate
-
0.001 mM, 19.6% inhibition
(1S,2R)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
-
0.0003 mM, 18% inhibition
(1S,2R)-1-([[5-(2-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
0.001 mM, 48% inhibition
(1S,2R)-1-([[5-(3-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-(propan-2-yl)cyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-cyclohexylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-([[5-(5-chloropyridin-2-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
-
-
(1S,2R)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
-
-
(1S,2R,3R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
-
(1S,2R,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
-
(1S,2S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methylcyclopropanecarboxylate
-
0.001 mM, 3.5% inhibition
(1S,2S)-2-benzyl-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)cyclopropanecarboxylate
-
0.001 mM, 25% inhibition
(1S,2S,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
-
-
(2R)-2-[4-(1,3-benzodioxol-5-yl)benzyl]-N4-hydroxy-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
nanomolar inhibitor of both ADAMTS-5
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
(2R,5R)-1-([4-[(2,4-dichlorobenzyl)oxy]phenyl]sulfonyl)-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamide
-
-
(2S,3R)-2-[(cyclopropylmethyl)amino]-N1-hydroxy-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-3-methylbutanediamide
the reduced pattern of H-bond interactions is suitable for the flexible environment of ADAMTS4 and ADAMTS5 since it enables the inhibitor to re-optimize its interaction pattern step-by-step, following the loop motion. The conformational flexibility observed for the S1' loop of ADAMTS4 and ADAMTS5 seems to be correlated to the motion of the TS-domain
(3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
-
(5E)-2-thioxo-5-([3-[3-(trifluoromethyl)phenoxy]phenyl]methylidene)-1,3-thiazolidin-4-one
-
-
(5E)-3-benzyl-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-([3-methoxy-4-[(4-methoxybenzyl)oxy]phenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-([4-[(4-chlorobenzyl)oxy]-3-methoxyphenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[(3-phenoxyphenyl)methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-(2-phenylethyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-methyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3,5-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(4-methoxyphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(4-methylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[3-(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5E)-5-[[4-(benzyloxy)-3-methoxyphenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
-
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-1-methyl-2-thioxoimidazolidin-4-one
-
-
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
-
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
-
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
-
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
potent small-molecule ADAMTS-5 inhibitor with good permeability
(E)-4-[2-(3,5-dihydroxyphenyl)ethenyl]1,2-benzenediol
-
i.e. piceatannol
(R)-2-(4'-((4-(4-fluorobenzoyl)phenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
-
-
(R)-2-(4'-((4-(cyclohexanecarbonyl)phenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
-
-
(R)-2-(4'-((4-isobutyrylphenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
-
-
(R)-3-methyl-2-(4'-((5-oxo-5,6,7,8-tetrahydronaphthalen-2-yloxy)methyl)biphenyl-4-ylsulfonamido)butanoic acid
-
-
(S)-2-dimethylamino-N-hydroxy-3,3-dimethyl-4-[(4-phenoxyphenyl)-sulfonyl]-butanamide
-
SC81956, potent inhibitor of ADAMTS-5
1-benzyl-4-((4-(4-chlorophenoxy) phenyl)-sulfonyl)-N-hydroxypiperidine-4-carboxamide
multi-MMP inhibitor
2-(4-acetylphenoxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]acetamide
-
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
-
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]acetamide
-
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
-
-
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
-
-
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
-
-
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
-
-
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]acetamide
-
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
-
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]acetamide
-
2-[4-(benzyloxy)phenyl]-2,3-dihydro-1-oxo-1H-pyrrolo[3,4-c]quinoline-4-carboxylate
-
the inhibitor is unable to discriminate between ADAMTS-5 and ADAMTS-4
2-[4-(benzyloxy)phenyl]-2,3-dihydro-N-hydroxy-1-oxo-1Hpyrrolo[3,4-c]quinoline-4-carboxamide
-
-
2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid
-
does not inhibit ADAMTS-4
2-[4-(benzyloxy)phenyl]-N-hydroxy-3-oxoisoindoline-4-carboxamide
-
does not inhibit ADAMTS-4
3-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
-
-
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
inhibits the spontaneous aggrecan degradation in IL-1-stimulated bovine cartilage, shows good selectivity over other metalloproteases; inhibits the spontaneous aggrecan degradation in IL-1-stimulated bovine cartilage, shows good selectivity over other metalloproteases
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-1H-pyrazole-1-carbonitrile
-
-
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-3-(trifluoromethyl)-1H-pyrazole-1-carbonitrile
-
-
5-([1,3-diphenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([1-methyl-5-[(2H-thiopyran-2-ylmethyl)sulfanyl]-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
40% inhibition at 0.02 mM
5-([1-methyl-5-[(4-methylphenyl)sulfanyl]-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([1-phenyl-5-[2-(tetrahydrothiophen-2-yl)ethoxy]-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(2-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(4-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(4-chlorobenzyl)sulfanyl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(4-chlorophenyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
47% inhibition at 0.02 mM
5-([5-[(4-methoxybenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
53% inhibition at 0.02 mM
5-([5-[(4-tert-butylbenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(furan-2-ylmethyl)sulfanyl]-1,3-diphenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(furan-2-ylmethyl)sulfanyl]-1-methyl-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[(furan-2-ylmethyl)sulfanyl]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
42% inhibition at 0.02 mM
5-([5-[2-(4-chlorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[2-(4-fluorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[2-(4-methoxyphenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
31% inhibition at 0.02 mM
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
-
-
5-[(4-chlorobenzyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-(2,2,2-trifluoroethyl)-1H-pyrazole-1-carbonitrile
-
-
5-[(furan-2-ylmethyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-1H-pyrazole-1-carbonitrile
-
-
5-[[1-methyl-5-(phenylsulfanyl)-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methylen]-2-thioxo-1,3-thiazolidin-4-one
-
28% inhibition at 0.02 mM
5-[[5-(4-methylpiperazin-1-yl)-1,3-diphenyl-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
-
-
5-[[5-(4-methylpiperazin-1-yl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
-
45% inhibition at 0.02 mM
5-[[5-(benzylsulfanyl)-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
-
44% inhibition at 0.02 mM
5-[[5-(benzylsulfanyl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
-
-
aggrecanase inhibitor BB-16
-
prevents aggrecan degradation in osteoarthritic cartilage
BB-16
-
(2S,5R,6S)-3-Aza-4-oxo-10-oxa-5-hexyl-2-(methylcarboxamido)-10-paracyclophane-6-N-hydroxycarboxamide
calcium pentosan polysulfate
chemically sulfated xylopyranose from beechwood. Multifaceted exosite inhibitor, protects cartilage against aggrecan degradation. Inhibitor interacts with the noncatalytic spacer domain of isoform ADAMTS-4 and the cysteine-rich domain of ADAMTS-5, blocking activity against their natural substrate aggrecan with inhibitory concentration 50 values of 10-40 nM but only weakly inhibiting hydrolysis of a nonglycosylated recombinant protein substrate. calcium pentosan polysulfate increases cartilage levels of tissue inhibitor of metalloproteinases TIMP-3, an endogenous inhibitor of ADAMTS-4 and -5
-
catechin gallate esters
from green tea Camellia sinensis, strong inhibition, independent of Zn2+, reversible
-
doxycycline
-
dose-dependently inhibits the activity of rhADAMTS4 in vitro
interleukin-1beta
lower mRNA level of aggrecan
-
minocycline
-
dose-dependently inhibits the activity of rhADAMTS4 in vitro
N-benzyl-N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-D-phenylalanine
30% inhibition at 0.01 mM
N-hydroxy-4-(4-(4-(trifluoromethyl)-phenoxy)phenylsulfonyl)-tetrahydro-2H-pyran-4-carboxamide
nanomolar inhibitor of both ADAMTS-5
N-hydroxy-4-([4-[4-(trifluoromethyl)phenoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
-
N-terminal domain of tissue inhibitor of metalloproteinases-3
-
all isoforms of ADAMTS-5 are effectively inhibited. Inhibited more strongly by N-terminal domain of tissue inhibitor of metalloproteinases-3 than by full-length tissue inhibitor of metalloproteinases-3
-
N-terminal inhibitory domain of tissue inhibitor of metalloproteinases 3
N-terminal mutants of N-TIMP-3 (tissue inhibitor of metalloproteinases 3) that have lost their matrix metalloproteinaseP-inhibitory activities (N-TIMP-3(T2G) and [-1A]N-TIMP-3), retain their ability to inhibit ADAMTS-4 and ADAMTS-5. The [-2A]N-TIMP-3 mutant also retains strong affinity with ADAMTS-5, but has a lower affinity for ADAMTS-4 and ADAM17
-
N-[(1R)-1-(dihydroxymethyl)-2-methylpropyl]-4'-{[4-(2-methylpropanoyl)phenoxy]methyl}biphenyl-4-sulfonamide
-
-
N-[(2-chlorophenyl)(8-hydroxy-5-methylquinolin-7-yl)methyl]-2-phenoxyacetamide
-
N-[(2-chlorophenyl)(8-hydroxy-5-nitroquinolin-7-yl)methyl]-2-phenoxyacetamide
-
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-D-phenylalanine
-
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-(cyclohexylmethyl)-D-phenylalanine
22% inhibition at 0.01 mM
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-(cyclopropylmethyl)-D-phenylalanine
46% inhibition at 0.01 mM
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-methyl-D-phenylalanine
-
N-[(5-bromo-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-bromo-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-cyanophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-fluorophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-methylphenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-nitrophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-(pyridin-3-yloxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methyl-N2-phenylglycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-chlorophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methoxyphenoxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methylphenoxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(pyridin-3-yloxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-cyanophenyl)glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methyl-N2-phenylglycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-[3-(dimethylamino)phenyl]glycinamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-nitrophenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-chlorophenoxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-methylphenoxy)acetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
-
N-[(5-chloro-8-hydroxyquinolin-7-yl)[2-(trifluoromethyl)phenyl]methyl]-2-phenoxyacetamide
-
N-[(5-fluoro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
-
N-[(8-hydroxy-5-methylquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
-
N-[(8-hydroxy-5-nitroquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
-
N-[(8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
-
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
-
inhibitor has excellent selectivity over other zinc metalloproteases such as TACE, MMP2, MMP3, MMP13, and MMP14
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
-
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
-
N2-(biphenyl-4-ylcarbonyl)-N-(2-phenylpropan-2-yl)-L-alpha-glutamine
-
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methylglycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]glycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methylglycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]glycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methylglycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methylglycinamide
-
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
-
N2-[4-(acetylamino)phenyl]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
-
NaCl
-
the activity is very low at or below 50 mM NaCl or above 500 mM NaCl
tetracycline
-
dose-dependently inhibits the activity of rhADAMTS4 in vitro
tissue inhibitor of matrix metalloproteinases-3
-
TIMP-3
-
tissue inhibitor of metalloproteinases-3
-
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
-
-
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
-
-
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
-
-
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
-
-
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
-
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
the reduced pattern of H-bond interactions is suitable for the flexible environment of ADAMTS4 and ADAMTS5 since it enables the inhibitor to re-optimize its interaction pattern step-by-step, following the loop motion. The conformational flexibility observed for the S1' loop of ADAMTS4 and ADAMTS5 seems to be correlated to the motion of the TS-domain
alpha2-Macroglobulin
-
-
-
alpha2-Macroglobulin
-
after 10 min 100% and 68% inhibition at concentrations of 2.5 and 7.5 nM, respectively, similar results when using 25 and 75 nM
-
alpha2-Macroglobulin
-
-
-
alpha2-Macroglobulin
-
-
-
heparin
-
TIMP-3
-
potent inhibitor
-
TIMP-3
-
recombinant human inhibitor protein from Escherichia coli, i.e. tissue inhibitor of metalloproteinases, strong inhibitor with regulatory function
-
TIMP-3
-
potent inhibitor
-
TIMP-3
-
potent inhibitor
-
tissue inhibitor of metalloproteinases-3
-
-
-
tissue inhibitor of metalloproteinases-3
-
all isoforms of ADAMTS-5 are effectively inhibited. Inhibited more strongly by N-terminal domain of tissue inhibitor of metalloproteinases-3 than by full-length tissue inhibitor of metalloproteinases-3
-
additional information
-
TIMP-1, TIMP-2 and TIMP-4 do not inhibit ADAMTS-5
-
additional information
-
no inhibition by matrix metalloprotease inhibitor XS309
-
additional information
-
[3S-[3R*,2-[2R*,2-(R*,S*)]-hexahydro-2-(2-[2-(hydroxyamino)-1-methyl-2-oxyethyl])-4-methyl-1-oxypentyl]-N-methyl]-3-pyridazinecarboxamide, i.e.XS309 is inactive at less than 0.01 mM in blocking ADAMTS-5
-
additional information
-
TIMP-1, TIMP-2 and TIMP-4 do not inhibit ADAMTS-5
-
additional information
-
not inhibited by N-TIMP-1 or TIMP-2; the general proteolytic activitiy of ADAMTS-5 as measured with carboxymethylated transferrin is unaffected by concentrations up to 1 M NaCl
-
additional information
-
substrate specificity of ADAMTS-5 against recombinant aggrecan, aggrecan mutants S377Q and S377T lead to aggrecan cleavage inhibition
-
additional information
-
lower expression level in majority of primary tumors
-
additional information
-
design of ADAMTS-5 inhibitors
-
additional information
design and development for potent and selective inhibitors of ADAMTS-4 and ADAMTS-5
-
additional information
-
TIMP-1, TIMP-2 and TIMP-4 do not inhibit ADAMTS-5
-
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0.0008
(1R,2R,3S)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2,3-dimethylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000073
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[5-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0045
(1R,2S)-1-([[4'-(acetylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0066
(1R,2S)-1-([[4'-(dimethylamino)biphenyl-4-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00088
(1R,2S)-1-([[4-(4-chlorophenyl)-3,6-dihydropyridin-1(2H)-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0011
(1R,2S)-1-([[6-(4-chlorophenyl)pyridin-3-yl]sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino)-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00082
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-2-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00029
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-3-ylethyl)amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00075
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl](2-pyridin-4-ylethyl)amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00027
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,3-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00018
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-1,2,4-triazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-imidazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00027
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(1H-tetrazol-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0001
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2,5-dioxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00018
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazinan-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00022
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00021
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopiperidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.0002
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2-oxopyrrolidin-1-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00026
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(2H-1,2,3-triazol-2-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00078
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(3-methoxy-2-oxopyridin-1(2H)-yl)ethyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
0.00019
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(4H-1,2,4-triazol-4-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.000071
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(7H-purin-7-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00017
(1R,2S)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl][2-(9H-purin-9-yl)ethyl]amino]-2-phenylcyclopropanecarboxylic acid
Homo sapiens
-
0.00021
(1S,2R)-1-([(4'-chlorobiphenyl-4-yl)sulfonyl][2-[4-(methoxycarbonyl)-1H-imidazol-1-yl]ethyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000094
(1S,2R)-1-([[5-(3-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00077
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-(propan-2-yl)cyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00036
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-cyclohexylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00008
(1S,2R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00006
(1S,2R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
(1S,2R)-1-([[5-(5-chloropyridin-2-yl)thiophen-2-yl]sulfonyl]amino)-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000084
(1S,2R)-1-[[(4'-chlorobiphenyl-4-yl)sulfonyl]amino]-2-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0000074
(1S,2R,3R)-1-([[5-(4-chloro-1H-pyrazol-1-yl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
(1S,2R,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
(1S,2S,3R)-1-([[5-(4-chlorophenyl)thiophen-2-yl]sulfonyl]amino)-2-methyl-3-phenylcyclopropanecarboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000129
(2R)-2-[4-(1,3-benzodioxol-5-yl)benzyl]-N4-hydroxy-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
Homo sapiens
pH and temperature not specified in the publication
0.000093
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
Homo sapiens
pH 7.5, 37°C
0.0000014
(2R,5R)-1-([4-[(2,4-dichlorobenzyl)oxy]phenyl]sulfonyl)-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamide
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.000017
(3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
Homo sapiens
pH 7.5, 37°C
0.0053
(5E)-2-thioxo-5-([3-[3-(trifluoromethyl)phenoxy]phenyl]methylidene)-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5E)-3-benzyl-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0116
(5E)-5-([3-methoxy-4-[(4-methoxybenzyl)oxy]phenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0035
(5E)-5-([4-[(4-chlorobenzyl)oxy]-3-methoxyphenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[(3-phenoxyphenyl)methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.0018
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-(2-phenylethyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-methyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.067
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0014
(5E)-5-[[3,5-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0032
(5E)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0025
(5E)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0049 - 0.022
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0162
(5E)-5-[[3-(4-methoxyphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0148
(5E)-5-[[3-(4-methylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0017
(5E)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0201
(5E)-5-[[3-(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[[4-(benzyloxy)-3-methoxyphenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.01
(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0092
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.022
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-1-methyl-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.067
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.0068
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.067
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
Homo sapiens
-
IC50 above 0.067 mM
0.00017 - 0.021
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
0.0026
(R)-2-(4'-((4-(cyclohexanecarbonyl)phenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
Mus musculus
-
-
0.0084
(R)-2-(4'-((4-isobutyrylphenoxy)methyl)biphenyl-4-ylsulfonamido)-3-methylbutanoic acid
Mus musculus
-
-
0.0066
(R)-3-methyl-2-(4'-((5-oxo-5,6,7,8-tetrahydronaphthalen-2-yloxy)methyl)biphenyl-4-ylsulfonamido)butanoic acid
Mus musculus
-
-
0.00042
1-benzyl-4-((4-(4-chlorophenoxy) phenyl)-sulfonyl)-N-hydroxypiperidine-4-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00233
2-(4-acetylphenoxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]acetamide
Homo sapiens
-
0.00083
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
Homo sapiens
-
0.0007
2-(benzyloxy)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]acetamide
Homo sapiens
-
0.0011
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
Homo sapiens
-
-
0.0013
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
Homo sapiens
-
-
0.0018
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
Homo sapiens
-
-
0.0016
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
Homo sapiens
-
-
0.00234
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]acetamide
Homo sapiens
-
0.00133
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]acetamide
Homo sapiens
-
0.00339
2-[4-(acetylamino)phenoxy]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]acetamide
Homo sapiens
-
0.012
2-[4-(benzyloxy)phenyl]-2,3-dihydro-1-oxo-1H-pyrrolo[3,4-c]quinoline-4-carboxylate
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.00095
2-[4-(benzyloxy)phenyl]-2,3-dihydro-N-hydroxy-1-oxo-1Hpyrrolo[3,4-c]quinoline-4-carboxamide
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.0053
3-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
Homo sapiens
-
-
0.00023 - 0.023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
0.008
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0117
4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-5-(2-pyrimidin-1(6H)-ylpiperazin-1-yl)-3-(trifluoromethyl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0037
5-([1,3-diphenyl-5-[(thiophen-2-ylmethyl)sulfanyl]-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0083
5-([1-methyl-5-[(4-methylphenyl)sulfanyl]-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0091
5-([1-phenyl-5-[2-(tetrahydrothiophen-2-yl)ethoxy]-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0232
5-([5-[(2-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0011
5-([5-[(4-chlorobenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0025
5-([5-[(4-chlorobenzyl)sulfanyl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0022
5-([5-[(4-tert-butylbenzyl)sulfanyl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0067
5-([5-[(furan-2-ylmethyl)sulfanyl]-1,3-diphenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0141
5-([5-[(furan-2-ylmethyl)sulfanyl]-1-methyl-3-phenyl-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0042
5-([5-[2-(4-chlorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0071
5-([5-[2-(4-fluorophenyl)ethoxy]-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.009
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-methyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0021
5-([5-[4-(4-chlorophenyl)piperazin-1-yl]-1-phenyl-3-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl]methyl)-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0042
5-[(4-chlorobenzyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-(2,2,2-trifluoroethyl)-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0046
5-[(furan-2-ylmethyl)sulfanyl]-4-[(4-oxo-2-thioxo-1,3-thiazolidin-5-yl)methyl]-3-phenyl-1H-pyrazole-1-carbonitrile
Homo sapiens
-
-
0.0046
5-[[5-(4-methylpiperazin-1-yl)-1,3-diphenyl-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0169
5-[[5-(benzylsulfanyl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.0707
doxycycline
Homo sapiens
-
pH and temperature not specified in the publication
0.000106
marimastat
Homo sapiens
pH 7.5, 37°C
0.111
minocycline
Homo sapiens
-
pH and temperature not specified in the publication
0.129
N-hydroxy-4-(4-(4-(trifluoromethyl)-phenoxy)phenylsulfonyl)-tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00029
N-hydroxy-4-([4-[4-(trifluoromethyl)phenoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5
0.00242
N-[(2-chlorophenyl)(8-hydroxy-5-methylquinolin-7-yl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00094
N-[(2-chlorophenyl)(8-hydroxy-5-nitroquinolin-7-yl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.002
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-D-phenylalanine
Homo sapiens
-
0.008
N-[(4'-chlorobiphenyl-4-yl)sulfonyl]-N-methyl-D-phenylalanine
Homo sapiens
-
0.00083
N-[(5-bromo-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00062
N-[(5-bromo-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00035
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00172
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00148
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00099
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00232
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-cyanophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00122
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-fluorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00185
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-methylphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00121
N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00062
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00337
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00143
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00125
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00166
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-(pyridin-3-yloxy)acetamide
Homo sapiens
-
0.00049
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00119
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00056
N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12. Good balance of potent ADAMTS-5 inhibition, moderate CYP3A4 inhibition and good rat liver microsome stability
0.00083
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-chlorophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00094
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methoxyphenoxy)acetamide
Homo sapiens
sub-micromol ADAMTS-5 potency and good selectivity over the related metalloproteases ADAMTS-4 (aggrecanase-1), MMP-13, and MMP-12
0.00077
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(4-methylphenoxy)acetamide
Homo sapiens
-
0.00298
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-(pyridin-3-yloxy)acetamide
Homo sapiens
-
0.00135
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00167
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methoxyphenyl)methyl]-2-[3-(dimethylamino)phenoxy]acetamide
Homo sapiens
-
0.00076
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00158
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-chloro-3-methylphenyl)glycinamide
Homo sapiens
-
0.00101
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-(4-cyanophenyl)glycinamide
Homo sapiens
-
0.00078
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methyl-N2-phenylglycinamide
Homo sapiens
-
0.00193
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-[3-(dimethylamino)phenyl]glycinamide
Homo sapiens
-
0.00046
N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00102
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-chlorophenoxy)acetamide
Homo sapiens
-
0.0019
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-(4-methylphenoxy)acetamide
Homo sapiens
-
0.00078
N-[(5-chloro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00083
N-[(5-chloro-8-hydroxyquinolin-7-yl)[2-(trifluoromethyl)phenyl]methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00484
N-[(5-fluoro-8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00132
N-[(8-hydroxy-5-methylquinolin-7-yl)(3-nitrophenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00135
N-[(8-hydroxy-5-nitroquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.00228
N-[(8-hydroxyquinolin-7-yl)(phenyl)methyl]-2-phenoxyacetamide
Homo sapiens
-
0.000004 - 0.000035
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
0.00107
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
Homo sapiens
-
0.00113
N2-(4-acetylphenyl)-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
Homo sapiens
-
0.0011
N2-(biphenyl-4-ylcarbonyl)-N-(2-phenylpropan-2-yl)-L-alpha-glutamine
Homo sapiens
-
37°C, pH and temperature not specified in the publication
0.00131
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00189
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(2-chlorophenyl)methyl]glycinamide
Homo sapiens
-
0.00144
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00172
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-fluorophenyl)methyl]glycinamide
Homo sapiens
-
0.00082
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00128
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]-N2-methylglycinamide
Homo sapiens
-
0.00183
N2-benzyl-N-[(5-chloro-8-hydroxyquinolin-7-yl)(4-methylphenyl)methyl]glycinamide
Homo sapiens
-
0.00277
N2-[4-(acetylamino)phenyl]-N-[(5-chloro-8-hydroxyquinolin-7-yl)(3-nitrophenyl)methyl]glycinamide
Homo sapiens
-
0.899
tetracycline
Homo sapiens
-
pH and temperature not specified in the publication
0.0000038
TIMP-3
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5
-
0.0009
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
Homo sapiens
-
-
0.0067
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
Homo sapiens
-
-
0.0013
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
Homo sapiens
-
-
0.0111
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
Homo sapiens
-
-
additional information
2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid
0.0049
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
-
0.022
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
Homo sapiens
-
IC50 above 0.022 mM
0.00017
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
Homo sapiens
pH 7.5, 37°C
0.021
(E)-2-((1H-benzo[d]imidazol-2-yl)methylene)-5-propylthiazolidin-4-one
Homo sapiens
pH 7.5, 37°C
0.00023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.023
3-[2-[(Z)-(4-oxo-1,3-thiazolidin-2-ylidene)methyl]-4-(pyridin-2-yl)-1,3-thiazol-5-yl]propanoic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000004
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C
0.000035
N-[[(4S)-4-(1-methylimidazol-2-yl)-2,5-dioxo-imidazolidin-4-yl]methyl]-5-(trifluoromethyl)benzofuran-2-carboxamide
Homo sapiens
-
pH 7.5, 22°C, presence of 50% rat plasma
additional information
2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid
Homo sapiens
-
IC25-value: 0.0075 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50%
additional information
2-[4-(benzyloxy)phenyl]-N-hydroxy-3-oxoisoindoline-4-carboxamide
Homo sapiens
-
IC25-value: 0.0025 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50%
additional information
additional information
Homo sapiens
inhibitors which show strong potency of IC50 with excellent selectivity over MMP-1 and TACE
-
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Boeckmann, B.; Bairoch, A.; Apweiler, R.; Blatter, M.C.; Estreicher, A.; Gasteiger, E.; Martin M.J.; Michoud, K.; O'Donovan, C.; Phan, I.; Pilbout, S.; Schneider, M.
The SWISS-PROT protein knowledgebase and its supplement TrEMBL
Nucleic Acids Res.
31
365-370
2003
Mus musculus (Q9R001), Bos taurus (Q9TT92), Homo sapiens (Q9UNA0)
brenda
Vankemmelbeke, M.N.; Holen, I.; Wilson, A.G.; Ilic, M.Z.; Handley, C.J.; Kelner, G.S.; Clark, M.; Liu, C.; Maki, R.A.; Burnett, D.; Buttle, D.J.
Expression and activity of ADAMTS-5 in synovium
Eur. J. Biochem.
268
1259-1268
2001
Homo sapiens, Bos taurus (Q9TT92), Bos taurus
brenda
Vankemmelbeke, M.N.; Jones, G.C.; Fowles, C.; Ilic, M.Z.; Handley, C.J.; Day, A.J.; Knight, C.G.; Mort, J.S.; Buttle, D.J.
Selective inhibition of ADAMTS-1, -4 and -5 by catechin gallate esters
Eur. J. Biochem.
270
2394-2403
2003
Homo sapiens (Q9UNA0)
brenda
Tang, B.L.
ADAMTS: a novel family of extracellular matrix proteases
Int. J. Biochem. Cell Biol.
33
33-44
2001
Bos taurus
brenda
Kashiwagi, M.; Tortorella, M.; Nagase, H.; Brew, K.
TIMP-3 is a potent inhibitor of aggrecanase 1 (ADAM-TS4) and aggrecanase 2 (ADAM-TS5)
J. Biol. Chem.
276
12501-12504
2001
Homo sapiens
brenda
Malfait, A.M.; Liu, R.Q.; Ijiri, K.; Komiya, S.; Tortorella, M.D.
Inhibition of ADAM-TS4 and ADAM-TS5 prevents aggrecan degradation in osteoarthritic cartilage
J. Biol. Chem.
277
22201-22208
2002
Homo sapiens
brenda
Nakada, M.; Miyamori, H.; Kita, D.; Takahashi, T.; Yamashita, J.; Sato, H.; Miura, R.; Yamaguchi, Y.; Okada, Y.
Human glioblastomas overexpress ADAMTS-5 that degrades brevican
Acta Neuropathol.
110
239-246
2005
Homo sapiens (Q9UHI8), Homo sapiens
brenda
Zeng, W.; Corcoran, C.; Collins-Racie, L.A.; LaVallie, E.R.; Morris, E.A.; Flannery, C.R.
Glycosaminoglycan-binding properties and aggrecanase activities of truncated ADAMTSs: Comparative analyses with ADAMTS-5, -9, -16 and -18
Biochim. Biophys. Acta
1760
517-524
2006
Homo sapiens (Q9UNA0), Homo sapiens
brenda
Miguel, R.F.; Pollak, A.; Lubec, G.
Metalloproteinase ADAMTS-1 but not ADAMTS-5 is manifold overexpressed in neurodegenerative disorders as Down syndrome, Alzheimers and Picks disease
Brain Res. Mol. Brain Res.
133
1-5
2005
Homo sapiens (Q9UHI8), Homo sapiens
brenda
Held-Feindt, J.; Paredes, E.B.; Bloemer, U.; Seidenbecher, C.; Stark, A.M.; Mehdorn, H.M.; Mentlein, R.
Matrix-degrading proteases ADAMTS4 and ADAMTS5 (disintegrins and metalloproteinases with thrombospondin motifs 4 and 5) are expressed in human glioblastomas
Int. J. Cancer
118
55-61
2005
Homo sapiens
brenda
Tortorella, M.D.; Arner, E.C.; Hills, R.; Easton, A.; Korte-Sarfaty, J.; Fok, K.; Wittwer, A.J.; Liu, R.Q.; Malfait, A.M.
Alpha2-macroglobulin is a novel substrate for ADAMTS-4 and ADAMTS-5 and represents an endogenous inhibitor of these enzymes
J. Biol. Chem.
279
17554-17561
2004
Homo sapiens
brenda
Stanton, H.; Rogerson, F.M.; East, C.J.; Golub, S.B.; Lawlor, K.E.; Meeker, C.T.; Little, C.B.; Last, K.; Farmer, P.J.; Campbell, I.K.; Fourie, A.M.; Fosang, A.J.
ADAMTS5 is the major aggrecanase in mouse cartilage in vivo and in vitro
Nature
434
648-652
2005
Mus musculus
brenda
Song, R.H.; Tortorella, M.D.; Malfait, A.M.; Alston, J.T.; Yang, Z.; Arner, E.C.; Griggs, D.W.
Aggrecan degradation in human articular cartilage explants is mediated by both ADAMTS-4 and ADAMTS-5
Arthritis Rheum.
56
575-585
2007
Homo sapiens
brenda
Sharghi-Namini, S.; Fan, H.; Sulochana, K.N.; Potturi, P.; Xiang, W.; Chong, Y.S.; Wang, Z.; Yang, H.; Ge, R.
The first but not the second thrombospondin type 1 repeat of ADAMTS5 functions as an angiogenesis inhibitor
Biochem. Biophys. Res. Commun.
371
215-219
2008
Homo sapiens
brenda
Bursavich, M.G.; Gilbert, A.M.; Lombardi, S.; Georgiadis, K.E.; Reifenberg, E.; Flannery, C.R.; Morris, E.A.
Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2)
Bioorg. Med. Chem. Lett.
17
1185-1188
2007
Homo sapiens
brenda
Gilbert, A.M.; Bursavich, M.G.; Lombardi, S.; Georgiadis, K.E.; Reifenberg, E.; Flannery, C.R.; Morris, E.A.
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5
Bioorg. Med. Chem. Lett.
17
1189-1192
2007
Homo sapiens
brenda
Bondeson, J.; Wainwright, S.; Hughes, C.; Caterson, B.
The regulation of the ADAMTS4 and ADAMTS5 aggrecanases in osteoarthritis: a review
Clin. Exp. Rheumatol.
26
139-145
2008
Homo sapiens, Mus musculus
brenda
Fosang, A.J.; Rogerson, F.M.; East, C.J.; Stanton, H.
ADAMTS-5: the story so far
Eur. Cell Mater.
15
11-26
2008
Bos taurus, Homo sapiens, Mus musculus
brenda
Gendron, C.; Kashiwagi, M.; Lim, N.H.; Enghild, J.J.; Thogersen, I.B.; Hughes, C.; Caterson, B.; Nagase, H.
Proteolytic activities of human ADAMTS-5: comparative studies with ADAMTS-4
J. Biol. Chem.
282
18294-18306
2007
Homo sapiens
brenda
Ilic, M.Z.; East, C.J.; Rogerson, F.M.; Fosang, A.J.; Handley, C.J.
Distinguishing aggrecan loss from aggrecan proteolysis in ADAMTS-4 and ADAMTS-5 single and double deficient mice
J. Biol. Chem.
282
37420-37428
2007
Mus musculus
brenda
Shieh, H.S.; Mathis, K.J.; Williams, J.M.; Hills, R.L.; Wiese, J.F.; Benson, T.E.; Kiefer, J.R.; Marino, M.H.; Carroll, J.N.; Leone, J.W.; Malfait, A.M.; Arner, E.C.; Tortorella, M.D.; Tomasselli, A.
High resolution crystal structure of the catalytic domain of ADAMTS-5 (aggrecanase-2)
J. Biol. Chem.
283
1501-1507
2008
Homo sapiens
brenda
Fushimi, K.; Troeberg, L.; Nakamura, H.; Lim, N.H.; Nagase, H.
Functional differences of the catalytic and non-catalytic domains in human ADAMTS-4 and ADAMTS-5 in aggrecanolytic activity
J. Biol. Chem.
283
6706-6716
2008
Homo sapiens
brenda
Mosyak, L.; Georgiadis, K.; Shane, T.; Svenson, K.; Hebert, T.; McDonagh, T.; Mackie, S.; Olland, S.; Lin, L.; Zhong, X.; Kriz, R.; Reifenberg, E.L.; Collins-Racie, L.A.; Corcoran, C.; Freeman, B.; Zollner, R.; Marvell, T.; Vera, M.; Sum, P.E.; Lavallie, E.R.; Stahl, M.; Somers, W.
Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5
Protein Sci.
17
16-21
2008
Homo sapiens
brenda
Gilbert, A.M.; Bursavich, M.G.; Lombardi, S.; Georgiadis, K.E.; Reifenberg, E.; Flannery, C.R.; Morris, E.A.
N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2)
Bioorg. Med. Chem. Lett.
18
6454-6457
2008
Homo sapiens (Q9UNA0)
brenda
Shiozaki, M.; Maeda, K.; Miura, T.; Ogoshi, Y.; Haas, J.; Fryer, A.M.; Laird, E.R.; Littmann, N.M.; Andrews, S.W.; Josey, J.A.; Mimura, T.; Shinozaki, Y.; Yoshiuchi, H.; Inaba, T.
Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (aggrecanase-2) inhibitors
Bioorg. Med. Chem. Lett.
19
1575-1580
2009
Homo sapiens (Q9UNA0)
brenda
McCulloch, D.R.; Goff, C.L.; Bhatt, S.; Dixon, L.J.; Sandy, J.D.; Apte, S.S.
Adamts5, the gene encoding a proteoglycan-degrading metalloprotease, is expressed by specific cell lineages during mouse embryonic development and in adult tissues
Gene Expr. Patterns
9
314-323
2009
Mus musculus (Q9R001), Mus musculus
brenda
Wang, Z.H.; Yang, Z.Q.; He, X.J.; Wang, L.; Li, L.X.; Tu, J.B.
Effects of RNAi-mediated inhibition of aggrecanase-1 and aggrecanase-2 on rat costochondral chondrocytes in vitro
Acta Pharmacol. Sin.
29
1215-1226
2008
Rattus norvegicus (Q6TY19)
brenda
Rogerson, F.M.; Stanton, H.; East, C.J.; Golub, S.B.; Tutolo, L.; Farmer, P.J.; Fosang, A.J.
Evidence of a novel aggrecan-degrading activity in cartilage: Studies of mice deficient in both ADAMTS-4 and ADAMTS-5
Arthritis Rheum.
58
1664-1673
2008
Mus musculus (Q9R001), Mus musculus
brenda
Pockert, A.J.; Richardson, S.M.; Le Maitre, C.L.; Lyon, M.; Deakin, J.A.; Buttle, D.J.; Freemont, A.J.; Hoyland, J.A.
Modified expression of the ADAMTS enzymes and tissue inhibitor of metalloproteinases 3 during human intervertebral disc degeneration
Arthritis Rheum.
60
482-491
2009
Homo sapiens
brenda
Miwa, H.E.; Gerken, T.A.; Huynh, T.D.; Duesler, L.R.; Cotter, M.; Hering, T.M.
Conserved sequence in the aggrecan interglobular domain modulates cleavage by ADAMTS-4 and ADAMTS-5
Biochim. Biophys. Acta
1790
161-172
2009
Homo sapiens
brenda
Hopper, D.W.; Vera, M.D.; How, D.; Sabatini, J.; Xiang, J.S.; Ipek, M.; Thomason, J.; Hu, Y.; Feyfant, E.; Wang, Q.; Georgiadis, K.E.; Reifenberg, E.; Sheldon, R.T.; Keohan, C.C.; Majumdar, M.K.; Morris, E.A.; Skotnicki, J.; Sum, P.E.
Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors
Bioorg. Med. Chem. Lett.
19
2487-2491
2009
Mus musculus
brenda
Hamel, M.G.; Ajmo, J.M.; Leonardo, C.C.; Zuo, F.; Sandy, J.D.; Gottschall, P.E.
Multimodal signaling by the ADAMTSs (a disintegrin and metalloproteinase with thrombospondin motifs) promotes neurite extension
Exp. Neurol.
210
428-440
2008
Homo sapiens
brenda
Troeberg, L.; Fushimi, K.; Khokha, R.; Emonard, H.; Ghosh, P.; Nagase, H.
Calcium pentosan polysulfate is a multifaceted exosite inhibitor of aggrecanases
FASEB J.
22
3515-3524
2008
Homo sapiens (Q9UNA0)
brenda
Takizawa, M.; Yatabe, T.; Okada, A.; Chijiiwa, M.; Mochizuki, S.; Ghosh, P.; Okada, Y.
Calcium pentosan polysulfate directly inhibits enzymatic activity of ADAMTS4 (aggrecanase-1) in osteoarthritic chondrocytes
FEBS Lett.
582
2945-2949
2008
Homo sapiens
brenda
Demircan, K.; Gunduz, E.; Gunduz, M.; Beder, L.B.; Hirohata, S.; Nagatsuka, H.; Cengiz, B.; Cilek, M.Z.; Yamanaka, N.; Shimizu, K.; Ninomiya, Y.
Increased mRNA expression of ADAMTS metalloproteinases in metastatic foci of head and neck cancer
Head Neck
10
793-801
2009
Homo sapiens
brenda
Lee, J.H.; Fitzgerald, J.B.; DiMicco, M.A.; Cheng, D.M.; Flannery, C.R.; Sandy, J.D.; Plaas, A.H.; Grodzinsky, A.J.
Co-culture of mechanically injured cartilage with joint capsule tissue alters chondrocyte expression patterns and increases ADAMTS5 production
Arch. Biochem. Biophys.
489
118-126
2009
Bos taurus
brenda
Seki, S.; Asanuma-Abe, Y.; Masuda, K.; Kawaguchi, Y.; Asanuma, K.; Muehleman, C.; Iwai, A.; Kimura, T.
Effect of small interference RNA (siRNA) for ADAMTS5 on intervertebral disc degeneration in the rabbit anular needle-puncture model
Arthritis Res. Ther.
11
R166
2009
Oryctolagus cuniculus
brenda
Chia, S.L.; Sawaji, Y.; Burleigh, A.; McLean, C.; Inglis, J.; Saklatvala, J.; Vincent, T.
Fibroblast growth factor 2 is an intrinsic chondroprotective agent that suppresses ADAMTS-5 and delays cartilage degradation in murine osteoarthritis
Arthritis Rheum.
60
2019-2027
2009
Mus musculus
brenda
Willems, S.H.; Tape, C.J.; Stanley, P.L.; Taylor, N.A.; Mills, I.G.; Neal, D.E.; McCafferty, J.; Murphy, G.
Thiol isomerases negatively regulate the cellular shedding activity of ADAM17
Biochem. J.
428
439-450
2010
Homo sapiens
brenda
Lim, N.H.; Kashiwagi, M.; Visse, R.; Jones, J.; Enghild, J.J.; Brew, K.; Nagase, H.
Reactive-site mutants of N-TIMP-3 that selectively inhibit ADAMTS-4 and ADAMTS-5: biological and structural implications
Biochem. J.
431
113-122
2010
Homo sapiens (Q9UNA0), Homo sapiens
brenda
Shiozaki, M.; Imai, H.; Maeda, K.; Miura, T.; Yasue, K.; Suma, A.; Yokota, M.; Ogoshi, Y.; Haas, J.; Fryer, A.M.; Laird, E.R.; Littmann, N.M.; Andrews, S.W.; Josey, J.A.; Mimura, T.; Shinozaki, Y.; Yoshiuchi, H.; Inaba, T.
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (aggrecanase-2) inhibitors
Bioorg. Med. Chem. Lett.
19
6213-6217
2009
Homo sapiens
brenda
Cudic, M.; Burstein, G.D.; Fields, G.B.; Lauer-Fields, J.
Analysis of flavonoid-based pharmacophores that inhibit aggrecanases (ADAMTS-4 and ADAMTS-5) and matrix metalloproteinases through the use of topologically constrained peptide substrates
Chem. Biol. Drug Des.
74
473-482
2009
Sus scrofa
brenda
Cappelli, A.; Nannicini, C.; Valenti, S.; Giuliani, G.; Anzini, M.; Mennuni, L.; Giordani, A.; Caselli, G.; Stasi, L.P.; Makovec, F.; Giorgi, G.; Vomero, S.
Design, synthesis, and preliminary biological evaluation of pyrrolo[3,4-c]quinolin-1-one and oxoisoindoline derivatives as aggrecanase inhibitors
ChemMedChem
5
739-748
2010
Homo sapiens
brenda
Longpre, J.; McCulloch, D.; Koo, B.; Alexander, J.; Apte, S.; Leduc, R.
Characterization of proADAMTS5 processing by proprotein convertases
Int. J. Biochem. Cell Biol.
41
1116-1126
2009
Homo sapiens
brenda
Tortorella, M.D.; Tomasselli, A.G.; Mathis, K.J.; Schnute, M.E.; Woodard, S.S.; Munie, G.; Williams, J.M.; Caspers, N.; Wittwer, A.J.; Malfait, A.M.; Shieh, H.S.
Structural and inhibition analysis reveals the mechanism of selectivity of a series of aggrecanase inhibitors
J. Biol. Chem.
284
24185-24191
2009
Homo sapiens (Q9UNA0)
brenda
Steinmeyer, J.; Kordelle, J.; Stuerz, H.
In vitro inhibition of aggrecanase activity by tetracyclines and proteoglycan loss from osteoarthritic human articular cartilage
J. Orthop. Res.
28
828-833
2010
Homo sapiens
brenda
Tsuzaka, K.; Itami, Y.; Takeuchi, T.; Shinozaki, N.; Morishita, T.
ADAMTS5 is a biomarker for prediction of response to infliximab in patients with rheumatoid arthritis
J. Rheumatol.
37
1454-1460
2010
Homo sapiens
brenda
Troeberg, L.; Fushimi, K.; Scilabra, S.D.; Nakamura, H.; Dive, V.; Thogersen, I.B.; Enghild, J.J.; Nagase, H.
The C-terminal domains of ADAMTS-4 and ADAMTS-5 promote association with N-TIMP-3
Matrix Biol.
28
463-469
2009
Homo sapiens
brenda
Echtermeyer, F.; Bertrand, J.; Dreier, R.; Meinecke, I.; Neugebauer, K.; Fuerst, M.; Lee, Y.J.; Song, Y.W.; Herzog, C.; Theilmeier, G.; Pap, T.
Syndecan-4 regulates ADAMTS-5 activation and cartilage breakdown in osteoarthritis
Nat. Med.
15
1072-1076
2009
Homo sapiens
brenda
Botter, S.; Glasson, S.; Hopkins, B.; Clockaerts, S.; Weinans, H.; van Leeuwen, J.; van Osch, G.
ADAMTS5-/- mice have less subchondral bone changes after induction of osteoarthritis through surgical instability: implications for a link between cartilage and subchondral bone changes
Osteoarthritis Cartilage
17
636-645
2009
Mus musculus
brenda
Malfait, A.M.; Ritchie, J.; Gil, A.S.; Austin, J.S.; Hartke, J.; Qin, W.; Tortorella, M.D.; Mogil, J.S.
ADAMTS-5 deficient mice do not develop mechanical allodynia associated with osteoarthritis following medial meniscal destabilization
Osteoarthritis Cartilage
18
572-580
2010
Mus musculus
brenda
Durigova, M.; Troeberg, L.; Nagase, H.; Roughley, P.J.; Mort, J.S.
Involvement of ADAMTS5 and hyaluronidase in aggrecan degradation and release from OSM-stimulated cartilage
Eur. Cell Mater.
21
31-45
2011
Homo sapiens
brenda
Hattori, N.; Carrino, D.A.; Lauer, M.E.; Vasanji, A.; Wylie, J.D.; Nelson, C.M.; Apte, S.S.
Pericellular versican regulates the fibroblast-myofibroblast transition: a role for ADAMTS5 protease-mediated proteolysis
J. Biol. Chem.
286
34298-34310
2011
Mus musculus
brenda
Verma, P.; Dalal, K.
ADAMTS-4 and ADAMTS-5: key enzymes in osteoarthritis
J. Cell. Biochem.
112
3507-3514
2011
Homo sapiens
brenda
Durigova, M.; Nagase, H.; Mort, J.S.; Roughley, P.J.
MMPs are less efficient than ADAMTS5 in cleaving aggrecan core protein
Matrix Biol.
30
145-153
2011
Homo sapiens
brenda
Groma, G.; Grskovic, I.; Schael, S.; Ehlen, H.W.; Wagener, R.; Fosang, A.; Aszodi, A.; Paulsson, M.; Brachvogel, B.; Zaucke, F.
Matrilin-4 is processed by ADAMTS-5 in late Golgi vesicles present in growth plate chondrocytes of defined differentiation state
Matrix Biol.
30
275-280
2011
Mus musculus
brenda
Shieh, H.S.; Tomasselli, A.G.; Mathis, K.J.; Schnute, M.E.; Woodard, S.S.; Caspers, N.; Williams, J.M.; Kiefer, J.R.; Munie, G.; Wittwer, A.; Malfait, A.M.; Tortorella, M.D.
Structure analysis reveals the flexibility of the ADAMTS-5 active site
Protein Sci.
20
735-744
2011
Homo sapiens (Q9UNA0)
brenda
Kumar, S.; Sharghi-Namini, S.; Rao, N.; Ge, R.
ADAMTS5 functions as an anti-angiogenic and anti-tumorigenic protein independent of its proteoglycanase activity
Am. J. Pathol.
181
1056-1068
2012
Homo sapiens
brenda
Ariyoshi, W.; Takahashi, N.; Hida, D.; Knudson, C.; Knudson, W.
Mechanisms involved in enhancement of the expression and function of aggrecanases by hyaluronan oligosaccharides
Arthritis Rheumatol.
64
187-197
2012
Bos taurus
brenda
Filou, S.; Stylianou, M.; Triantaphyllidou, I.E.; Papadas, T.; Mastronikolis, N.S.; Goumas, P.D.; Papachristou, D.J.; Ravazoula, P.; Skandalis, S.S.; Vynios, D.H.
Expression and distribution of aggrecanases in human larynx: ADAMTS-5/aggrecanase-2 is the main aggrecanase in laryngeal carcinoma
Biochimie
95
725-734
2013
Homo sapiens
brenda
Atobe, M.; Maekawara, N.; Ishiguro, N.; Sogame, S.; Suenaga, Y.; Kawanishi, M.; Suzuki, H.; Jinno, N.; Tanaka, E.; Miyoshi, S.
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors
Bioorg. Med. Chem. Lett.
23
2106-2110
2013
Homo sapiens, Homo sapiens (Q9UNA0)
brenda
Sogame, S.; Suenaga, Y.; Atobe, M.; Kawanishi, M.; Tanaka, E.; Miyoshi, S.
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping
Eur. J. Med. Chem.
71
250-258
2014
Homo sapiens (Q9UNA0)
brenda
Didangelos, A.; Mayr, U.; Monaco, C.; Mayr, M.
Novel role of ADAMTS-5 protein in proteoglycan turnover and lipoprotein retention in atherosclerosis
J. Biol. Chem.
287
19341-19345
2012
Mus musculus
brenda
Durham, T.; Klimkowski, V.; Rito, C.; Marimuthu, J.; Toth, J.; Liu, C.; Durbin, J.; Stout, S.; Adams, L.; Swearingen, C.; Lin, C.; Chambers, M.; Thirunavukkarasu, K.; Wiley, M.
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis
J. Med. Chem.
57
10476-10485
2014
Homo sapiens
brenda
Filomia, F.; Saxena, P.; Durante, C.; De Rienzo, F.; Cocchi, M.; Menziani, M.
Computational insights into ADAMTS4, ADAMTS5 and MMP13 inhibitor selectivity
Mol. Inform.
31
421-430
2012
Homo sapiens (Q9UNA0)
brenda
Wang, Z.; Luo, J.; Iwamoto, S.; Chen, Q.
Matrilin-2 is proteolytically cleaved by ADAMTS-4 and ADAMTS-5
Molecules
19
8472-8487
2014
Homo sapiens (Q9UNA0), Homo sapiens
brenda
Apte, S.S.
Anti-ADAMTS5 monoclonal antibodies implications for aggrecanase inhibition in osteoarthritis
Biochem. J.
473
e1-e4
2016
Mus musculus (P59384), Mus musculus
brenda
Dancevic, C.M.; Gibert, Y.; Berger, J.; Smith, A.D.; Liongue, C.; Stupka, N.; Ward, A.C.; McCulloch, D.R.
The ADAMTS5 metzincin regulates zebrafish somite differentiation
Int. J. Mol. Sci.
19
E766
2018
Danio rerio
brenda
McMahon, M.; Ye, S.; Izzard, L.; Dlugolenski, D.; Tripp, R.A.; Bean, A.G.; McCulloch, D.R.; Stambas, J.
ADAMTS5 is a critical regulator of virus-specific T cell immunity
PLoS Biol.
14
e1002580
2016
Mus musculus (P59384)
brenda
Bauters, D.; Bedossa, P.; Lijnen, H.R.; Hemmeryckx, B.
Functional role of ADAMTS5 in adiposity and metabolic health
PLoS ONE
13
e0190595
2018
Mus musculus (P59384)
brenda
Aydos, O.S.; Yukselten, Y.; Ozkavukcu, S.; Sunguroglu, A.; Aydos, K.
ADAMTS1 and ADAMTS5 metalloproteases produced by Sertoli cells a potential diagnostic marker in azoospermia
Syst. Biol. Reprod. Med.
65
29-38
2019
Homo sapiens (Q8TE58), Homo sapiens
brenda