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
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3.4.24.B4
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cartilage
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chondrocytes
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osteoarthritis
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metalloproteinases
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joint
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articular
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aggrecan
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degeneration
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mmp-2
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tnf
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knee
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timp-1
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arthritis
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synovial
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interleukin-1
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proteoglycans
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degener
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cox-2
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osteoblast
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adamts-5
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ligament
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intra-articular
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collagenases
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col2a1
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thrombospondin
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pulposus
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runx2
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cruciate
-
zymography
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chondrogenic
-
gelatinase
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meniscus
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intervertebral
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subchondral
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disintegrin
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endochondral
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safranin
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synoviocytes
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collagenolytic
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matrix-degrading
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chondroprotective
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ossification
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temporomandibular
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mt1-mmp
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chondrogenesis
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medicine
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stromelysin-1
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diagnostics
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cartilage-specific
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condylar
-
analysis
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osteophyte
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drug development
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aggrecanase
- 3.4.24.B4
- cartilage
- chondrocytes
- osteoarthritis
- metalloproteinases
- joint
-
articular
- aggrecan
- degeneration
- mmp-2
- tnf
- knee
- timp-1
- arthritis
- synovial
- interleukin-1
- proteoglycans
-
degener
- cox-2
- osteoblast
- adamts-5
- ligament
-
intra-articular
- collagenases
-
col2a1
- thrombospondin
- pulposus
- runx2
-
cruciate
-
zymography
-
chondrogenic
- gelatinase
- meniscus
-
intervertebral
-
subchondral
-
disintegrin
-
endochondral
-
safranin
- synoviocytes
-
collagenolytic
-
matrix-degrading
-
chondroprotective
-
ossification
-
temporomandibular
- mt1-mmp
-
chondrogenesis
- medicine
- stromelysin-1
- diagnostics
-
cartilage-specific
-
condylar
- analysis
- osteophyte
- drug development
- aggrecanase
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
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Inhibitors
Inhibitors on EC 3.4.24.B4 - matrix metalloproteinase-13
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(2R)-N,3-dihydroxy-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]propanamide
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(2R)-N-hydroxy-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]-2-(tetrahydro-2H-pyran-4-yl)ethanamide
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(2R)-N-hydroxy-4-(4-hydroxyphenyl)-2-[(3-methylbutyl)(naphthalen-2-ylsulfonyl)amino]butanamide
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(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
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(2R)-[1-(tert-butoxycarbonyl)piperidin-4-yl][([5-[4-(dimethylamino)phenyl]thiophen-2-yl]sulfonyl)amino]ethanoic acid
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(2R,3R)-4-[[4-(2-chloro-4-fluorophenoxy)phenyl]sulfonyl]-N,2-dihydroxy-2-methylmorpholine-3-carboxamide
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(2R,4S)-1-((4-[(2-chlorobenzyl)oxy]phenyl)sulfonyl)-N,4-dihydroxypiperidine-2-carboxamide
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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
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(2S,3R)-2-[(cyclopropylmethyl)amino]-N1-hydroxy-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-3-methylbutanediamide
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(2Z,5E)-2-(1,2-benzothiazol-3-ylimino)-5-(2-methoxybenzylidene)-1,3-thiazolidin-4-one
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(2Z,5E)-2-(1,2-benzothiazol-3-ylimino)-5-(3-methoxybenzylidene)-1,3-thiazolidin-4-one
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(3S)-N,3-dihydroxy-4-[(3'-methylbiphenyl-4-yl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
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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
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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
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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
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50% inhibition at 2.7 nM
(3S)-N,3-dihydroxy-4-[(4-(3-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
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50% inhibition at 2.4 nM
(3S)-N,3-dihydroxy-4-[(4-(3-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
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50% inhibition at 5 nM
(3S)-N,3-dihydroxy-4-[(4-(4-chlorobenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
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50% inhibition at 0.88 nM, selective for enzyme
(3S)-N,3-dihydroxy-4-[(4-(4-methylbenzoxy)phenyl)sulfonyl]tetrahydro-2H-pyran-3-carboxamide
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50% inhibition at 1.3 nM
(3S,3'S)-astaxanthin
i.e. 3S,3S-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
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-
(4R)-1-[4-(4-fluorophenoxy)benzyl]-N-hydroxy-2-oxoimidazolidine-4-carboxamide
-
-
(E)-2-(4-(2-(biphenyl-4-yl)vinyl)-N-isopropoxyphenylsulfonamido)-N-hydroxyacetamide
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(R)-2-(4'-(4-chlorobenzyloxy)-N-isopropoxybiphenyl-4-ylsulfonamido)-N-hydroxy-3-methylbutanamide
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-(1-cyclohexanecarbonyl-piperidin-4-yl)-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-(1-iso-propylcarbamoyl-piperidin-4-yl)-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2,2-dimethylpropionyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2,2-dimethylpropyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(2-methylpropane-1-sulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(3,3-dimethylbutyryl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(benzenesulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(methane-1-sulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(phenylmethanesulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(propane-1-sulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(propane-2-sulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(tetrahydropyran-4-carbonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-benzylpiperidin-4-yl]-acetic acid
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(R)-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-iso-butylpiperidin-4-yl]-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-diethylcarbamoylpiperidin-4-yl)-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-iso-butyl-piperidin-4-yl)-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-isopropylcarbamoyl-piperidin-4-yl)-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-(1-tertbutylcarbamoyl-piperidin-4-yl)-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-[1-(benzenesulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4'-methoxyphenyl)-thiophene-2-sulfonylamino]-[1-(toluene-4-sulfonyl)-piperidin-4-yl]-acetic acid
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(R)-[5-(4-ethoxyphenyl)-thiophene-2-sulfonylamino]-[1-(butane-1-sulfonyl)-piperidin-4-yl]-acetic acid
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1,5-anhydro-2,3-dideoxy-3-[[4-(2,4-dichlorophenoxy)phenyl]sulfonyl]-4-C-(hydroxycarbamoyl)-D-threo-pentitol
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(1-hydroxyethyl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(1-methoxyethyl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(2-methoxyphenyl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(2-phenylethyl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(propan-2-yl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyrazin-2-yl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyridin-2-yl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyridin-4-yl)piperazin-1-yl]piperidine-4-carboxamide
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1-(4-[[4-(hydroxycarbamoyl)tetrahydro-2H-pyran-4-yl]sulfonyl]phenyl)-N,N-bis[4-(pyrimidin-4-yl)piperazin-1-yl]piperidine-4-carboxamide
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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
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1-acetyl-4-hydroxypyrrolidine-2-carboxylic acid
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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
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1-cyclopropyl-4-[[4-(4-[[4-(2,3-dimethylphenyl)piperazin-1-yl]carbonyl]piperidin-1-yl)phenyl]sulfonyl]-N-hydroxypiperidine-4-carboxamide
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1-cyclopropyl-N-hydroxy-4-([4-[4-(4-methoxyphenyl)piperazin-1-yl]phenyl]sulfonyl)piperidine-4-carboxamide
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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
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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
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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
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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
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comparison of selectivity with other matrix metalloproteinases
1-[4-(3-methoxyphenoxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
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comparison of selectivity with other matrix metalloproteinases
1-[4-(4-chlorophenoxy)phenyl]-1,7,9-triazaspiro[4.5]decane-2,6,8,10-tetrone
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comparison of selectivity with other matrix metalloproteinases
2,3-dihydro-1,4-benzodioxine-2-carboxylic acid
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binding structure, modelling, overview
2,3-dihydro-1,4-benzodioxine-5-carboxylic acid
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binding structure, modelling, overview
2-(2-[(2-chlorobenzoyl)amino]-1,3-thiazol-4-yl)acetic acid
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binding structure, modelling, overview
2-(4'-(4-chlorobenzyloxy)-N-isopropoxybiphenyl-4-ylsulfonamido)-N-hydroxyacetamide
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2-(5-((4-butylphenyl)ethynyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
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2-(5-(4-ethylphenyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
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2-(5-(4-fluorophenyl)-N-isopropoxythiophene-2-sulfonamido)-N-hydroxyacetamide
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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
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2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
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2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
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2-fluoro-N-hydroxy-6-([4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl]sulfonyl)benzamide
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2-[benzyl[(4-methoxyphenyl)sulfonyl]amino]-N-hydroxy-3,5-dimethylbenzamide
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WAY- 152177
2-[[(4'-chlorobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
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2-[[(4'-cyanobiphenyl-4-yl)oxy]methyl]-N-hydroxy-4-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)butanamide
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2-[[(4'-[[(5-bromo-4-methoxy-3-methyl-1-benzofuran-2-yl)carbonyl]amino]biphenyl-4-yl)sulfonyl]methyl]-3-methylbutanoic acid
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2-[[[4-(4-chlorophenoxy)phenyl]sulfonyl](methyl)amino]-N-hydroxy-3-[(4-methylpiperazin-1-yl)methyl]benzamide
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3-(carboxymethyl)-2-methylenepentanedioic acid
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binding structure, modelling, overview
4-((R)-carboxy-[5-[4'-(2-methoxyethoxy)-phenyl]-thiophene-2-sulfonylamino]-methyl)-piperidine-1-carboxylic acid iso-propyl ester
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4-(3-[3-[3-(3,4-difluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]prop-2-yn-1-yl]phenyl)butanoic acid
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4-(4-[[(3R)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyridin-4-ylmethyl)benzamide
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4-(4-[[(3R)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyrimidin-4-ylmethyl)benzamide
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4-(4-[[(3S)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyridin-4-ylmethyl)benzamide
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4-(4-[[(3S)-3-hydroxy-1-azabicyclo[2.2.2]oct-3-yl]ethynyl]phenoxy)-N-(pyrimidin-4-ylmethyl)benzamide
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4-(4-[[5-(2-ethoxyethyl)-2,4,6-trioxohexahydropyrimidin-5-yl]oxy]phenoxy)-N-(2-fluorobenzyl)benzamide
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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
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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
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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
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50% inhibition at 0.40 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-8, MMP-12
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
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4-([4-[4-(2,4-dimethylphenyl)piperazin-1-yl]phenyl]sulfonyl)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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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
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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
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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
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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
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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
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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
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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
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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
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4-([5-[2-(benzylcarbamoyl)-6-methylpyridin-4-yl]-2H-tetrazol-2-yl]methyl)cyclohexanecarboxylic acid
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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
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4-([[4-(4-fluorophenoxy)phenyl]sulfonyl]amino)-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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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-[(4-[3-[(2,2-dimethylpentanoyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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4-[(4-[3-[(2,4-dimethylbenzoyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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4-[(4-[3-[(cyclohexylcarbonyl)amino]propoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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4-[(4-[3-[4-(dimethylamino)phenyl]-3-oxopropoxy]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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4-[(4-[4-[(1,3-diethenyl-1,3-dimethyltriazan-2-yl)carbonyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxytetrahydro-2H-pyran-4-carboxamide
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-
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
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4-[(4-[4-[bis(3,5-dimethylpiperidin-1-yl)carbamoyl]piperidin-1-yl]phenyl)sulfonyl]-N-hydroxy-1-(2-methoxyethyl)piperidine-4-carboxamide
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4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
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4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
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4-[(5-[2-[(3,4-difluorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
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4-[(5-[2-[(3-chloro-4-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
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4-[(5-[2-[(3-chlorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
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4-[(5-[2-[(3-cyanobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
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4-[(5-[2-[(3-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
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4-[(5-[2-[(3-fluorobenzyl)carbamoyl]-6-methylpyridin-4-yl]-2H-tetrazol-2-yl)methyl]cyclohexanecarboxylic acid
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4-[(5-[2-[(3-fluorobenzyl)carbamoyl]pyridin-4-yl]-2H-tetrazol-2-yl)methyl]benzoic acid
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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-[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-[(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-[[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-(5-chloropyridin-2-yl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
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-(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
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
-
cilostazol
docking-based screening of existing drugs and binding free-energy calculation suggests eltrombopag, cilostazol and domperidone as potential MMP-13 inhibitors
clodronate
-
77% inhibition at 0.4 mM and physiological Ca2+-concentration, 35.7% inhibition at 0.4 mM and high Ca2+-concentration
domperidone
docking-based screening of existing drugs and binding free-energy calculation suggests eltrombopag, cilostazol and domperidone as potential MMP-13 inhibitors
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-3-[[(6-oxo-1,6-dihydropyridin-3-yl)methyl]carbamoyl]-1H-pyrazol-5-yl)-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
-
-
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
mannose-6-phosphate/insulin-like growth factor 2 receptor
-
inhibition of enzyme induction by TGFbeta1 in chondrocytes
-
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
N,N'-bis(4-fluoro-3-methylbenzyl)pyrimidine-4,6-dicarboxamide
50% inhibition at 8 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-(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-([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-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-5-(4-methoxyphenyl)thiophene-2-sulfonamido)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-(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-[(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-[(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-[(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-[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-[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-[[(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-({4'-[(4-chlorobenzyl)oxy]biphenyl-4-yl}sulfonyl)-N-hydroxy-N2-(propan-2-yloxy)glycinamide
-
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
-
-
N2-[(6-ethoxynaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
N2-[(6-ethylnaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
N2-[(7-ethoxynaphthalen-2-yl)sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
N2-[2-(dimethylamino)ethyl]-N-hydroxy-N2-(naphthalen-2-ylsulfonyl)-D-valinamide
-
-
N2-[[6-(benzyloxy)naphthalen-2-yl]sulfonyl]-N-hydroxy-N2-(3-methylbutyl)-D-valinamide
-
-
O-tert-butyl-N-hydroxy-N2-(3-methylbutyl)-N2-(naphthalen-2-ylsulfonyl)-D-serinamide
-
-
P53
-
down-regulation of enzyme expression, possibly contributes to the dysregulation of the enzyme observed in cancer
tissue matrix metalloproteinase inhibitor hybrid N.TIMP-1/C.TIMP-2
-
complex formation is not affected by the C-terminal domain of the enzyme, inhibition mechanism, wild-type enzyme and enzyme fragment 249-451
-
tissue matrix metalloproteinase inhibitor-1
-
in a ratio of enzyme to inhibitor of 1:1
-
tissue matrix metalloproteinase inhibitor-2
-
in a ratio of enzyme to inhibitor of 1:1
-
tissue matrix metalloproteinase inhibitor-3
-
fast inhibition, in a ratio of enzyme to inhibitor of 1:1
-
transforming growth factor-beta1
-
i.e. TGFbeta1, accelerates the decay of the enzymes mRNA and decreased enzyme expression in osteoblasts
-
-
comparison of selectivity with other matrix metalloproteinases
-
4-([6-[(4-methoxybenzyl)carbamoyl]-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl]methyl)benzoic acid
-
a less potent MMP13 inhibitor
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
inhibitor of MMP-13 having no activity against MMP-1 (collagenase-1) or tumor necrosis factor-R converting enzyme
4-[(R)-carboxy-[5-(4'-ethoxyphenyl)-thiophene-2-sulfonylamino]-methyl]-piperidine-1-carboxylic acid iso-propyl ester
-
orally active carboxylic acid-derived MMP-13 inhibitor with subnanomolar potency is identified and tested in a rat intraarticular injection model. Greater than 20000fold in vitro selectivity for MMP-13 over MMP-1 is achieved
4-[[1-methyl-2,4-dioxo-6-(3-phenylprop-1-yn-1-yl)-1,4-dihydroquinazolin-3(2H)-yl]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
-
noncompetitive, extremely selective for inhibition of MMP13 over all other MMPs
4-[[1-methyl-2,4-dioxo-6-(3-phenylprop-1-yn-1-yl)-1,4-dihydroquinazolin-3(2H)-yl]methyl]benzoic acid
-
-
-
discovery and optimization of potency and selectivity of the non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information, binding mode, overview. 1 binds in the active site region despite not interacting with the catalytic zinc
5-(4-chlorophenyl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
-
-
a specific MMP-13 inhibitor, inhibits also the metastatic activity of chloramphenicol-treated cells
the intact peptide backbone scaffold is optimum to fix the inhibitor into the rigid environment of the MMP13 binding site
50% inhibition at 72 nM
N,N'-bis(3-methylbenzyl)pyrimidine-4,6-dicarboxamide
-
extremely selective for inhibition of MMP13 over all other MMPs
N,N'-bis(3-methylbenzyl)pyrimidine-4,6-dicarboxamide
-
a MMP13-specific inhibitor
50% inhibition at 6600 nM
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
-
i.e. PF152, a potent and highly selective MMP-13 inhibitor, that binds the S1' active site pocket of the enzyme, is not a ligand to the catalytic zinc atom, and dose-dependently decreases cartilage degradation ex vivo. PF152 treatment of osteoarthritis dogs reduces cartilage lesions and decreased biomarkers of type II collagen and aggrecan degradation
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
-
i.e. PF152, a non-hydroxamic acid and a potent and highly selective MMP-13 inhibitor, that binds the S1' active site pocket of the enzyme and is not a ligand to the catalytic zinc atom
-
50% inhibition at 1.3 nM, comparison with inhibition of matrix metalloproteinases MMP-2, MMP-14
N2-[(4'-bromobiphenyl-4-yl)sulfonyl]-N-hydroxy-D-valinamide
-
a nonselective inhibitor
-
a small molecule preferential inhibitor of MMP13, the compound is able to potently inhibit the release of type II collagen degradation peptides from human osteoarthritis articular cartilage explants
tissue matrix metalloproteinase inhibitor TIMP-1
-
complex formation is promoted by the C-terminal domain of the enzyme, inhibition mechanism, wild-type enzyme and enzyme fragment 249-451
-
tissue matrix metalloproteinase inhibitor TIMP-2
-
complex formation is not affected by the C-terminal domain of the enzyme, inhibition mechanism, wild-type enzyme and enzyme fragment 249-451
-
tissue matrix metalloproteinase inhibitor TIMP-3
-
complex formation is promoted by the C-terminal domain of the enzyme, inhibition mechanism, wild-type enzyme and enzyme fragment 249-451
-
-
development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors
-
additional information
-
synthesis of a series of phenyl piperidine alpha-sulfone hydroxamate derivatives, utilizing a combination of solution-phase and resin-bound library technologies, to afford compounds that are potent and highly selective for MMP-13, selectivity analysis compared to other MMPs, overview
-
additional information
-
development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors
-
additional information
-
development and optimization of potent 3,4-disubstituted benzofuran P1' MMP-13 inhibitors, overview
-
additional information
-
development of MMP-13 selective isonipecotamide alpha-sulfone hydroxamate inhibitors, overview
-
additional information
-
selectivity and metabolic stability of non-zinc-chelating MMP-13 inhibitors, overview
-
additional information
discovery of (pyridin-4-yl)-2H-tetrazole as a scaffold to identify highly selective MMP-13 inhibitors for the treatment of osteoarthritis
-
additional information
design, synthesis and biological evaluation of selective matrix metalloproteinase-13 N-O-isopropyl sulfonamido-based hydroxamate inhibitors as potential therapeutic agents for osteoarthritis, docking study and molecular modelling, overview
-
additional information
-
MMP-13 activity is not directly inhibited by the imidazo[5,1-c][1,4]thiazine derivative ITZ-1
-
additional information
-
structure-function relationships of different inhibitor types, overview. No inhibition by 27, i.e. CGS27023A
-
additional information
-
selective inhibition of MMP-13 may be achieved by targeting the hemopexin domain of the protease, which is critical for substrate specificity, systematic cheminformatics-based drug design with virtual screening, overview
-
additional information
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no inhibition of MMP-13 by MMP-3 inhibitor N-isobutyl-N-[4-methoxyphenylsulphonyl] glycyl hydroxamic acid or by doxycycline
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additional information
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orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. Two series, quinazolinones and pyrido[3,4-d]pyrimidin-4-ones, that are potent and specific MMP-13 inhibitors, some of which are orally bioavailable. These specific MMP-13 inhibitors, occupying the unique S1'-specificity pocket, do not bind to the Zn2+ ion, effectively preventing cartilage damage in animal models of osteoarthritis without inducing musculoskeletal side effects when given at extremely high doses to rats
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additional information
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development of MMP-13 inhibitors mechanistically distinct from previously reported broad-spectrum MMP inhibitors with improved selectivity and pharmacokinetics. Chondroprotective effect of MMP-13-selective inhibitors. Effect of MMP-13 inhibition on cartilage degradation in the rat medial meniscal tear model of osteoarthritis, overview
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additional information
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MMP-13 activity is not directly inhibited by the imidazo[5,1-c][1,4]thiazine derivative ITZ-1
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