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3.4.24.B4: matrix metalloproteinase-13

This is an abbreviated version!
For detailed information about matrix metalloproteinase-13, go to the full flat file.

Word Map on EC 3.4.24.B4

Reaction

proteolytic degradation of proteins =

Synonyms

collagenase, collagenase 3, collagenase-3, M10.013, matrix metalloproteinase 13, matrix metalloproteinase-13, MMP-13, MMP13, MMP13a, More, UMRCASE

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.B4 matrix metalloproteinase-13

Inhibitors

Inhibitors on EC 3.4.24.B4 - matrix metalloproteinase-13

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2R)-N,3-dihydroxy-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]propanamide
-
-
(2R)-N-hydroxy-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]-2-(tetrahydro-2H-pyran-4-yl)ethanamide
-
-
(2R)-N-hydroxy-3-methyl-2-[(naphthalen-2-ylsulfonyl)amino]butanamide
-
-
(2R)-N-hydroxy-3-methyl-2-[methyl(naphthalen-2-ylsulfonyl)amino]butanamide
-
-
(2R)-N-hydroxy-4-(4-hydroxyphenyl)-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]butanamide
-
-
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
-
(2R)-[1-(tert-butoxycarbonyl)piperidin-4-yl][([5-[4-(dimethylamino)phenyl]thiophen-2-yl]sulfonyl)amino]ethanoic acid
-
-
(2R,3R)-4-[[4-(2-chloro-4-fluorophenoxy)phenyl]sulfonyl]-N,2-dihydroxy-2-methylmorpholine-3-carboxamide
-
-
(2R,4S)-1-((4-[(2-chlorobenzyl)oxy]phenyl)sulfonyl)-N,4-dihydroxypiperidine-2-carboxamide
-
i.e. rTACE, 50% inhibition at 12 nM
(2S,3R)-1-acetyl-N-hydroxy-2-methyl-4-[[4-(2-methylbenzyl)phenyl]sulfonyl]piperidine-3-carboxamide
-
-
(2S,3R)-2-[(cyclopropylmethyl)amino]-N1-hydroxy-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-3-methylbutanediamide
-
(2Z,5E)-2-(1,2-benzothiazol-3-ylimino)-5-(2-methoxybenzylidene)-1,3-thiazolidin-4-one
-
(2Z,5E)-2-(1,2-benzothiazol-3-ylimino)-5-(3-methoxybenzylidene)-1,3-thiazolidin-4-one
-
(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
(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
(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
(3S)-N,3-dihydroxy-4-[(4-(2-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
-
50% inhibition at 2.7 nM
(3S)-N,3-dihydroxy-4-[(4-(3-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
-
50% inhibition at 2.4 nM
(3S)-N,3-dihydroxy-4-[(4-(3-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
-
50% inhibition at 5 nM
(3S)-N,3-dihydroxy-4-[(4-(4-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
-
50% inhibition at 0.88 nM, selective for enzyme
(3S)-N,3-dihydroxy-4-[(4-(4-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
-
50% inhibition at 1.3 nM
(3S,3'S)-astaxanthin
i.e. 3S,3’S-dihydoxy-beta, beta-carotene-4,4’-dione, active metabolite of some soft drugs, binds to enzyme at or near active site
(4-[[([5-[2-(ethoxycarbonyl)-1H-indol-5-yl]-1-methyl-1H-pyrazol-3-yl]carbonyl)amino]methyl]phenyl)acetic acid
-
-
(4R)-1-[4-(4-fluorophenoxy)benzyl]-N-hydroxy-2-oxoimidazolidine-4-carboxamide
-
-
(4S)-4-[4-(4-fluorophenoxy)phenyl]-N-hydroxy-5-oxo-D-prolinamide
-
-
(E)-2-(4-(2-(biphenyl-4-yl)vinyl)-N-isopropoxyphenylsulfonamido)-N-hydroxyacetamide
-
(R)-2-(4'-(4-chlorobenzyloxy)-N-isopropoxybiphenyl-4-ylsulfonamido)-N-hydroxy-3-methylbutanamide
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-(1-cyclohexanecarbonyl-piperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-(1-iso-propylcarbamoyl-piperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2,2-dimethylpropionyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2,2-dimethylpropyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2-methylpropane-1-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(3,3-dimethylbutyryl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(benzenesulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(methane-1-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(phenylmethanesulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(propane-1-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(propane-2-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(tetrahydropyran-4-carbonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-benzylpiperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-iso-butylpiperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-diethylcarbamoylpiperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-iso-butyl-piperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-isopropylcarbamoyl-piperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-tertbutylcarbamoyl-piperidin-4-yl)-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-[1-(benzenesulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
(R)-[5-(4-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(butane-1-sulfonyl)-piperidin-4-yl]-acetic acid
-
-
1,10-phenanthroline
1 mM, no residual activity
1,5-anhydro-2,3-dideoxy-3-[[4-(2,4-dichlorophenoxy)phenyl]sulfonyl]-4-C-(hydroxycarbamoyl)-D-threo-pentitol
-
-
1-(4-amino-2-methylquinolin-6-yl)-3-(4-methoxyphenyl)urea
-
-
1-(4-phenoxyphenyl)-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(1-hydroxyethyl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(1-methoxyethyl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(2-methoxyphenyl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(2-phenylethyl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(propan-2-yl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyrazin-2-yl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyridin-2-yl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyridin-4-yl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyrimidin-4-yl)piperazin-1-yl]piperidine-4-carboxamide
-
-
1-(6-[4-[4-(4-fluorophenyl)-1,3-oxazol-2-yl]phenoxy]pyridin-3-yl)-1,7,9-triazaspiro[4.5]decane-6,8,10-trione
-
-
1-acetyl-4-hydroxypyrrolidine-2-carboxylic acid
-
binding structure, modelling, overview
1-cyclopropyl-4-[(4-[4-[(1,3-dibenzyl-1,3-dimethyltriazan-2-yl)carbonyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
1-cyclopropyl-4-[[4-(4-[[4-(2,3-dimethylphenyl)piperazin-1-yl]carbonyl]piperidin-1-yl)phenyl]sulfonyl]-N-hydroxypiperidine-4-carboxamide
-
-
1-cyclopropyl-N-hydroxy-4-([4-[4-(4-methoxyphenyl)piperazin-1-yl]phenyl]sulfonyl)piperidine-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
1-cyclopropyl-N-hydroxy-4-[(4-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]phenyl)sulfonyl]piperidine-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
1-cyclopropyl-N-hydroxy-4-[[4-(4-phenylpiperazin-1-yl)phenyl]sulfonyl]piperidine-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
1-[4-((4-phenoxy)phenoxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
-
comparison of selectivity with other matrix metalloproteinases
1-[4-(1,3-benzodioxol-5-yloxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
-
comparison of selectivity with other matrix metalloproteinases
1-[4-(3-methoxyphenoxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
-
comparison of selectivity with other matrix metalloproteinases
1-[4-(4-chlorophenoxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
-
comparison of selectivity with other matrix metalloproteinases
2,3-dihydro-1,4-benzodioxine-2-carboxylic acid
-
binding structure, modelling, overview
2,3-dihydro-1,4-benzodioxine-5-carboxylic acid
-
binding structure, modelling, overview
2-(2-[(2-chlorobenzoyl)amino]-1,3-thiazol-4-yl)acetic acid
-
binding structure, modelling, overview
2-(4'-(4-chlorobenzyloxy)-N-isopropoxybiphenyl-4-ylsulfonamido)-N-hydroxyacetamide
-
2-(4'-butoxy-N-isopropoxybiphenyl-4-ylsulfonamido)-N-hydroxyacetamide
-
2-(5-((4-butylphenyl)ethynyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
-
2-(5-(4-ethylphenyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
-
2-(5-(4-fluorophenyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
-
2-(benzo[d]isothiazol-3-ylimino)-5-(4-methoxybenzylidene)thiazolidin-4-one
potent and selective MMP-13 inhibitor
2-(ethyl[[4-(prop-1-yn-1-yloxy)phenyl]sulfonyl]amino)-5-phenylpentane(thioperox)ic O-acid
-
-
2-butanoyl-1H-indole-5-carboxamide
-
-
2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
-
-
2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
-
-
2-fluoro-N-hydroxy-6-([4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl]sulfonyl)benzamide
-
-
2-fluoroisophthalic acid
-
binding structure, modelling, overview
2-[(4-chlorobenzyl)sulfanyl]-6-methylpyrimidin-4-ol
-
competitive
2-[benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-hydroxy-3,5-dimethylbenzamide
-
WAY- 152177
2-[[(4'-chlorobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
-
-
2-[[(4'-cyanobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
-
-
2-[[(4'-[[(5-bromo-4-methoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]methyl]-3-methylbutanoic acid
-
-
2-[[[4-(4-chlorophenoxy)phenyl]sulfonyl](methyl)amino]-N-hydroxy-3-[(4-methylpiperazin-1-yl)methyl]benzamide
-
-
3-(carboxymethyl)-2-methylenepentanedioic acid
-
binding structure, modelling, overview
3-[(4-methoxyphenyl)sulfonyl]propane-1-thiol
-
-
3-[(4-phenoxyphenyl)sulfonyl]cyclohexanethiol
-
-
3-[[4-(phenylsulfanyl)phenyl]sulfonyl]cyclohexanethiol
-
-
4'-aminobiphenyl-4-sulfonamide
-
competitive
4-((R)-carboxy-[5-[4'-(2-methoxyethoxy)-phenyl]-thiophene-2-sulfonylamino]-methyl)-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-(2-cyanophenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(2-phenylethoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(3-methoxy-4-nitrophenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(3-[3-[3-(3,4-difluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]prop-2-yn-1-yl]phenyl)butanoic acid
-
-
4-(4-methylphenoxy)-N-(pyridin-3-ylmethyl)benzamide
-
-
4-(4-methylphenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(4-methylphenoxy)-N-[2-(pyridin-4-yl)ethyl]benzamide
-
-
4-(4-nitrophenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(4-[[(3R)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(4-[[(3R)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-(4-[[(3S)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-(4-[[(3S)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)-N-(2-fluorobenzyl)benzamide
-
50% inhibition at 01.1 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-8, MMP-12
4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)-N-(3-fluorobenzyl)benzamide
-
50% inhibition at 0.85 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-8, MMP-12
4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)-N-phenylbenzamide
-
50% inhibition at 0.84 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-8, MMP-12
4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)-N-pyridin-3-ylbenzamide
-
50% inhibition at 0.40 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-8, MMP-12
4-(benzyloxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
4-([(2-([(3-methoxyphenyl)methyl]carbamoyl)-4-oxo-3H,4H-thieno[2,3-d]pyrimidin-5-yl)methoxy]methyl)benzoic acid
highly potent and selective MMP-13 inhibitor. Compound shows shows more than 2600fold selectivity over the other related metalloenzymes. The disodium salt formulation is well absorbed in all species tested at the oral dose of 10-20 mg/kg. Compound is active in in bovine nasal cartilage explants assay
4-([4-[(5-[[4-(dimethylamino)phenyl]amino]-5-oxopentyl)oxy]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-([4-[4-(2,4-dimethylphenyl)piperazin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(2-chlorophenyl)piperazin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(2-chlorophenyl)piperidin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(2-ethoxyphenyl)piperidin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(2-fluorophenyl)piperazin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(4'-fluorobiphenyl-2-yl)piperidin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(4-chlorophenyl)piperazin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([4-[4-(4-chlorophenyl)piperidin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
4-([5-[2-(benzylcarbamoyl)-6-methylpyridin-4-yl]-2H-tetrazol-2-yl]methyl)benzoic acid
-
4-([5-[2-(benzylcarbamoyl)-6-methylpyridin-4-yl]-2H-tetrazol-2-yl]methyl)cyclohexanecarboxylic acid
-
4-([6-[(4-methoxybenzyl)carbamoyl]-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl]methyl)benzoic acid
4-([[4-(4-chlorophenoxy)phenyl]sulfonyl]methyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-([[4-(4-fluorophenoxy)phenyl]sulfonyl]amino)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-methoxy-N,N'-bis(pyridin-3-ylmethyl)benzene-1,3-dicarboxamide
-
competitive
4-methoxy-N-(pyridin-4-ylmethyl)benzamide
-
-
4-oxo-N-[[40-([[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]sulfonyl]methyl)biphenyl-3-yl]methyl]-3,4-dihydroquinazoline-2-carboxamide
compound exhibits excellent potency and selectivity (greater than 170fold) over MMP1, 2, 3, 7, 8, 9, 10, 12, and 14 and tumor necrosis factor-alpha converting enzyme
4-phenoxy-N-(pyridin-4-ylmethyl)benzamide
-
-
4-[(4-[3-[(2,2-dimethylpentanoyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[3-[(2,4-dimethylbenzoyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[3-[(cyclohexylcarbonyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[3-[4-(dimethylamino)phenyl]-3-oxopropoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[4-[(1,3-diethenyl-1,3-dimethyltriazan-2-yl)carbonyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[4-[4-(dimethylamino)benzoyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
MMP-13 selective
4-[(4-[4-[4-(dimethylamino)phenyl]-4-oxobutoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[(4-[4-[bis(3,5-dimethylpiperidin-1-yl)carbamoyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxy-1-(2-methoxyethyl)piperidine-4-carboxamide
-
-
4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3-chloro-4-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3-chlorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3-cyanobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3-fluorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3-hydroxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3-methoxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(3-methoxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(3-methoxybenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(4-chlorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(4-fluoro-3-hydroxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(4-fluoro-3-methoxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(4-fluoro-3-methylbenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(4-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(4-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(4-fluorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(4-methoxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(5-[2-[(4-methoxybenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
-
4-[(5-[2-[(4-methoxybenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
-
4-[(R)-(benzofuran-2-sulfonylamino)-carboxy-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-(benzo[b]thiophene-2-sulfonylamino)-carboxy-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(4'-dimethylamino-biphenyl-4-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(4'-ethoxybiphenyl-4-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(4'-fluorobiphenyl-4-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(4'-methoxybiphenyl-4-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(4'-methylbiphenyl-4-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(5-phenylthiophene-2-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(5-pyridin-2-yl-thiophene-2-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-(5-pyridin-4-yl-thiophene-2-sulfonylamino)-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(3',4'-difluorophenyl)-furan-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(3',4'-methylenedioxyphenyl)-furan-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(3,4-dimethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(3-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid 1-ethyl-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid 4-tetrahydropyranyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid butyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid cyclohexyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid ethyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-butyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid methyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid neopentyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid propyl ester
-
-
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(4'-hydroxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-iso-propoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-methylphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-N,N-dimethylaminophenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid
-
-
4-[(R)-carboxy-[5-(4'-n-propoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid
-
-
4-[(R)-carboxy-[5-(4'-piperidin-1-yl-phenyl)-thiophene-2-sulfonylamino]-methyl]piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-piperidin-1-yl-phenyl)-thiophene-2-sulfonylamino]-methyl]piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(4'-trifluoromethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-(4'-trifluoromethylphenyl)-furan-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[(R)-carboxy-[5-(4'-trifluoromethylphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[(R)-carboxy-[5-phenylthiophene-2-sulfonylamino]-methyl]piperidine-1-carboxylic acid iso-propyl ester
-
-
4-[([3-[(3-methoxybenzyl)carbamoyl]benzoyl]amino)methyl]benzoic acid
-
4-[([3-[2-(3-methoxybenzyl)-2H-tetrazol-5-yl]benzoyl]amino)methyl]benzoic acid
-
4-[([3-[2-(4-methoxybenzyl)-2H-tetrazol-5-yl]benzoyl]amino)methyl]benzoic acid
-
4-[([[5-(1H-indol-5-yl)-1-methyl-1H-pyrazol-3-yl]carbonyl]amino)methyl]benzoic acid
-
-
4-[2-([6-fluoro-2-[([[3-(methyloxy)phenyl]methyl]amino)-carbonyl]-4-oxo-3,4-dihydroquinazolin-5-yl]oxy)ethyl]-benzoic acid
inhibitor exhibits excellent potency and selectivity for MMP-13 over other MMPs. No overt toxicity is observed in a preliminary repeat dose oral toxicity study of compound in rats. A single oral dose of the monosodium salt significantly reduces degradation products released from articular cartilage into the joint cavity in a rat MIA model in vivo
4-[2-[4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)phenyl]-1,3-oxazol-4-yl]benzonitrile
-
-
4-[4-(2,6,8,10-tetraoxo-1,7,9-triazaspiro[4.5]dec-1-yl)phenoxy]benzoic acid
-
comparison of selectivity with other matrix metalloproteinases
4-[4-(methylcarbamoyl)phenoxy]-N-(pyridin-4-ylmethyl)benzamide
-
-
4-[4-[(3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl)ethynyl]phenoxy]-N-(pyridin-4-ylmethyl)benzamide
-
-
4-[4-[(3-methoxy-1-azabicyclo[2.2.2]oct-3-yl)ethynyl]phenoxy]-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-[4-[(E)-2-(1-azabicyclo[2.2.2]oct-2-en-3-yl)ethenyl]phenoxy]-N-(pyridin-4-ylmethyl)benzamide
-
-
4-[4-[(E)-2-(1-azabicyclo[2.2.2]oct-2-en-3-yl)ethenyl]phenoxy]-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-[4-[(E)-2-(3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl)ethenyl]phenoxy]-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-[4-[2-(3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl)ethyl]phenoxy]-N-(pyrimidin-4-ylmethyl)benzamide
-
-
4-[carboxy-[5-(4-N,N-dimethylaminophenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[carboxy-[5-(6-methoxy-pyridin-3-yl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid tert-butyl ester
-
-
4-[[([5-[2-(ethoxycarbonyl)-1H-indol-5-yl]-1-methyl-1H-pyrazol-3-yl]carbonyl)amino]methyl]benzoic acid
-
-
4-[[([5-[2-(ethoxymethyl)-1H-indol-5-yl]-1-methyl-1H-pyrazol-3-yl]carbonyl)amino]methyl]benzoic acid
-
-
4-[[1-methyl-2,4-dioxo-6-(3-phenylprop-1-yn-1-yl)-1,4-dihydroquinazolin-3(2H)-yl]methyl]benzoic acid
4-[[4-(3-[[4-(dimethylamino)benzoyl]amino]propoxy)phenyl]sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[[4-(4-[[1-ethynyl-1,3-dimethyl-3-(prop-2-yn-1-yl)triazan-2-yl]carbonyl]piperidin-1-yl)phenyl]sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[[4-(4-[[4-(2,3-dimethylphenyl)piperazin-1-yl]carbonyl]piperidin-1-yl)phenyl]sulfonyl]-N-hydroxy-1-(2-methoxyethyl)piperidine-4-carboxamide
-
-
4-[[4-(4-[[4-(2,3-dimethylphenyl)piperazin-1-yl]carbonyl]piperidin-1-yl)phenyl]sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[[4-(4-[[4-(dimethylamino)phenyl]amino]-4-oxobutoxy)phenyl]sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
-
4-[[4-([5-[4-(dimethylamino)phenyl]-5-oxopentyl]oxy)phenyl]sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
-
MMP-13 selective
4-[[4-oxo-6-(3-phenylprop-1-yn-1-yl)quinazolin-3(4H)-yl]methyl]benzoic acid
-
-
4-[[5-(2-methyl-6-[[3-(propan-2-yloxy)benzyl]carbamoyl]pyridin-4-yl)-2H-tetrazol-2-yl]methyl]cyclohexanecarboxylic acid
-
4-[[5-(2-methyl-6-[[3-(trifluoromethyl)benzyl]carbamoyl]pyridin-4-yl)-2H-tetrazol-2-yl]methyl]benzoic acid
-
4-[[5-(2-[[3-(trifluoromethyl)benzyl]carbamoyl]pyridin-4-yl)-2H-tetrazol-2-yl]methyl]benzoic acid
-
4-[[5-(2-[[4-fluoro-3-(trifluoromethyl)benzyl]carbamoyl]-6-methylpyridin-4-yl)-2H-tetrazol-2-yl]methyl]cyclohexanecarboxylic acid
-
4-[[6-(2-[3-[3-(hydroxyamino)-3-oxopropoxy]phenyl]-1,3-oxazol-5-yl)-4-oxoquinazolin-3(4H)-yl]methyl]benzoic acid
-
-
5-(2-ethoxyethyl)-5-[4-[4-(1,3,4-oxadiazol-2-yl)phenoxy]phenoxy]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-(3,4-difluorobenzyl)-7-methyl-4,6-dioxo-N-[[2-(3-sulfanylpropoxy)pyridin-4-yl]methyl]-3a,4,5,6-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
-
5-(4-chlorophenoxy)-5-methylpyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-(4-chlorophenyl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
5-(5-chloropyridin-2-yl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
5-hexyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-methyl-5-(4-phenoxyphenoxy)pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-[3-[(4-carboxybenzyl)carbamoyl]-1-methyl-1H-pyrazol-5-yl]-1H-indole-2-carboxylic acid
-
-
5-[3-[(acetylamino)methyl]phenyl]-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
5-[4-(1-benzofuran-2-ylmethoxy)phenyl]-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-1,2-dihydro-3H-pyrazol-3-one
-
-
5-[4-(acetylamino)phenyl]-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
6-hydroxy-2-(methylsulfanyl)-4-pyrimidinecarboxylic acid
-
binding structure, modelling, overview
AG1296
-
a platelet-derived growth factor receptor inhibitor, shows several physiological effects, overview
alendronate
-
inhibits the in vitro invasion and random cell migration, 99% inhibition at 0.4 mM and physiological Ca2+-concentration, 67% inhibition at 0.4 mM and high Ca2+-concentration
ALS 1-0635
-
BB94
-
a broadspectrum MMP inhibitor, significantly inhibits keratinocyte migration
benzyl 6-benzyl-5,7-dioxo-6,7-dihydro-5H-[1,3]thiazolo[3,2-c]pyrimidine-2-carboxylate
-
competitive, does not ligate the catalytic zinc, zinc binding is unnecessary to achieve nanomolar affinity, extremely selective for inhibition of MMP13 over all other MMPs
bone morphogenetic protein 2
-
down-regulation of enzyme expression in osteoblasts, can be overcome by noggin
-
bone morphogenetic protein 4
-
down-regulation of enzyme expression in osteoblasts, can be overcome by noggin
-
bone morphogenetic protein 6
-
down-regulation of enzyme expression in osteoblasts, can be overcome by noggin
-
CGS027023
-
-
cilostazol
docking-based screening of existing drugs and binding free-energy calculation suggests eltrombopag, cilostazol and domperidone as potential MMP-13 inhibitors
cipemastat
-
-
CL 82198
CL-82198
clodronate
-
77% inhibition at 0.4 mM and physiological Ca2+-concentration, 35.7% inhibition at 0.4 mM and high Ca2+-concentration
CP-471474
Cu2+
10 mM, 15% residual activity
domperidone
docking-based screening of existing drugs and binding free-energy calculation suggests eltrombopag, cilostazol and domperidone as potential MMP-13 inhibitors
EDTA
10 mM, 1% residual activity
eltrombopag
docking-based screening of existing drugs and binding free-energy calculation suggests eltrombopag, cilostazol and domperidone as potential MMP-13 inhibitors
ethyl 5-(1-methyl-1H-imidazol-5-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-(1-methyl-3-[[(6-oxo-1,6-dihydropyridin-3-yl)methyl]carbamoyl]-1H-pyrazol-5-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-(3-methylpyridin-4-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-(acetylamino)-1H-indole-2-carboxylate
-
-
ethyl 5-(pyridin-2-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-(pyridin-3-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-(pyridin-4-yl)-1H-indole-2-carboxylate
-
-
ethyl 5-carbamoyl-1H-indole-2-carboxylate
-
-
ethyl 5-phenyl-1H-indole-2-carboxylate
-
-
ethyl 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylate
-
-
ethyl 5-[1-methyl-3-[(pyridin-4-ylmethyl)carbamoyl]-1H-pyrazol-5-yl]-1H-indole-2-carboxylate
-
-
ethyl 5-[3-(methoxycarbonyl)-1-methyl-1H-pyrazol-5-yl]-1H-indole-2-carboxylate
-
-
ethyl 5-[5-methyl-2-[(pyridin-4-ylmethyl)carbamoyl]pyridin-4-yl]-1H-indole-2-carboxylate
-
-
Fe2+
10 mM, 9% residual activity
furin
-
inhibition of enzyme induction by TGFbeta1 in chondrocytes
-
hydroxamate inhibitor RS-113456
a diphenyl ether sulfon compound, complexing of the enzyme via His205 and Glu202
-
hydroxamic acid inhibitor CGS 27023
complex formation with the catalytic fragment of the enzyme, inhibitor binding mechanism
hydroxamic acid inhibitor WAY-151693
complex formation with the catalytic fragment of the enzyme
hydroxamic acid-based inhibitor CT1399
-
-
-
hydroxamic acid-based inhibitor CT1847
-
-
-
ilomastat
mannose-6-phosphate/insulin-like growth factor 2 receptor
-
inhibition of enzyme induction by TGFbeta1 in chondrocytes
-
marimastat
matrix metalloprotease inhibitor GW9471
-
broad spectrum
methyl 3-[4-(1H-imidazol-1-yl)phenyl]propanoate
-
-
methyl 4-[4-(2,6,8,10-tetraoxo-1,7,9-triazaspiro[4.5]dec-1-yl)phenoxy]benzoate
-
comparison of selectivity with other matrix metalloproteinases
Mg2+
10 mM, 38% residual activity
minocycline
-
inhibits MMP-13 activity in synoviocytes
Mn2+
10 mM, 2.5% residual activity
N,N'-bis(3-methoxybenzyl)benzene-1,3-dicarboxamide
-
N,N'-bis(3-methylbenzyl)pyrimidine-4,6-dicarboxamide
N,N'-bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-dicarboxamide
50% inhibition at 8 nM
N,N'-bis(pyridin-3-ylmethyl)pyrimidine-4,6-dicarboxamide
N,N'-dibenzylpyrimidine-4,6-dicarboxamide
50% inhibition at 400 nM
N,N-bis(2,6-dimethylmorpholin-4-yl)-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis(3,5-dimethylpiperidin-1-yl)-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis(4-acetylpiperazin-1-yl)-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis(7,8-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis[4-(2,4-dimethylphenyl)piperazin-1-yl]-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis[4-(2-fluorophenyl)piperazin-1-yl]-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis[4-(4-acetylphenyl)piperazin-1-yl]-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis[4-(4-fluorophenyl)piperazin-1-yl]-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-bis[4-[1-(dimethylamino)ethyl]piperazin-1-yl]-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N,N-di(3,4-dihydroisoquinolin-2(1H)-yl)-1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)piperidine-4-carboxamide
-
-
N-(2-hydroxyethyl)-4-(4-methylphenoxy)benzamide
-
-
N-(3-methoxybenzyl)-4-(4-methylphenoxy)benzamide
-
-
N-(3-methoxybenzyl)-4-oxo-3,4-dihydroquinazoline-2-carboxamide
lead compound for the development of thieno[2,3-d]pyrimidine-2-carboxamide inhibitors
N-(4-fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide
N-(cyclohexylmethyl)-4-(4-methylphenoxy)benzamide
-
-
N-(pyridin-4-ylmethyl)biphenyl-4-carboxamide
-
-
N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)valine
N-([4'-[([3-methyl-4-[(methylsulfonyl)amino]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-threonine
-
-
N-([4'-[([3-methyl-4-[(methylsulfonyl)amino]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-valine
-
-
N-([4'-[([4-[(1-methoxy-2-methyl-1-oxopropan-2-yl)oxy]-3-methyl-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-valine
-
-
N-([4'-[([4-[(2-carboxypropan-2-yl)oxy]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)-L-valine
-
-
N-([4'-[([5-[(methylsulfonyl)amino]-1-benzofuran-2-yl]carbonyl)amino]biphenyl-4-yl]sulfonyl)valine
-
50% inhibition at 0.43 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-benzyl-4-(4-methylphenoxy)benzamide
-
-
N-hydroxy-1-(2-methoxyethyl)-4-([4-[4-(phenylcarbamoyl)piperidin-1-yl]phenyl]sulfonyl)piperidine-4-carboxamide
-
-
N-hydroxy-1-(4-methoxyphenyl)sulfonyl-4-(4-biphenylcarbonyl)piperazine-2-carboxamide
-
-
N-hydroxy-2,2-dimethyl-4-[[4-(pyridin-4-yloxy)phenyl]sulfonyl]thiomorpholine-3-carboxamide
-
-
N-hydroxy-2,6-dimethoxy-3-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]pyridine-4-carboxamide
-
-
N-hydroxy-2-(N-isopropoxy-4'-(methylthio)biphenyl-4-ylsulfonamido)acetamide
-
N-hydroxy-2-(N-isopropoxy-4'-methoxybiphenyl-4-ylsulfonamido)acetamide
-
N-hydroxy-2-(N-isopropoxy-4-phenoxyphenylsulfonamido)-acetamide
-
N-hydroxy-2-(N-isopropoxy-5-(4-methoxyphenyl)thiophene-2-sulfonamido)acetamide
-
N-hydroxy-2-[(2-methylpropyl)(naphthalen-2-ylsulfonyl)amino]acetamide
-
-
N-hydroxy-2-[(naphthalen-2-ylsulfonyl)amino]acetamide
-
-
N-hydroxy-2-[[(4-methoxyphenyl)sulfonyl](pyridin-3-ylmethyl)amino]-3-methylbenzamide
-
-
N-hydroxy-3-methyl-2-(methyl[[4-(pyridin-4-yloxy)phenyl]sulfonyl]amino)benzamide
-
-
N-hydroxy-3-methyl-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-4-([4-[(4-hydroxybut-2-yn-1-yl)oxy]phenyl]sulfonyl)-2,2-dimethylthiomorpholine-3-carboxamide
-
-
N-hydroxy-4-([4-[4-(2-hydroxyphenyl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(2-methoxyphenyl)piperazin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(2-methoxyphenyl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(2-methylphenyl)piperazin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(2-methylphenyl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(3,3,6-trimethoxycyclohexa-1,5-dien-1-yl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(3-methoxyphenyl)piperazin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(4,4,6-trimethoxycyclohexa-1,5-dien-1-yl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(4-methoxy-2-methylphenyl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(4-methoxyphenoxy)butoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-([4-[4-(4-methoxyphenyl)piperazin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(4-methylphenyl)piperazin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-(naphthalen-1-yl)piperidin-1-yl]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-([4-[4-oxo-4-(piperidin-1-yl)butoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[(4-[3-[(4-methoxybenzoyl)amino]propoxy]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[(4-[4-[(4-methoxyphenyl)amino]-4-oxobutoxy]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[(4-[4-[2-(trifluoromethyl)phenyl]piperidin-1-yl]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[(4-[4-[2-methoxy-5-(propan-2-yl)phenyl]piperidin-1-yl]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[(4-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[(4-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[[4-(3-[[4-(trifluoromethoxy)benzoyl]amino]propoxy)phenyl]sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[[4-(4-oxo-4-[[4-(trifluoromethoxy)phenyl]amino]butoxy)phenyl]sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[[4-(4-phenylpiperazin-1-yl)phenyl]sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[[4-(4-phenylpiperidin-1-yl)phenyl]sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
pH not specified in the publication, temperature not specified in the publication
N-hydroxy-4-[[4-(4-[methyl[4-(trifluoromethoxy)phenyl]amino]-4-oxobutoxy)phenyl]sulfonyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-hydroxy-4-[[4-(phenylsulfanyl)phenyl]sulfonyl]-1-(prop-2-yn-1-yl)piperidine-4-carboxamide
-
i.e. SC-276
N-hydroxy-N2-(2-methylpropyl)-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(2,3,3a,7a-tetrahydro-1-benzofuran-5-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-5-phenyl-D-norvalinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-leucinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-threoninamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(quinolin-2-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(quinolin-3-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-(quinolin-6-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-[(6-propoxynaphthalen-2-yl)sulfonyl]-D-valinamide
-
-
N-hydroxy-N2-(3-methylbutyl)-N2-[[6-(2-methylpropoxy)naphthalen-2-yl]sulfonyl]-D-valinamide
-
-
N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-N2-(2-phenylethyl)-D-valinamide
-
-
N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-N2-(3-phenylpropyl)-D-valinamide
-
-
N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-N2-(pyridin-2-ylmethyl)-D-valinamide
-
-
N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-N2-(pyridin-3-ylmethyl)-D-valinamide
-
-
N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-N2-(pyridin-4-ylmethyl)-D-valinamide
-
-
N-hydroxy-N2-methyl-3-[(4-phenoxyphenyl)sulfonyl]-L-alaninamide
-
-
N-hydroxy-N2-[(4-methoxyphenyl)sulfonyl]-N2-(pyridin-4-ylmethyl)valinamide
-
-
N-hydroxy-N2-[(6-hydroxynaphthalen-2-yl)sulfonyl]-N2-(3-methylbutyl)-D-valinamide
-
-
N-hydroxy-N2-[(6-methoxynaphthalen-2-yl)sulfonyl]-N2-(3-methylbutyl)-D-valinamide
-
-
N-hydroxy-N2-[(7-hydroxynaphthalen-2-yl)sulfonyl]-N2-(3-methylbutyl)-D-valinamide
-
-
N-hydroxy-N2-[(7-methoxynaphthalen-2-yl)sulfonyl]-N2-(3-methylbutyl)-D-valinamide
-
-
N-hydroxy-N2-[2-(morpholin-4-yl)ethyl]-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N-hydroxy-N2-[[6-(3-methylbutoxy)naphthalen-2-yl]sulfonyl]-N2-(3-methylbutyl)-D-valinamide
-
-
N-methyl-4-(4-methylphenoxy)-N-(pyridin-4-ylmethyl)benzamide
-
-
N-methyl-4-(4-methylphenoxy)benzamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(3-[[(furan-2-ylcarbonyl)amino]methyl]phenyl)furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(4-ethoxyphenyl)furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(4-methoxyphenyl)furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(4-methylphenyl)furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(4-phenoxyphenyl)furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[3-([[(2-methylfuran-3-yl)carbonyl]amino]methyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-(1H-pyrazol-3-ylmethoxy)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-(methylcarbamoyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-(methylsulfamoyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(1,5-dimethyl-1H-pyrazol-3-yl)methoxy]phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(1-methyl-1H-pyrazol-3-yl)methoxy]phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(5-methyl-1H-pyrazol-3-yl)methoxy]phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(6-methylpyridin-2-yl)methoxy]phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(methylsulfonyl)amino]phenyl]furan-2-carboxamide
-
-
N-[(4'-[[(3,4-dimethyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(3-methyl-4-phenoxy-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(3-methyl-4-phenyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-amino-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-cyano-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-ethenyl-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-ethoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-ethyl-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-hydroxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(4-methoxy-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]valine
-
50% inhibition at 2.33 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[(4'-[[(4-methoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]-L-valine
-
-
N-[(4'-[[(5-amino-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]valine
-
50% inhibition at 1.5 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[(4'-[[(5-chloro-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]valine
-
50% inhibition at 0.6 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[(4'-[[(5-methoxy-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]valine
-
50% inhibition at 0.66 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[(4'-[[(5-nitro-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]valine
-
50% inhibition at 0.7 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[(4-[5-[([3-methyl-4-[(methylsulfonyl)amino]-1-benzofuran-2-yl]carbonyl)amino]pyridin-2-yl]phenyl)sulfonyl]-L-threonine
-
replacing a backbone benzene with a pyridine and valine with threonine results in greatly reduced plasma protein binding of the compound
N-[(4-[5-[([3-methyl-4-[(methylsulfonyl)amino]-1-benzofuran-2-yl]carbonyl)amino]pyridin-2-yl]phenyl)sulfonyl]-L-valine
-
-
N-[2-(4,5-dihydro-1,3-oxazol-2-yl)-1H-indol-5-yl]acetamide
-
-
N-[2-(4-[benzyl[2-(hydroxycarbamoyl)-4,6-dimethylphenyl]sulfamoyl]phenoxy)ethyl]-1-benzofuran-2-carboxamide
-
WAY-170523
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-imidazole-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-3-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-4-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-methyl-1,3-thiazole-4-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylfuran-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylpyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-ethylpyridine-3-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-methylfuran-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-methylpyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-7-methylimidazo[1,2-a]pyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-8-methylimidazo[1,2-a]pyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]imidazo[1,2-a]pyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-2-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-3-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
-
-
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
-
-
N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
-
N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
-
N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
-
N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
-
N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
-
N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
-
N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
-
N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
-
N-[3-(dimethylamino)propyl]-4-(4-methylphenoxy)benzamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-1-benzofuran-2-carboxamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-1-methyl-1H-pyrazole-3-carboxamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-4,5-dimethylfuran-2-carboxamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-5-methyl-1H-pyrazole-3-carboxamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-5-methylfuran-2-carboxamide
-
-
N-[4-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)phenyl]-6-methylpyridine-2-carboxamide
-
-
N-[4-(morpholin-4-yl)butyl]-1-benzofuran-2-carboxamide
-
i.e. CL-82198
N-[[(3-phenyl-1,2-oxazol-5-yl)methyl]carbamothioyl]benzamide
-
competitive, is synergic with acetohydroxamic acid
N-[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]-L-phenylalanine
-
-
N-[[4'-([[3-methyl-4-(methylamino)-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[3-methyl-4-(morpholin-4-yl)-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[3-methyl-4-(prop-1-yn-1-yl)-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[4-(3-hydroxypropyl)-3-methyl-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[4-(3-methoxypropyl)-3-methyl-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[4-(acetylamino)-3-methyl-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[4-(dimethylamino)-3-methyl-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[4-(furan-2-yl)-3-methyl-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]-L-valine
-
-
N-[[4'-([[5-(acetylamino)-1-benzofuran-2-yl]carbonyl]amino)biphenyl-4-yl]sulfonyl]valine
-
50% inhibition at 0.98 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N-[[4-(4-fluorophenoxy)phenyl]sulfonyl]-N-[1-(hydroxycarbamoyl)cyclopentyl]-b-alanine
-
-
N-[[4-(5-[[(4-cyano-3-methyl-1-benzofuran-2-yl)carbonyl]amino]pyridin-2-yl)phenyl]sulfonyl]-L-valine
-
-
N2,N5-bis(3-methylbenzyl)-6-oxo-1,6-dihydropyrimidine-2,5-dicarboxamide
compound shows about 75fold selectivity over metalloproteases MMP3, MMP12
N2,N5-bis(4-fluoro-3-methylbenzyl)-6-oxo-1,6-dihydropyrimidine-2,5-dicarboxamide
compound shows about 65fold and 47fold selectivity over metalloproteases MMP3, MMP12, respectively
N2-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
N2-(3a,7a-dihydro-1-benzothiophen-5-ylsulfonyl)-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
N2-(biphenyl-4-ylsulfonyl)-N-hydroxy-N2-(2-methylpropyl)glycinamide
-
N2-(biphenyl-4-ylsulfonyl)-N-hydroxy-N2-(propan-2-yloxy)-L-valinamide
-
N2-(biphenyl-4-ylsulfonyl)-N-hydroxy-N2-(propan-2-yloxy)glycinamide
-
N2-(biphenyl-4-ylsulfonyl)-N-hydroxyglycinamide
-
N2-({4'-[(4-chlorobenzyl)oxy]biphenyl-4-yl}sulfonyl)-N-hydroxy-N2-(propan-2-yloxy)glycinamide
-
N2-benzyl-N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N2-ethyl-1H-indole-2,5-dicarboxamide
-
-
N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-4-phenylbutanoyl]-N,3-dimethyl-L-valinamide
-
-
N2-[(2S)-2-[[(4-benzylbenzyl)(hydroxy)phosphoryl]methyl]-6-phenoxyhexanoyl]-N,3-dimethyl-L-valinamide
-
-
N2-[(3,4-dimethoxyphenyl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
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N2-[(4'-bromobiphenyl-4-yl)sulfonyl]-N-hydroxy-D-valinamide
N2-[(6-ethoxynaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
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N2-[(6-ethylnaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
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N2-[(7-ethoxynaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
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N2-[2-(dimethylamino)ethyl]-N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
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N2-[[6-(benzyloxy)naphthalen-2-yl]sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
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O-tert-butyl-N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-serinamide
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P53
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down-regulation of enzyme expression, possibly contributes to the dysregulation of the enzyme observed in cancer
PD-331179
Ro32-3555
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a broad-spectrum MMP inhibitor
RS 102,481
SC-276
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tissue matrix metalloproteinase inhibitor fragments of TIMP-1
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tissue matrix metalloproteinase inhibitor fragments of TIMP-2
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tissue matrix metalloproteinase inhibitor hybrid N.TIMP-1/C.TIMP-2
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complex formation is not affected by the C-terminal domain of the enzyme, inhibition mechanism, wild-type enzyme and enzyme fragment 249-451
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tissue matrix metalloproteinase inhibitor TIMP-1
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tissue matrix metalloproteinase inhibitor TIMP-2
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tissue matrix metalloproteinase inhibitor TIMP-3
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tissue matrix metalloproteinase inhibitor-1
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in a ratio of enzyme to inhibitor of 1:1
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tissue matrix metalloproteinase inhibitor-2
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in a ratio of enzyme to inhibitor of 1:1
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tissue matrix metalloproteinase inhibitor-3
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fast inhibition, in a ratio of enzyme to inhibitor of 1:1
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transforming growth factor-beta1
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i.e. TGFbeta1, accelerates the decay of the enzymes mRNA and decreased enzyme expression in osteoblasts
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additional information
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